Relevant bibliographies by topics / Agonistes de la dopamine

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Academic literature on the topic 'Agonistes de la dopamine'

Author: Grafiati
Published: 4 June 2021
Last updated: 1 February 2022

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Journal articles on the topic "Agonistes de la dopamine"

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Cumming, Paul, Dean F. Wong, Nicholas Gillings, John Hilton, Ursula Scheffel, and Albert Gjedde. "Specific Binding of [11C]Raclopride and N-[3H]Propyl-Norapomorphine to Dopamine Receptors in Living Mouse Striatum: Occupancy by Endogenous Dopamine and Guanosine Triphosphate–Free G Protein." Journal of Cerebral Blood Flow & Metabolism 22, no. 5 (2002): 596–604. http://dx.doi.org/10.1097/00004647-200205000-00011.

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According to the ternary complex model of G-protein linkage to receptors, agonists increase the affinity of the receptors for the G protein. The model predicts that an endogenous agonist's constant of inhibition toward an agonist radioligand is lower than that toward an antagonistic radioligand. The authors hypothesized that competition from endogenous dopamine in striatum of living mice should have a greater effect on the binding of the D2,3 partial agonist N-[3H]propylnorapomorphine than on the binding of the D2,3 antagonist [11C]raclopride. The baseline binding potential ( pB(0)), defined as the ratio of bound-to-unbound ligand in the absence of competition from endogenous dopamine, was simultaneously measured in mouse striatum for [11C]raclopride ( pB(0) = 8.5) and N-[3H]propylnorapomorphine ( p′B(0) = 5.3). The baseline was established by treatment with α-methyl- p-tyrosine and reserpine. Relative to these baseline values in saline-treated mice, the pB of N-[3H]propylnorapomorphine decreased 52% whereas the pB of [11C]raclopride decreased only 30%, indicating greater sensitivity of the former compound to inhibition by synaptic dopamine. Furthermore, amphetamine decreased the pB of N-[3H]propylnorapomorphine to a greater extent (73%) than that of [11C]raclopride (43%) relative to the reserpine condition. For both radioligands, the occupancy of the dopamine receptors by endogenous agonist obeyed Michaelis-Menten kinetics over a wide range of agonist concentrations established by the pharmacologic treatments. The apparent inhibition constant of endogenous dopamine depended on the dopamine occupancy and decreased to a value 1.66 times greater for N-[3H]propylnorapomorphine than for [11C]raclopride at its highest occupancies. The results are consistent with the hypothesis that agonist binding is more sensitive than antagonist binding to competition from endogenous dopamine. Therefore, dopamine agonist ligands may be superior to benzamide antagonist ligands for the estimation of dopamine receptor occupancy by endogenous synaptic dopamine. The analysis of the effect of dopamine occupancy on the inhibition of N-[3H]propylnorapomorphine binding indicated a limited supply of G protein with a maximum ternary complex fraction of 40% of maximum agonist binding capacity.
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Binde, Caroline D., Ingunn F. Tvete, and Marianne Klemp. "Time until Need for Levodopa among New Users of Dopamine Agonists or MAO-B Inhibitors." Parkinson's Disease 2021 (July 1, 2021): 1–7. http://dx.doi.org/10.1155/2021/9952743.

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Objective. To investigate the use of dopamine agonists and monoamine oxidase type B (MAO-B) inhibitors in the Norwegian population, between 1 July 2006 and 31 December 2016. Our primary endpoint was time until need for levodopa among new monotherapy users of dopamine agonists and MAO-B inhibitors. Methods. A prospective cohort study including all patients, aged 50 years or above, who had at least one prescription for a dopamine agonist or a MAO-B inhibitor dispensed in the study period. We used data from the Norwegian Prescription Database (NorPD). As we wished to focus on new Parkinson patients, we excluded patients who had levodopa dispensed less than 180 days prior to their first dopamine agonist or MAO-B inhibitor redemption. We explored the demographics and the time until monotherapy was insufficient treatment (defined as need for levodopa prescription). Results. We included 22958 new monotherapy users. Of these, 22108 used dopamine agonists and 850 used MAO-B inhibitors. The mean number of days until the first prescription of levodopa was dispensed was higher among the dopamine agonist users (621 days) compared to the MAO-B inhibitor users (352 days). The proportion of dopamine agonist users who started levodopa treatment during the study period was less than 7%, while the corresponding proportion of MAO-B inhibitor users was almost 59%. Conclusions. We found that new dopamine agonist users had a much greater delay in the need for levodopa than new MAO-B inhibitor users. It seems to be beneficial to initiate treatment with dopamine agonists when starting pharmacological treatment for new Parkinson patients.
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Molitch, Mark E. "Dopamine agonists and antipsychotics." European Journal of Endocrinology 183, no. 3 (2020): C11—C13. http://dx.doi.org/10.1530/eje-20-0607.

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There can potentially be a number of clinical interactions that could adversely affect patient outcomes in a patient with a prolactinoma and psychiatric disease that might require antipsychotic and dopamine agonist treatment. Dopamine agonists stimulate the dopamine D2 receptor, resulting in a decrease in prolactin (PRL) levels and in prolactinoma size but action on dopamine receptors in the meso-limbic system may rarely cause psychosis and more commonly cause impulse control disorders. The psychiatric benefits of antipsychotic agents involve blocking the D2 and other dopamine receptors but this blockade often also causes hyperprolactinemia. In patients with macroprolactinomas and psychosis, observation, estrogen/progestin replacement, and surgery can be considered in addition to dopamine agonists. In those who require dopamine agonists for PRL and tumor size control, the introduction of antipsychotics may blunt this effect, so that higher doses of the dopamine agonists may be needed. Alternatively, antipsychotics that have less of a blocking effect at the D2 receptor, such as aripiprazole, can be tried, if appropriate. For patients already on antipsychotic drugs who are found to have a macroprolactinoma for which dopamine agonists are required, dopamine agonists can be initiated at low dose and the dose escalated slowly. However, such patients require careful monitoring of psychiatric status to avoid the rare complication of exacerbation of the underlying psychosis. Again, if appropriate, use of antipsychotics that have less of a blocking effect at the D2 receptor may allow lower doses of dopamine agonists to be used in this situation.
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Oh, Michael C., and Manish K. Aghi. "Dopamine agonist–resistant prolactinomas." Journal of Neurosurgery 114, no. 5 (2011): 1369–79. http://dx.doi.org/10.3171/2010.11.jns101369.

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The authors' object in this paper was to review the definition, epidemiology, biology, resistance mechanisms, and treatment options for dopamine agonist–resistant prolactinomas (DARPs). Prolactinomas are relatively unique among primary brain tumors in that medical treatment alone using dopamine agonists carries a high probability of disease control or even radiographic and endocrine remission, and thus has replaced surgery as the first line of therapy. Unfortunately, slightly less than 10% of patients with prolactinomas do not experience normalization of their prolactin levels in response to dopamine agonists, and harbor tumors that are resistant to dopamine agonist therapy. A literature review underscores that in male patients these DARPs are more likely to be invasive macroadenomas than dopamine agonist–responsive prolactinomas and that they are also more angiogenic, more proliferative, and more likely to exhibit cellular atypia. Estrogen receptor antagonists and temozolomide are the most commonly applied medical therapies in cases in which resection and radiosurgery have not induced remission of the hyperprolactinemia. Dopamine agonist–resistant prolactinomas exhibit aggressive behavior and tend to be large, invasive, hyperangiogenic tumors with high mitotic indices, which makes their management via surgery, radiosurgery, or alternative medical therapies challenging, thus underscoring the need for novel medical therapies or treatment regimens that target these lesions.
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Robertson, H. A. "Synergistic Interactions of D1- and D2-Selective Dopamine Agonists in Animal Models for Parkinson’s Disease: Sites of Action and Implications for the Pathogenesis of Dyskinesias." Canadian Journal of Neurological Sciences / Journal Canadien des Sciences Neurologiques 19, S1 (1992): 147–52. http://dx.doi.org/10.1017/s0317167100041536.

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ABSTRACT:The addition of a D2 agonist such as bromocriptine to L-Dopa therapy can often improve the response of patients with Parkinson’s disease dramatically. Simultaneous activation of D1 and D2 dopamine receptors can produce a synergistic effect on locomotion in rats and primates. However, despite the importance of this addition of a D2 agonist to the D1/D2 agonist L-Dopa, little is known of the sites of action of these agents. Recent work suggests that, in addition to D1 and D2 dopamine receptor sites in the striatum (caudate-putamen), L-Dopa and D1 agonists have important effects at D1 dopamine receptors in the substantia nigra. Animal experiments suggest that D1 and D2 dopamine receptor agonists probably also affect different outflow pathways from the striatum. An understanding of these pathways and how dopamine agonists affect them gives insight into some of the clinical problems experienced in treating Parkinson’s disease (the “on-off phenomenon, for example). D1/D2 dopamine receptors also differentially affect gene expression and regulation in the striatum. An understanding of the anatomical and biochemical location of the actions of dopamine receptor agonists will be important in maximizing the beneficial effects and minimizing the side-effects of both presently-used drugs and new treatments.
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Berretta, S., H. A. Robertson, and A. M. Graybiel. "Dopamine and glutamate agonists stimulate neuron-specific expression of Fos-like protein in the striatum." Journal of Neurophysiology 68, no. 3 (1992): 767–77. http://dx.doi.org/10.1152/jn.1992.68.3.767.

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1. The monoamine dopamine and the amino acid glutamate are major neurotransmitters in the basal ganglia implicated in the normal functions of the striatum and in extrapyramidal disease states. To study the effects of these neurotransmitters on gene transcription in striatal neurons, we treated rats with dopamine (monoamine) agonists and with glutamate agonists and monitored the induction of Fos-like protein in striatal neurons. We administered the indirect monoamine agonists cocaine and amphetamine intraperitoneally and gave the glutamate agonist quinolinic acid by direct intrastriatal injection. We identified the phenotypes of the responsive neurons by immunohistochemistry and by enzyme histochemistry in double staining protocols. 2. Both the indirect monoamine agonists and the glutamate receptor agonist stimulated rapid nuclear expression of Fos-like protein in specific classes of striatal neurons. The induction by cocaine and amphetamine was blocked by pretreatment with the dopamine D1-like receptor antagonist SCH23390, and the induction by quinolinic acid was blocked by pretreatment with MK-801, a noncompetitive antagonist of the N-methyl-D-aspartate (NMDA) glutamate receptor. 3. The monoamine and glutamate agonists both induced Fos-like protein exclusively in striatal neurons that constitutively expressed the protein phosphatase inhibitor DARPP-32 (dopamine and cAMP-regulated phosphoprotein). 4. The dopamine agonists failed to induce detectable Fos-like protein in striatal neurons expressing enkephalin, even though many such neurons expressed DARPP-32. By contrast, many enkephalinergic neurons did express Fos-like protein in response to glutamatergic stimulation. 5. Glutamate agonist stimulation, but not dopamine agonist stimulation, induced Fos-like protein in a subpopulation of striatal interneurons, namely, a group of neurons exhibiting NADPH-diaphorase activity. 6. These findings suggest that stimulation of dopamine D1-like receptors (or related monoamine receptors) and glutamate NMDA receptors activates neuron-specific programs of immediate-early gene expression in the striatum. Our findings further suggest that monoamine and glutamate may act cooperatively at the transcriptional level on a functionally defined subset of striatal neurons.
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Davis, J. P., and R. M. Pitman. "Characterization of receptors mediating the actions of dopamine on an identified inhibitory motoneurone of the cockroach." Journal of Experimental Biology 155, no. 1 (1991): 203–17. http://dx.doi.org/10.1242/jeb.155.1.203.

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1. The effects of a number of dopaminergic agonists and antagonists upon the soma of a prothoracic inhibitory motoneurone of the cockroach (Periplaneta americana) have been recorded under voltage-clamp conditions. 2. Dopamine generates inward currents that are extremely voltage-dependent: currents increase rapidly at membrane potentials more negative than about −120 to −150 mV and also show a peak at membrane potentials of approximately −20 mV. As a result of this voltage-dependence, dopamine induces a region of negative resistance in the current-voltage relationship of the neurone. 3. The dopaminergic agonists apomorphine, bromocriptine, ergometrine and A-6,7-DTN mimic the action of dopamine on this neurone, all having a similar voltage-dependence to that of dopamine. The selective D-1 receptor agonist SK&F82526 and the D-2 agonist LY 171555, however, were both inactive on the preparation. 4. Responses to dopamine were suppressed by a number of D-1 and D-2 receptor antagonists, indicating that the pharmacological profile of the dopamine-sensitive receptor in this insect preparation is different from that of vertebrate dopamine receptors.
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&NA;. "Dopamine agonists." Reactions Weekly &NA;, no. 798 (2000): 7–8. http://dx.doi.org/10.2165/00128415-200007980-00020.

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Factor, Stewart A. "DOPAMINE AGONISTS." Medical Clinics of North America 83, no. 2 (1999): 415–43. http://dx.doi.org/10.1016/s0025-7125(05)70112-7.

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Tuite, Paul, and Brenda Ebbitt. "Dopamine Agonists." Seminars in Neurology 21, no. 01 (2001): 009–14. http://dx.doi.org/10.1055/s-2001-13114.

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Dissertations / Theses on the topic "Agonistes de la dopamine"

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Vasse, Marc. "Analyse des rôles des sous-types de récepteurs de la dopamine dans différents comportements chez la souris." Rouen, 1988. http://www.theses.fr/1988ROUES042.

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Les rôles des récepteurs dopaminergiques D-1, D-2 et D-4 dans différents comportements (verticalisation, reniflements, lèchements, morsures, toilettage) spontanés ou stéréotypés sont étudiés chez la souris à l'aide d'un agoniste non sélectif (apomorphine) ou d'agonistes sélectifs des récepteurs D-1 (SK&F 38393) ou D-2 (RU 24926, LY 171555) et d'antagonistes non sélectifs, sélectifs des récepteurs D-1 (SCH 23390) ou D-2 (métoclopramide), ou discriminant les récepteurs D-2 des récepteurs D-4 (sulpiride, amisulpride, RIV 2093). Les récepteurs D-1 et D-2 semblent impliqués dans l'expression de ces différents comportements alors que les récepteurs D-4 semblent responsables de leur inhibition. La comparaison des modifications de l'activité adénylate cyclase liée aux récepteurs D-1 et des comportements stéréotypés induits par l'apomorphine lors d'une déplétion dopaminergique induite par la réserpine et l'alpha méthyl paratyrosine suggère un renforcement de la stimulation des récepteurs D-1 dans ces conditions expérimentales. L'analyse des résultats obtenus avec les 12 antagonistes dopaminergiques étudiés suggère que l'évaluation simultanée des 5 comportements permet une classification des neuroleptiques en fonction de leur activité à l'égard des différents sous-types de récepteurs de la dopamine. Le rôle potentiel du blocage de chacun des sous-type de récepteurs de la dopamine dans l'activité antipsychotique des neuroleptiques est discuté.
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Cendrès-Bozzi, Christophe. "Troubles du cycle veille/sommeil liés à la maladie de Parkinson : modèle animal, mécanismes et approches thérapeutiques." Thesis, Lyon 1, 2011. http://www.theses.fr/2011LYO10081.

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Les troubles du sommeil, tels que la somnolence diurne excessive et les attaques narcoleptiques, sont fréquemment observés chez les patients Parkinsoniens. Malgré de nombreux efforts cliniques à l’échelle mondiale, il reste à déterminer si ces troubles sont causés par les lésions neuronales dopaminergiques (DAergiques) ou non DAergiques, par les troubles moteurs ou par les effets délétères des médicaments anti-parkinsoniens. Par une approche pluridisciplinaire (analyse EEG; mesure de l’activité locomotrice; tests pharmacologiques; immunohistochimie) chez le félin traité au MPTP, nous avons étudié la corrélation possible entre perte DAergique et troubles du cycle veille-sommeil (V/S). Le MPTP (5mg/kg/jour x5, i.p.) induit en période aiguë, une hypersomnie en sommeil lent (SL), une suppression du sommeil paradoxal (SP), ainsi qu’une diminution de la locomotion et une difficulté à l’initiation des mouvements. Les agonistes DAergiques (L-dopa; ropinirole) empêchent l’hypersomnie en SL de façon transitoire. Durant la période chronique, les taux d’éveil et de SL reviennent à la normale. Le SP augmente transitoirement et s’associe à des épisodes narcoleptiques. Les analyses ex-vivo révèlent une diminution du marquage TH (corps cellulaire de la substance noire ; fibres du striatum). Le marquage des neurones cholinergiques (cerveau antérieur basal et tegmentum mésopontique) semblent inchangée. Nos résultats montrent donc que le MPTP induit chez le félin des symptômes moteurs et des troubles du sommeil proches de ceux observés chez les patients parkinsoniens. Cette étude suggère également une corrélation possible entre les troubles du cycle V/S et la perte des cellules DAergiques
Motors disorders are not the only symptoms of Parkinson disease (PD), and sleep disorders such as somnolence and narcolepsy are frequently reported in PD patients. Despite much investigation worldwide, it remains unknown whether these disorders are caused by dopaminergic (DArgic), non-DArgic neural lesions, nocturnal motor disability or deleterious effect of anti-PD drugs. Using multiple experimental approaches (EEG and sleep-wake recordings/pharmacological dosing / immunohistochemistry) in cats treated with MPTP, which causes DArgic neuronal loss, we have studied the possible correlation between the induced effects on the sleep-wake (S/W) cycle and those on DArgic neurons. MPTP (5mg/kg/day x 5, i.p.) caused, during the acute period, a slow wave sleep hypersomnia (SWS, up to 80% of recorded time) and a suppression of paradoxical sleep (PS), accompanied with pronounced behavioural somnolence, marked decrease in locomotion and difficulty to initiate movements. DArgic agonists L-dopa and ropinirole transiently prevented hypersomnia in SWS. During the chronic period, whereas the amount of W and SWS returned to control, PS transiently increased, associated with narcolepsy-like episodes. Ex-vivo analyses revealed marked decrease in TH labelling (cell bodies in the substantia nigra and terminal-like dots in the striatum) whereas cholinergic neurons in the basal forebrain and mesopontine-tegmentum seemed unchanged. Thus, MPTP treated cats showed major signs of motor and S/W disorders similar to those seen in PD patients and so could serve as useful animal model. Our results also suggest a possible correlation/causality between the MPTP-induced S/W disorders and DArgic cell loss
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Haddjeri, Alexis. "Robustesse du phénotype électrique des neurones dopaminergiques de la substance noire compacte à la délétion des canaux potassium Kv4.3 et SK3." Thesis, Aix-Marseille, 2019. http://theses.univ-amu.fr.lama.univ-amu.fr/191211_HADDJERI_482kf140lioz770fao837wbiyys_TH.pdf.

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Ce travail de thèse concerne la caractérisation des variations du phénotype électrique des neurones DA de la SNc chez les animaux KOs SK3 et Kv4.3, en conditions physiologiques et physiopathologiques. Dans une première étude, j'ai analysé un grand nombre de paramètres électrophysiologiques chez ces animaux. En association avec des blocages pharmacologiques aigus de ces canaux, la délétion chronique du canal Kv4.3 conduit à une variation phénotypique semblable au blocage aigu du canal tandis que la délétion du canal SK3 semble compensée par d'autres canaux (notamment le SK2). Dans une seconde étude, préliminaire, nous avons utilisé un modèle de lésion bilatérale partielle pour étudier les répercussions comportementales et électrophysiologiques de la délétion du canal SK3 dans le développement de la maladie de Parkinson. Nos résultats suggèrent qu’en condition "Parkinson", la suppression constitutive du canal SK3 est associée à un léger effet anxiolytique, à l’abolition de l’hypersensibilité aux agonistes dopaminergiques mais aussi à des déficits de l’apprentissage moteur. Du point de vue électrophysiologique, les neurones DA de la SNc présentent un profil de décharge régulier similaire à la condition non-traitée. Ces deux études suggèrent que l'activité électrique des neurones DA de la SNc présente une robustesse partielle et variable à la délétion des canaux potassium qui peut être révélée dans des contextes physiologiques et physiopathologiques. Ce travail devrait permettre de mieux comprendre comment les mutations génétiques de canaux ioniques pourraient altérer la vulnérabilité des neurones DA de la SNc dans le contexte de la maladie de Parkinson
During my PhD, I precisely characterized the variations in electrical phenotype of the SNc DA neurons in Kv4.3 and SK3 KO animals, in physiological and pathophysiological conditions. In a first study, I analyzed a large number of electrophysiological parameters in these animals Combined with acute pharmacological blockade of these ion channels, I showed that Kv4.3 chronic deletion leads to a phenotypic change similar to the one induced by acute blockade of the channel while SK3 deletion appears to be compensated by other ion channels (in particular SK2). Motor behavior testing of Kv4.3 and SK3 KO animals confirmed the robustness of SK3 animals and the absence of robustness of Kv4.3 animals. In a second preliminary study, we used a bilateral partial lesion model to assess the behavioral and electrophysiological consequences of SK3 deletion on Parkinson's disease development. Our results suggest that in "Parkinson's" conditions, the chronic deletion of SK3 channel is associated with a slight anti-anxiety effect, the suppression of dopaminergic agonist hypersensitivity but also with motor deficits. From an electrophysiological viewpoint, the SNc DA neurons display a pacemaking behavior similar to the untreated condition. These two studies suggest that SNc DA neuron activity displays a partial and variable robustness to potassium channel deletion (robust to SK3 deletion, sensitive to Kv4.3 deletion) that can be revealed in physiological and pathophysiological conditions. This work will help understanding how ion channel mutations may alter SNc DA neuron vulnerability in Parkinson's disease
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Ouachikh, Omar. "Effets motivationnels des agonistes dopaminergiques dans un modèle de rat ayant une lésion bilatérale de l'aire tegmentale ventrale." Thesis, Clermont-Ferrand 1, 2013. http://www.theses.fr/2013CLF1MM18.

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Le traitement médicamenteux de la maladie de Parkinson idiopathique (MPI) repose essentiellement,t sur la restauration de la transmission dopaminergique par la L-Dopa et par les agonistes dopaminergiques (DARAs) agissant sur les récepteurs dopaminergiques de la classe D2R et D3R. Cependant au cours du traitement apparaissent des comportements addictifs (addiction aux médicaments dopaminergiques, hyper-sexualité, addiction aux jeux, addiction aux achats impulsifs...). Ces troubles du comportement impulsifs (TCI) observés chez les patients parkinsoniens traités aux agonistes dopaminergiques ressemblent bien à ceux observés chez les utilisateurs chroniques de drogues d'abus telles que la morphine, les amphétamines ou la cocaïne. [...] Dans le but de comprendre la physiopathologie des manifestations addictives chez le patient parkinsonien, notre étude s'est proposée d'étudier les effets renforçateurs ou motivationnels des agonistes dopaminergiques chez l'animal dont l'ATV postérieur ou antérieure ont été bilatéralement lésés. Les manifestations addictives seront investies en utilisant le test de préférence de place conditionnée (PPC), un paradigme qui étudie l'effet motivationnel / renforçateur des agonistes utilisés. Une particularité de notre étude est qu'elle a été réalisée chez l'animal naïf sans être au préalable sensibilisé à une drogue d'abus. Son intérêt est de montrer l'effet direct des agonistes dopaminergiques sur le comportement recherché
Néant
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Helfenbein, Julie. "Développement des médicaments radiopharmaceutiques pour l'exploration des transporteurs de la dopamine et de la sérotomine dans le système nerveux central." Tours, 1999. http://www.theses.fr/1999TOUR4022.

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Les transporteurs des monoaminés sont impliqués dans des maladies neurodégéératives et neuropsychiatriques. Il est important de pouvoir explorer in vivo ces transporteurs pour le diagnostic et le suivi thérapeutique de ces maladies par scintigraphies pet ou spet. Ces techniques d'imagerie nécessitent le développement de radiologands spécifiques du transporteur étudié. La première partie de cettre thèse concerne le développement d'un radioligand pour l'exploration pet du transporteur de la dopamine (TDA) : le [76 Br] (E)-N-(3-bromoprop-2-ényl)-2β-Carbomethoxy-3β-(4'-tolyl) nortropane. Le [76 Br]PE2Br est obtenu en 7 étapes à partir du chlorhydrate de cocaine. Chez le rat et le singe, le [76Br]PE2Br s'accumule de manière spécifique dans le striatum, région riche en TDA. La deuzième partie concerne le développement de radioligands spécifiques du transporteur de la sérotonine (T5-HT). Dans cet objectif, nous avons entrepris des modifications structurales de la cocaine afin d'améliorer son affinité et sa spécificité pour le T5-HT. Nous avons introduit un groupement alkyle en position 4 et un atome d'iode en position 3 sur le noyau aromatique. Nous avons synthétisé 4 séries de composés : 2-carbométhoxy-3-(4-substituesphényl) tropanes, 2-carbométhoxy-3-(4-substituesphényl) nortropanes, 2-carbométhody-3-(3-iodo-4-substituesphényl) tropanes et 2-carbométhoxy-3(3-iodo-4-substituesphényl) nortropanes. Ces synthèses en 6 étapes utilisent la chimie des organométalliques, ainsi que des réactions stéréosélectives. La caractérisation biologique in vitro de tous ces composés permet de mettre en évidence les substituants favorisant l'interaction avec le T5-HT. Les composés qui présentent les meilleures caractéristiques in vitro ont été radiomarqués (I 1 2 5 ou C 1 1) pour réaliser des études in vivo. Ces radioligands se fixent dans les régions riches en T5-HT. Cependant les faibles rapports signal spécifique / bruit de fond limitent leur utilisation pour l'exploration du T5-HT
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Martin-Iverson, Mathew Thomas. "The effect of a dopamine antagonist and an agonist on rats’ perception of reward quantity : an examination of the anhedonia hypothesis." Thesis, University of British Columbia, 1985. http://hdl.handle.net/2429/25938.

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A procedure was developed to determine the effect of a dopamine (DA) antagonist (haloperidol) and a DA agonist (d-amphetamine) on rats' perceptions of the hedonic value of food. Eighteen rats were trained to discriminate between two quantities of sweet food pellets (1 and 4), in a forced-choice two-lever successive discrimination procedure. To control for non-specific perceptual effects of the treatments, the rats were also trained to discriminate between 1 and 4 tones. It was established that rats attended to the value of food, as well as the proportional differences in quantity, when discriminating food quantities. This was accomplished by altering the value of the food in two ways. Firstly, "hunger" was altered by changing the degree of food deprivation during testing. Secondly, unsweetened food pellets were introduced as probe cues. These two methods of altering the value of food pellets were utilized while quantity generalization gradients were determined, by presenting animals with 1,2, 3 and 4 numbers of stimuli as probe cues. Two measures were derived from these generalization gradients: the point of subjective equality (PSE), which is the calculated number of stimuli that would maintain responses equally distributed between the two levers, and the slope of the gradient. The PSE primarily reflects perceptual processes, while the slopes of the gradients provide an index of performance impairment. It was observed that decreasing the value of food by either decreasing food deprivation or reducing the sweetness of the food pellets resulted in the rats perceiving a given quantity of food as larger than before these treatments (decreased the food PSE). Neither altering food deprivation nor introducing novel tone probes had an effect on the numerical attributes of tones, as reflected by the tone PSE. Haloperidol (0.030, 0.50 and 0.083 mg/kg, i.p.) produced a statistically significant, but slight dose-dependent performance deficit, as reflected by the slope of the generalization gradients. It did not affect the perception of food pellet quantities at any dose, as reflected by the food PSE. Haloperidol decreased the number of tones a given quantity was perceived as by rats (increased the tone PSE). Amphetamine (0.25, 0.50 and 1.0 mg/kg, i.p.) decreased the perception of a given quantity of food (increased the food PSE) in a dose-dependent manner, without a significant effect on performance. Thus, amphetamine enhanced the hedonic value of food. Amphetamine also increased rats' perceptions of a given number of tones (decreased the tone PSE). It therefore appears that while d-amphetamine can enhance the perceived hedonic value of food, haloperidol has no effect on rats' perceptions of the hedonic value of food. Furthermore, evidence that DA systems are involved in the mechanism of an "internal clock" or "counter" was obtained.
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Gadjou, Caroline Honoré. "Recherche de nouvelles thérapies des toxicomanies : préparation d'antigènes dérivés des amphétamines et synthèse d'agonistes mixtes dopaminergiques D1 et D3." Paris 5, 2004. http://www.theses.fr/2004PA05P611.

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L'objectif de cette Thèse est la recherche de nouveaux traitements d'effets toxiques liés à la consommation de drogues : toxicité aigue͏̈ (overdose) due aux amphétamines dans la première partie et traitement de la dépendance dans la seconde. Compte tenu de la multiplicité des récepteurs impliqués dans les effets toxiques des amphétamines, une approche d'immunothérapie est envisagée dans ce travail. Les principales propriétés des amphétamines sont d'abord présentées : mécanismes d'action, relation structure activité. A ce niveau, l'influence de la chiralité sur l'activité biologique est plus particulièrement développée. De très nombreuses études suggèrent que l'énantiomère S des amphétamines est le plus toxique. La préparation des immunogènes est ensuite réalisée. Dans une première étape des haptènes dérivés des amphétamines de configuration S et des racémiques correspondants sont préparés. Les haptènes synthétisés sont ensuite couplés sur différentes protéines porteuses. Les anticorps produits à partir des immunogènes issus des haptènes dont le centre chiral est de configuration S reconnaissent plus fortement la (S)-méthamphétamine que le racémique. Nous avons au cours de ce travail, expérimenté plusieurs procédés de construction du squelette amphétaminique. La réduction par l'hydrure d'aluminium lithium du tosylate de dérivés du phénylalaninol constitue le procédé le plus efficace. Lorsque le phénylalaninol est protégé par un groupement tert-butyloxycarbonyle, ce groupement est transformé en groupement méthyle simultanément avec la réduction du tosylate. Dans la seconde partie de cette Thèse, des éléments portant sur l'implication du système dopaminergique dans le circuit de la récompense sont d'abord présentés. Ces données suggèrent l'intérêt thérapeutique d'agonistes dopaminergiques et plus particulièrement des agonistes D1 et D3 dans le traitement de la dépendance induite par les drogues. Dans cet optique les relations existant entre la structure et l'activité des agonistes dopaminergiques connus sont examinées. Nous avons synthétisé des agonistes mixtes (D1/D3) dopaminergiques en combinant des fragments présents dans les molécules décrites dans la littérature. L'affinité des produits préparés a ensuite été évaluée sur des récepteurs D2 de rat et D3 humains. Enfin la réponse fonctionnelle a été déterminée dans un test de mitogénèse. Parmi les molécules synthétisées, une molécule possédant une structure originale a montré une activité agoniste relativement élevée pour les récepteurs D3 dopaminergiques. Ce produit est en outre légèrement antagoniste au niveau des récepteurs D2. Ces premiers résultats, particulièrement prometteurs devrait encourager une étude plus complète de cette nouvelle série d'agonistes dopaminergiques
The objective is to search for new treatments against toxic/unwanted side effects resulting from drug consumption. In part one, we will examine treatments against amphetamine overdose and in part two we will review treatments against drug dependence. Given the large number of receptors involved in harmful side effects generated by amphetamine consumption, immunotherapy seemed a realistic approach to treat acute toxicity. First we present amphetamines main characteristics: mechanisms of action, structure activity relationship. At this point, the influence of chirality on biological activity is largely developed: many studies suggest that the S enantiomer of amphetamine is the most toxic. Several series of immunogens are then prepared. In a first step haptens derived from S amphetamines and from the corresponding racemics were synthesized. Coupling of haptens was then preformed onto various carrier proteins. Antibodies produced from immunogens derived from haptens with S stereogenic centers were able to recognize S-methamphetamine stronger than racemic methamphetamine. During this study, we have tried different processes to build the amphetaminic skeleton. The reduction by lithium aluminum hydride of the tosylate of phenylalaninol and of its derivatives appeared to be the most efficient procedures. When the phenylalaninol moiety was protected by a tert-butyloxycarbonyl group, the group became the N-methyl group simultaneously with the reduction of the tosylate. In part two of this Thesis, elements on the implication of the dopaminergic system within the reward process were first presented. Theses data show the potential therapeutic interest of dopaminergic agonists and particularly of D1 and D3 agonists in the treatment drug induced dependence. We have studied structure-activity relationship of previously known dopaminergic agonists. Then we synthesized mixed dopaminergic agonists (D1/D3) by combining fragments found in molecules that exhibit affinity to these two receptors. The affinity of the newly synthesized compounds was then evaluated on rat D2 receptors and on human D3 receptors. Then the functional response was determined through a mitogenesis test. Among the synthesized molecules, one with an original structure showed a strong agonist activity on D3 dopaminergic receptors and a slight inhibition of D2 receptors. This promising findings should stimulate the synthesis of derivatives
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Cosford, Nicholas D. P. "Studies in the synthesis of dopamine agonists." Thesis, University of Bath, 1989. https://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.234645.

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Robein-Dobremez, Marie-José. "Hypersensibilité des réponses cardiovasculaires d'origine spinale induites par des agonistes dopaminergiques chez le rat : mécanismes impliqués." Université Joseph Fourier (Grenoble), 1999. http://www.theses.fr/1999GRE18013.

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Kim, Douglas S. "Dopamine and adenosine receptor function in adult and developing dopamine-deficient mice /." Thesis, Connect to this title online; UW restricted, 2002. http://hdl.handle.net/1773/5063.

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Books on the topic "Agonistes de la dopamine"

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Serotonin-dopamine interaction: Experimental evidence and therapeutic relevance. Elsevier, 2008.

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Lawlor, T. Mark. Investigations of agonist activity at dopamine D2 receptors and associated G proteins in bovine brain. University College Dublin, 1995.

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razmy, Ajmal. Daytime sleep and wakefulness in parkinson's disease patients treated with dopamine agonists. National Library of Canada, 2002.

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Johnson, T. The preparation of some novel 2-[2-arylethyl]catecholamines required for evaluation as peripheral dopamine receptor agonists. University of East Anglia, 1994.

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Rusk, Ilene Naomi. The effects of selective dopamine D [inferior] 1 and D [inferior] 2 agonists and antagonists on feeding and associated behaviour. University of Birmingham, 1989.

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Kabbani, Nadine, ed. Dopamine. Humana Press, 2013. http://dx.doi.org/10.1007/978-1-62703-251-3.

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Imaging dopamine. Cambridge University Press, 2009.

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Schuster, John. Descartes-Agonistes. Springer Netherlands, 2013. http://dx.doi.org/10.1007/978-94-007-4746-3.

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Cheung, Hermia. Effect of dopamine depletion on D1 receptor binding in rat brain; and metabolism studies of D1 agonist R-[11C]SKF 82957 and phosphodiesterase-4 inhibitor R-[11C}rolipram. National Library of Canada, 2003.

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The dopamine receptors. 2nd ed. Humana Press, 2010.

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Book chapters on the topic "Agonistes de la dopamine"

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Simola, Nicola, Micaela Morelli, Tooru Mizuno, et al. "Dopamine Agonist." In Encyclopedia of Psychopharmacology. Springer Berlin Heidelberg, 2010. http://dx.doi.org/10.1007/978-3-540-68706-1_947.

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Carroll, Marilyn E., Peter A. Santi, Joseph Zohar, et al. "Indirect-Acting Dopamine Agonists." In Encyclopedia of Psychopharmacology. Springer Berlin Heidelberg, 2010. http://dx.doi.org/10.1007/978-3-540-68706-1_1370.

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Bonneville, Jean-François, Françoise Cattin, and Jean-Louis Dietemann. "Prolactinomas and Dopamine Agonists." In Computed Tomography of the Pituitary Gland. Springer Berlin Heidelberg, 1986. http://dx.doi.org/10.1007/978-3-642-70375-1_6.

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Bonneville, Jean-François. "Prolactinoma and Dopamine Agonists." In MRI of the Pituitary Gland. Springer International Publishing, 2016. http://dx.doi.org/10.1007/978-3-319-29043-0_6.

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Pirtošek, Zvezdan, and Dušan Flisar. "Neuroprotection and Dopamine Agonists." In Advances in Experimental Medicine and Biology. Springer US, 2004. http://dx.doi.org/10.1007/978-1-4419-8969-7_4.

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Herrera-Solís, Andrea, Oscar Arias-Carrión, Andrea Sarro-Ramírez, Mireille Salas-Crisóstomo, and Eric Murillo-Rodríguez. "The Effects of Dopamine Receptor Agonists on the Sleep-Wake Cycle." In Dopamine and Sleep. Springer International Publishing, 2016. http://dx.doi.org/10.1007/978-3-319-46437-4_3.

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McGrath, Barry P., Naoki Sano, and Bernard F. Jover. "Use of Dopamine Agonists in Cardiovascular Medicine." In Peripheral Actions of Dopamine. Macmillan Education UK, 1988. http://dx.doi.org/10.1007/978-1-349-09503-2_12.

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Cannon, Joseph G. "Dopamine agonists: structure-activity relationships." In Progress in Drug Research. Birkhäuser Basel, 1985. http://dx.doi.org/10.1007/978-3-0348-9315-2_9.

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Behere, Prakash B., Anweshak Das, and Aniruddh P. Behere. "Sympathomimetics and Dopamine Receptor Agonists (Psycho Stimulants)." In Clinical Psychopharmacology. Springer Singapore, 2018. http://dx.doi.org/10.1007/978-981-13-2092-7_6.

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Carlsson, A. "Pharmacological Properties of Presynaptic Dopamine Receptor Agonists." In Dyskinesia. Springer Berlin Heidelberg, 1985. http://dx.doi.org/10.1007/978-3-642-70140-5_4.

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Conference papers on the topic "Agonistes de la dopamine"

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Hernández Huerta, Daniel, and Jessenia Paola Morillo González. "Psicosis dual, ¿puede ser el agonismo parcial dopaminérgico D3 una diana terapéutica?" In 22° Congreso de la Sociedad Española de Patología Dual (SEPD) 2020. SEPD, 2020. http://dx.doi.org/10.17579/sepd2020p136.

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Objetivos: Revisión sobre el efecto del agonismo parcial del receptor dopaminérgico D3 en las psicosis duales Material y métodos Búsqueda bibliográfica en MEDLINE introduciendo los términos "schizophrenia", "dopamine D3 receptor partial agonist" y "substance use disorder". Resultados y conclusiones Existe creciente evidencia sobre la eficacia del agonismo parcial dopaminérgico en los trastornos por uso de sustancias (TUS), más allá de su eficacia contrastada en el tratamiento de la esquizofrenia. Aportan como principales ventajas una baja probabilidad de abuso (respecto a los agonistas completos) así como una mejor tolerabilidad (comparados con los antagonistas). En los últimos años, el receptor dopaminérgico D3, debido a su alta distribución en el sistema límbico (donde se encuentra el núcleo accumbens, implicado en los sistemas de motivación y recompensa) se ha postulado como una diana terapéutica prometedora para trastornos relacionados con la dopamina, como son la esquizofrenia y los TUS. En dicha línea, cariprazina (antipsicótico con mayor afinidad por el receptor D3, donde presenta un mecanismo de agonismo parcial, y con eficacia demostrada en los síntomas positivos y negativos de la esquizofrenia) mostraba en una investigación básica ser igual de eficaz que aripiprazol y bifeprunox en reducir el efecto reforzante de la cocaína, así como en la prevención de recaídas. En conclusión, el agonismo parcial del receptor dopaminérgico D3 se posiciona como una alternativa farmacológica a considerar en el tratamiento de las psicosis duales. Una mayor investigación al respecto y la evidencia empírica de la práctica clínica precisarán su verdadero rol.
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Jang, T. S., J. Nair, S. Nair, and A. Lavin. "Modulation of PFC Pyramidal Cell Excitability by Clonidine: A Computational Modeling Study." In ASME 2006 International Mechanical Engineering Congress and Exposition. ASMEDC, 2006. http://dx.doi.org/10.1115/imece2006-15109.

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The prefrontal cortex (PFC) is critically involved in cognitive processes underlying working memory (WM), attention, and inhibition of responses to non-relevant stimuli (Fuster, 2000; Goldman-Rakic, 1996). In this context, catecholaminergic inputs have proven to be critical for the regulation of these cognitive processes (Levitt et al., 1984; Lewis et al., 1987; Lewis and Morrison, 1989; Porrino and Goldman-Rakic, 1982). Aston-Jones and Bloom (1981a, b) showed that, in addition to dopamine (DA) the norepinephrine (NE) neurons located in the locus coeruleus (LC) and terminating in the PFC are important in mediating selective and sustained attention and vigilance. Moreover, stimulation of the LC increases the discrimination of incoming external stimuli to the PFC by reducing the background noise, therefore enhancing the cortical signal-to-noise ratio (Aston-Jones et al., 1985; Berridge and Waterhouse, 2003; Foote et al., 1980, 1983; Waterhouse et al., 1980; Robbins, 2000). More recently, several studies have shown that adrenergic agonists, especially specific alpha-2 agonists, are very effective in enhancing WM and attention. Indeed, administration of alpha-2 agonists can ameliorate some of the negative effects on cognition produced by NE depletion due to aging in monkeys (Arnsten and Goldman-Rakic, 1985; Arnsten et al., 1988; Arnsten and Leslie, 1991) and improve performance in WM-related tasks in young monkeys with NE depletion (Arnsten and Goldman-Rakic, 1985; Cai et al., 1993). Moreover, the therapeutic effects of the specific alpha-2 agonists, clonidine and guanfacine in treating disorders related to dysfunction of WM in patients have been proved (Fields et al., 1988; Mair and McEntree 1986, 1988; Hunt et al., 1985, 1990, 1995).
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SUKUL, N. C. "INTERACTION OF A HIGH DILUTION OF AGARICUS MUSCARIUS L WITH DOPAMINE AGONISTS AND ANTAGONISTS IN MODULATING CATALEPSY OF MICE." In Proceedings of the International School of Biophysics. WORLD SCIENTIFIC, 1998. http://dx.doi.org/10.1142/9789812816887_0019.

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Rios Landeo, Ana Karina, Rafael Rodríguez García, Mireia Borràs Torralbo, et al. "Cariprazina y craving por cocaína." In 22° Congreso de la Sociedad Española de Patología Dual (SEPD) 2020. SEPD, 2020. http://dx.doi.org/10.17579/sepd2020p070.

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La adicción a la cocaína comparte, probablemente, los mismos circuitos subyacentes de la impulsividad. El transportador de dopamina (DAT) se ha identificado como el mecanismo de acción principal para el refuerzo de la adicción en el consumo de cocaína. Se ha demostrado que a largo plazo la anticipación de la recompensa y la búsqueda de sensaciones son más relevantes que la recompensa en sí misma. Además, la cocaína inhibe el transportador de norepinefrina (NET) y el transportador de serotonina (SERT). Los agonistas y antagonistas parciales de los receptores D2 y D₃ de dopamina podrían tener un importante papel en la prevención de recaídas en la adicción a la cocaína. Cariprazina se une preferentemente a receptores D3 de forma fásica, por lo que de esta manera podría ser útil para tratar el trastorno por dependencia de sustancias estimulantes, además de mejorar síntomas negativos, motivación y la cognición. Además, de ser agonista parcial del receptor 5HT1A y antagonista del receptor 5HT2B por lo que actuaría hipotéticamente como modulador y neutralizador de los efectos estimulantes de la cocaína y reduciendo el deseo por consumo. Métodos: Se realiza estudio observacional prospectivo, en pacientes en tratamiento con cariprazina (dosis entre 3 y 6mg/d) y trastorno por uso de cocaína con síntomas psicóticos , evaluando la respuesta al tratamiento mediante la anamnesis y tres cuestionarios: Escala de valoración de la gravedad selectiva para cocaína (CSSA) y Cuestionario de craving de cocaína (CCQ-GB) al inicio del tratamiento. Al mes de tratamiento, se revaloran escalas y se añade Inventario de actitudes al medicamento, (DAI) que valora la respuesta subjetiva a la medicación antipsicótica Resultados: pendientes.
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Martínez Rico, Alejandro, and Ana Beatriz Mulero García. "Evidencia disponible sobre la reducción del consumo de cocaína del antipsicótico atípico Cariprazina." In 22° Congreso de la Sociedad Española de Patología Dual (SEPD) 2020. SEPD, 2020. http://dx.doi.org/10.17579/sepd2020p128.

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1. Descripción precisa de los objetivos El principal objetivo es tratar de demostrar los efectos del antipsicótico atípico Cariprazina en la reducción del consumo de cocaína. El abuso de sustancias es una comorbilidad frecuente de las dos indicaciones para las que está aprobado este fármaco, como son la esquizofrenia y episodios maníacos y está asociada con problemas de salud graves. Con base en la eficacia preclínica, se supone que los agonistas y antagonistas parciales de los receptores de dopamina D2 y D3 tienen un potencial de prevención de recaídas en la adicción a la cocaína humana. Todos los antipsicóticos se unen al receptor D3 in vitro, pero solo la Cariprazina tiene una afinidad a este receptor mayor que la propia dopamina. Este agonismo parcial D3, se ha postulado que podría ser útil para tratar la cognición, ánimo, emociones y tener efectos sobre el uso de sustancias y sistema de recompensa. 2. Material y métodos Se ha realizado una búsqueda blibliográfica en Pubmed, usando los descriptores “Cariprazine”, “anti-abuse potential” y “cocaine addiction” obteniéndose un artículo publicado al respecto. En dicho este estudio se estudiaron los efectos de la Cariprazina y Aripiprazol sobre el efecto gratificante de la cocaína y su potencial de prevención de recaídas en su consumo, se estudió en ratas con antecedentes de abuso de cocaína después de un período de abstinencia completa. 3. Resultados y conclusiones La Cariprazina, así como el Aripiprazol, fueron capaces de reducir el efecto gratificante de la cocaína y atenuaron la recaída en su consumo con la mitad de dosis efectiva máxima. Estos resultados pueden predecir una acción preventiva de recaídas en el consumo para la cariprazina en humanos, además de su eficacia antipsicótica y antimaníaca ya establecida.
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Patil, Vidya, and Mugdha Patki. "Growth of dopamine crystals." In INTERNATIONAL CONFERENCE ON CONDENSED MATTER AND APPLIED PHYSICS (ICC 2015): Proceeding of International Conference on Condensed Matter and Applied Physics. Author(s), 2016. http://dx.doi.org/10.1063/1.4946478.

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Kulkarni, Tanmay, Deepa Gupta, Dan Covey, Joseph Cheer, and Gymama Slaughter. "Dopamine sensing upon amphetamine administration." In 2015 IEEE Sensors. IEEE, 2015. http://dx.doi.org/10.1109/icsens.2015.7370580.

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Wang, Ran, Wei Yang, Yujing Luan, Jian Mao, Hong Qing, and Yulin Deng. "Salsolinol, a Dopamine-derived Tetrahydroisoquinoline, Occur in Dopaminergic SH-SY5Y Cells Induced by Dopamine." In 2007 IEEE/ICME International Conference on Complex Medical Engineering. IEEE, 2007. http://dx.doi.org/10.1109/iccme.2007.4381975.

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Yue, Kun, and Alice C. Parker. "Analog Neurons with Dopamine-Modulated STDP." In 2019 IEEE Biomedical Circuits and Systems Conference (BioCAS). IEEE, 2019. http://dx.doi.org/10.1109/biocas.2019.8919047.

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Kamasak, Mustafa E., Charles A. Bouman, Bradley T. Christian, and Evan D. Morris. "Imaging D2-Dopamine Receptor using PET." In 2007 IEEE 15th Signal Processing and Communications Applications. IEEE, 2007. http://dx.doi.org/10.1109/siu.2007.4298698.

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Reports on the topic "Agonistes de la dopamine"

1

Seegal, Richard F. PCBs Alter Dopamine Mediated Function in Aging Workers. Defense Technical Information Center, 2009. http://dx.doi.org/10.21236/ada501075.

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Marek, Kenneth. Dopamine Transporter Imaging Assessment of Parkinson's Disease Progression. Defense Technical Information Center, 2000. http://dx.doi.org/10.21236/ada383333.

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Seegal, Richard F., Edward F. Fitzgerald, Eric S. Molho, Kenneth L. Marek, and John P. Seibyl. PCBs Alter Dopamine Mediated Function in Aging Workers. Defense Technical Information Center, 2003. http://dx.doi.org/10.21236/ada416007.

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Seegal, Richard F. PCBs Alter Dopamine Mediated Function in Aging Workers. Defense Technical Information Center, 2006. http://dx.doi.org/10.21236/ada452372.

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Seegal, Richard F. PCBs Alter Dopamine Mediated Function in Aging Workers. Defense Technical Information Center, 2005. http://dx.doi.org/10.21236/ada433063.

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Seegal, Richard F. PCBs Alter Dopamine Mediated Function in Aging Workers. Defense Technical Information Center, 2010. http://dx.doi.org/10.21236/ada517349.

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Seegal, Richard F. PCBs Alter Dopamine Mediated Function in Aging Workers. Defense Technical Information Center, 2007. http://dx.doi.org/10.21236/ada466563.

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Carvey, Paul M. Cytokine Induction of Dopamine Neurons from Progenitor Cells. Defense Technical Information Center, 2000. http://dx.doi.org/10.21236/ada391417.

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Seegal, Richard F. PCBs Alter Dopamine Mediated Function in Aging Workers. Defense Technical Information Center, 2008. http://dx.doi.org/10.21236/ada478614.

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Seegal, Richard F. PCBs Alter Dopamine Mediated Function in Aging Workers. Defense Technical Information Center, 2011. http://dx.doi.org/10.21236/ada593238.

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