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Artigos de revistas sobre o tema "Receptors; Irreversible antagonist; Drug abuse"

Autor: Grafiati

Publicado: 4 de junho de 2021

Última modificação: 6 de fevereiro de 2022

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1

Burroughs, SF, and GJ Johnson. "Beta-lactam antibiotic-induced platelet dysfunction: evidence for irreversible inhibition of platelet activation in vitro and in vivo after prolonged exposure to penicillin." Blood 75, no. 7 (1990): 1473–80. http://dx.doi.org/10.1182/blood.v75.7.1473.1473.

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Abstract beta-Lactam antibiotics cause platelet dysfunction with bleeding complications. Previous in vitro studies documented reversible inhibition of agonist-receptor interaction. This mechanism is inadequate to explain the effect of beta-lactam antibiotics in vivo. Platelet function does not return to normal immediately after drug treatment, implying irreversible inhibition of platelet function. We report here evidence of irreversible platelet functional and biochemical abnormalities after in vitro and in vivo exposure to beta-lactam antibiotics. Irreversible binding of [14C]-penicillin (Pen

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Burroughs, SF, and GJ Johnson. "Beta-lactam antibiotic-induced platelet dysfunction: evidence for irreversible inhibition of platelet activation in vitro and in vivo after prolonged exposure to penicillin." Blood 75, no. 7 (1990): 1473–80. http://dx.doi.org/10.1182/blood.v75.7.1473.bloodjournal7571473.

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beta-Lactam antibiotics cause platelet dysfunction with bleeding complications. Previous in vitro studies documented reversible inhibition of agonist-receptor interaction. This mechanism is inadequate to explain the effect of beta-lactam antibiotics in vivo. Platelet function does not return to normal immediately after drug treatment, implying irreversible inhibition of platelet function. We report here evidence of irreversible platelet functional and biochemical abnormalities after in vitro and in vivo exposure to beta-lactam antibiotics. Irreversible binding of [14C]-penicillin (Pen) occurre

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3

Vieira-Coelho, M., J. Azevedo, and M. Esteves. "New Potential Molecular Targets for Cannabis Addition." European Psychiatry 24, S1 (2009): 1. http://dx.doi.org/10.1016/s0924-9338(09)70703-5.

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Cannabis is considerer the most widely abused illicit drug in the world. The recent rising prevalence of cannabis use by young adults and increasing evidence of adverse health effects makes the search for new pharmacotherapy to reduce cannabis abuse extremely important. To date no medication has been approved for the treatment of cannabis addition.This study reviews recent results with potential interest for future pharmacological treatment of Cannabis dependence. Most of the relevant data obtained for treatment of cannabis dependence target the endocannabinoid or the central cholinergic syste

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4

Althobaiti, Yusuf S. "Quetiapine-Induced Place Preference in Mice: Possible Dopaminergic Pathway." Pharmaceuticals 14, no. 2 (2021): 156. http://dx.doi.org/10.3390/ph14020156.

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Quetiapine, an atypical antipsychotic, is effective in the management of schizophrenia, depression, and anxiety. Although quetiapine overdosage and misuse have been reported, its abuse potential has not been investigated in animals. In this study, the abuse potential of quetiapine was assessed based on the conditioned place preference (CPP) paradigm of drug addiction in a mouse model. First, mice received intraperitoneal injections of quetiapine (40, 80, or 120 mg/kg) every other day during the conditioning phase. In the second experiment, mice were pretreated with 0.03 mg/kg SKF-35866, a D1 r

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Lebedev, Andrei Andreevich, Eugeny Grigorievich Shumilov, Eugeny Rudolfovich Bychkov, Vitaly Ivanovich Morozov, and Petr Dmitriyevich Shabanov. "Orexin A role in mechanisms of reinforcement in the bed nucleus of stria terminalis." Reviews on Clinical Pharmacology and Drug Therapy 13, no. 2 (2015): 20–26. http://dx.doi.org/10.17816/rcf13220-26.

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The orexin family of hypothalamic neuropeptides has been implicated in reinforcement mechanisms relevant to both food and drug reward. Previous behavioral studies with antagonists at the orexin A-selective receptor OX(1), have demonstrated its involvement in behavioral sensitization, conditioned place-preference, self-administration and reinstatement of drugs abuse. There are dense concentrations of hypocretin receptors, in brain regions implicated in drug reinforcement processes, such as the nucleus accumbens, ventral tegmental area and bed nucleus of the stria terminalis Adult male Wistar ra

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6

Davis, Corey, Damika Webb, and Scott Burris. "Changing Law from Barrier to Facilitator of Opioid Overdose Prevention." Journal of Law, Medicine & Ethics 41, S1 (2013): 33–36. http://dx.doi.org/10.1111/jlme.12035.

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Drug overdose has recently surpassed motor vehicle accidents to become the leading cause of unintentional injury death in the United States. The epidemic is largely driven by opioids such as oxycodone, hydrocodone, and methadone, which kill more Americans than heroin and cocaine combined. The demographics of overdose have changed over the past few decades as well: according to the latest data, the average overdose victim is now a non-Hispanic white man aged 45-54.These deaths — over 16,000 per year — are almost entirely preventable. Opioid overdose kills by slowly depressing respiration, a pro

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7

Altarifi, Ahmad A., Megan J. Moerke, Mohammad I. Alsalem, and S. Stevens Negus. "Preclinical assessment of tramadol abuse potential: Effects of acute and repeated tramadol on intracranial self-stimulation in rats." Journal of Psychopharmacology 34, no. 11 (2020): 1316–25. http://dx.doi.org/10.1177/0269881120944153.

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Background: Tramadol is a widely used analgesic that activates mu-opioid receptors (MOR) and inhibits serotonin and norepinephrine transporters. This mixed pharmacology may limit both its own abuse potential and its modulation of abuse potential of other MOR agonists. Aims: This study used an intracranial self-stimulation (ICSS) procedure to compare abuse-related effects produced by acute or repeated treatment with tramadol or morphine in rats. Abuse potential in ICSS procedures is indicated by a drug-induced increase (or ‘facilitation’) of ICSS responding. Methods: Adult male Sprague–Dawley r

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Marszalek-Grabska, Marta, Kinga Gawel, Dariusz Matosiuk, Ewa Gibula-Tarlowska, Joanna Listos, and Jolanta H. Kotlinska. "Effects of the Positive Allosteric Modulator of Metabotropic Glutamate Receptor 5, VU-29, on Maintenance Association between Environmental Cues and Rewarding Properties of Ethanol in Rats." Biomolecules 10, no. 5 (2020): 793. http://dx.doi.org/10.3390/biom10050793.

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Metabotropic glutamate subtype 5 (mGlu5) receptors are implicated in various forms of synaptic plasticity, including drugs of abuse. In drug-addicted individuals, associative memories can drive relapse to drug use. The present study investigated the potential of the mGlu5 receptor positive allosteric modulator (PAM), VU-29 (30 mg/kg, i.p.), to inhibit the maintenance of a learned association between ethanol and environmental context by using conditioned place preference (CPP) in rats. The ethanol-CPP was established by the administration of ethanol (1.0 g/kg, i.p. ×10 days) using an unbiased p

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9

Helm II, Standiford. "Opioid Antagonists, Partial Agonists, and Agonists/Antagonists: The Role of OfficeBased Detoxification." Pain Physician 2;11, no. 3;2 (2008): 225–35. http://dx.doi.org/10.36076/ppj.2008/11/225.

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Background: The opioid receptor antagonists naloxone and naltrexone are competitive antagonists at the mu, kappa, and sigma receptors with a higher affinity for the mu receptor and lacking any mu receptor efficacy. Buprenorphine is classified as a partial agonist. It has a high affinity, but low efficacy at the mu receptor where it yields a partial effect upon binding. It also, however, possesses kappa receptor antagonist activity making it useful not only as an analgesic, but also in opioid abuse deterrence, detoxification, and maintenance therapies. Naloxone is added to sublingual buprenorph

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10

Colman, Atalie S., та John H. Miller. "μ-1 Opioid Receptor Stimulation Decreases Body Temperature in Conscious, Unrestrained Neonatal Rats". Experimental Biology and Medicine 227, № 6 (2002): 377–81. http://dx.doi.org/10.1177/153537020222700602.

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The influence of μ-selective opioid agonists on neonatal thermoregulatory mechanisms has received little attention. Opioid treatment in adult subjects can cause either hyper- or hypothermia, depending on the experimental conditions, the strain of rat used, and the dose and route of administration of the drug. The present study assessed the effect of two μ opioid agonists on body temperature in neonatal Wistar rats aged 2 to 13 days. Rat pups were administered either saline or one of the two μ-selective opioid agonists, dermorphin (0.4 mg/kg) or fentanyl (0.06 mg/kg), by subcutaneous injection.

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11

Butler, Stephen. "Buprenorphine—Clinically useful but often misunderstood." Scandinavian Journal of Pain 4, no. 3 (2013): 148–52. http://dx.doi.org/10.1016/j.sjpain.2013.05.004.

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AbstractBackgroundThere are a number of false myths about buprenorphine based on unconfirmed animal data, even from isolated animal organs, and early clinical research. These myths came into textbooks on pharmacology and pain about 30 years ago and have been difficult to eradicate. Animal models of pain and pain relief are notoriously unreliable as predictors of human clinical effects. The fact is that in clinical practice there is NO bell-shaped dose-response curve, there is NO plateau on the dose-response curve, and there is NO antagonist effect from buprenorphine on other mu-opioid agonists

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12

Leo, Luciana M., and Mary E. Abood. "CB1 Cannabinoid Receptor Signaling and Biased Signaling." Molecules 26, no. 17 (2021): 5413. http://dx.doi.org/10.3390/molecules26175413.

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The CB1 cannabinoid receptor is a G-protein coupled receptor highly expressed throughout the central nervous system that is a promising target for the treatment of various disorders, including anxiety, pain, and neurodegeneration. Despite the wide therapeutic potential of CB1, the development of drug candidates is hindered by adverse effects, rapid tolerance development, and abuse potential. Ligands that produce biased signaling—the preferential activation of a signaling transducer in detriment of another—have been proposed as a strategy to dissociate therapeutic and adverse effects for a vari

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13

Asser, Andres, Atsuko Hikima, Mari Raki, et al. "Subacute administration of both methcathinone and manganese causes basal ganglia damage in mice resembling that in methcathinone abusers." Journal of Neural Transmission 127, no. 5 (2019): 707–14. http://dx.doi.org/10.1007/s00702-019-02110-z.

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AbstractAn irreversible extrapyramidal syndrome occurs in man after intravenous abuse of “homemade” methcathinone (ephedrone, Mcat) that is contaminated with manganese (Mn) and is accompanied by altered basal ganglia function. Both Mcat and Mn can cause alterations in nigrostriatal function but it remains unknown whether the effects of the ‘homemade’ drug seen in man are due to Mcat or to Mn or to a combination of both. To determine how toxicity occurs, we have investigated the effects of 4-week intraperitoneal administration of Mn (30 mg/kg t.i.d) and Mcat (100 mg/kg t.i.d.) given alone, on t

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14

Atehortua-Martinez, Luisa Alessandra, Cyriaque Masniere, Patrizia Campolongo, et al. "Acute and chronic neurobehavioral effects of the designer drug and bath salt constituent 3,4-methylenedioxypyrovalerone in the rat." Journal of Psychopharmacology 33, no. 3 (2019): 392–405. http://dx.doi.org/10.1177/0269881118822151.

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Background: The substantial increase in use of 3,4-methylenedioxypyrovalerone (MDPV), a popular recreational synthetic cathinone, has raised legitimate questions about its behavioral consequences and abuse liability. Aims: The aim of this study was to study MDPV-induced neurobehavioral effects in the rat, using different paradigms traditionally developed to study drug-attributed addictive properties. Methods: Different patterns of intraperitoneal 3 mg/kg MDPV administration were investigated. Consequences on rat horizontal locomotion and behavior of acute, intermittent (once daily dosing over

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15

Jablonski, Sarah A., Michael T. Williams, and Charles V. Vorhees. "Learning and Memory Effects of Neonatal Methamphetamine Exposure in Sprague-Dawley Rats: Test of the Role of Dopamine Receptors D1 in Mediating the Long-Term Effects." Developmental Neuroscience 41, no. 1-2 (2019): 44–55. http://dx.doi.org/10.1159/000498884.

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Methamphetamine (MA) abuse is a worldwide issue that produces health and cognitive effects in the user. MA is abused by some women who then become pregnant and expose their developing child to the drug. Preclinical rodent models demonstrate cognitive deficits following developmental MA exposure, an effect observed in children exposed to MA in utero. To determine if the dopamine receptor D1 (DRD1) is involved in the learning and memory deficits following MA exposure, male Sprague-Dawley rats were treated 4 times daily at 2 h intervals with 0 (saline) or 10 mg/kg of MA from postnatal day (P)6–15

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16

Cornelissen, Ivo, Erica De Candia, Daniel Palmer, and Shaun R. Coughlin. "Inhibition of the ADP/P2Y12 Pathway Confers Additional Protection against Arterial Thrombosis in PAR-4 Deficient Mice." Blood 112, no. 11 (2008): 3933. http://dx.doi.org/10.1182/blood.v112.11.3933.3933.

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Abstract Clopidogrel, a potent anti-thrombotic drug widely used for the secondary prevention of myocardial infarction and ischemic stroke, inhibits the ADP/P2Y12 pathway by inducing irreversible alteration of the platelet receptor P2Y12, ultimately uncoupling ADP from adenylyl cyclase inhibition. Clinical trials have demonstrated additional benefits of dual antiplatelet therapy, such as combined treatment with clopidogrel and aspirin, in the prevention of ischemic cardiovascular disease. We previously established that protease-activated receptor (PAR) signaling is necessary for platelet activa

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17

Pereira, Jaime, María P. Hernández, Claudia G. Saez, Karla Pereira-Flores, Alberto Leguina, and Diego Mezzano. "Role of Sigma-1 Receptor in Cocaine-Induced Endothelial Cell Damage." Blood 124, no. 21 (2014): 1446. http://dx.doi.org/10.1182/blood.v124.21.1446.1446.

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Abstract Background :Cocaine abuse is associated with an increased risk of cardiac and cerebrovascular events, such as myocardial infarction, sudden cardiac death, and ischemic stroke. The underlying mechanisms leading to these complications are not fully understood although intravascular thrombus formation and accelerated atherosclerosis are prominent findings. We showed that chronic cocaine use is associated with markers of endothelial dysfunction (ED) (Sáez et al. Thromb Res 2011; 128:18). The hallmark of ED is a change to a prothrombotic and proadhesive phenotype associated with a decrease

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18

Palandri, Josephine, Sharon L. Smith, David J. Heal, Sue Wonnacott та Chris P. Bailey. "Contrasting effects of the α7 nicotinic receptor antagonist methyllycaconitine in different rat models of heroin reinstatement". Journal of Psychopharmacology, 10 березня 2021, 026988112199157. http://dx.doi.org/10.1177/0269881121991570.

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Background: α7 Nicotinic acetylcholine receptors are implicated in the reinstatement of drug-seeking, an important component of relapse. We showed previously that the α7 nicotinic acetylcholine receptor antagonist, methyllycaconitine, specifically attenuated morphine-primed reinstatement of conditioned place preference in rodents and this effect was mediated in the ventral hippocampus. Aims: The purpose of this study was to evaluate α7 nicotinic acetylcholine receptor antagonism in reinstatement of the conditioned place preference for the more widely abused opioid, heroin, and to compare the e

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19

Althobaiti, Yusuf S., Farooq M. Almutairi, Fahad S. Alshehri, et al. "Involvement of the dopaminergic system in the reward-related behavior of pregabalin." Scientific Reports 11, no. 1 (2021). http://dx.doi.org/10.1038/s41598-021-88429-8.

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AbstractThere has been an increase in cases of drug addiction and prescription drug abuse worldwide. Recently, pregabalin abuse has been a focus for many healthcare agencies, as highlighted by epidemiological studies. We previously evaluated the possibility of pregabalin abuse using the conditioned place preference (CPP) paradigm. We observed that a 60 mg/kg dose could induce CPP in mice and that pregabalin-rewarding properties were mediated through glutamate neurotransmission. Notably, the dopaminergic reward circuitry is also known to play a crucial role in medication-seeking behavior. There

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Senćanski, Milan, Milovan Ivanović, and Ljiljana Došen-Mićović. "Modelling of ORL1 receptor-ligand interactions." Chemical Papers 68, no. 10 (2014). http://dx.doi.org/10.2478/s11696-014-0577-z.

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AbstractAn opioid receptor like (ORL1) receptor is one of a family of G-protein-coupled receptors (GPCR); it represents a new pharmaceutical target with extensive therapeutic potential for the regulation of important biological functions such as nociception, mood disorders, drug abuse, learning or cardiovascular control. Although the crystal structure of the inactive form of the ORL1 receptor has been determined, little is known about its activation. By using X-ray structures of the β2-adrenegic receptor in its inactive (2RH1) and active (3P0G) states as templates, inactive and active homology

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He, Xiang-Hu, Ewa Galaj, Guo-Hua Bi та ін. "β-caryophyllene, an FDA-Approved Food Additive, Inhibits Methamphetamine-Taking and Methamphetamine-Seeking Behaviors Possibly via CB2 and Non-CB2 Receptor Mechanisms". Frontiers in Pharmacology 12 (9 вересня 2021). http://dx.doi.org/10.3389/fphar.2021.722476.

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Recent research indicates that brain cannabinoid CB2 receptors are involved in drug reward and addiction. However, it is unclear whether β-caryophyllene (BCP), a natural product with a CB2 receptor agonist profile, has therapeutic effects on methamphetamine (METH) abuse and dependence. In this study, we used animal models of self-administration, electrical brain-stimulation reward (BSR) and in vivo microdialysis to explore the effects of BCP on METH-taking and METH-seeking behavior. We found that systemic administration of BCP dose-dependently inhibited METH self-administration under both fixe

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