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Journal articles on the topic 'Recepto 5-HT1A'

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Published: 4 June 2021

Last updated: 10 February 2022

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1

García-Pedraza, José Ángel, Oswaldo Hernández-Abreu, Mónica García, Asunción Morán, and Carlos M. Villalón. "Chronic 5-HT2 receptor blockade unmasks the role of 5-HT1F receptors in the inhibition of rat cardioaccelerator sympathetic outflow." Canadian Journal of Physiology and Pharmacology 96, no. 4 (2018): 328–36. http://dx.doi.org/10.1139/cjpp-2017-0191.

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Serotonin (5-hydroxytryptamine; 5-HT) inhibits the rat cardioaccelerator sympathetic outflow by 5-HT1B/1D/5 receptors. Because chronic blockade of sympatho-excitatory 5-HT2 receptors is beneficial in several cardiovascular pathologies, this study investigated whether sarpogrelate (a 5-HT2 receptor antagonist) alters the pharmacological profile of the above sympatho-inhibition. Rats were pretreated for 2 weeks with sarpogrelate in drinking water (30 mg/kg per day; sarpogrelate-treated group) or equivalent volumes of drinking water (control group). Animals were pithed and prepared for spinal sti

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2

Lee, T. J., M. Ueno, N. Sunagane, and M. H. Sun. "Serotonin relaxes porcine pial veins." American Journal of Physiology-Heart and Circulatory Physiology 266, no. 3 (1994): H1000—H1006. http://dx.doi.org/10.1152/ajpheart.1994.266.3.h1000.

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The effect of serotonin [5-hydroxytryptamine (5-HT)] on pial venous tone of the pig was examined using in vitro tissue bath techniques. Isolated pial venous rings exhibited spontaneous rhythmic contractions (SRC) on mechanical stretching and/or applications of several vasoactive substances, including norepinephrine. On the other hand, KCl induced sustained active muscle tone (SAT) without SRC. The SRC induced by mechanical stretching were not affected by tetrodotoxin, nitro-L-arginine, alpha- and beta-adrenergic, histaminergic, and muscarinic receptor antagonists, indicating that the SRC in po

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3

Montgomery, Stuart A., and Naomi Fineberg. "Is there a Relationship between Serotonin Receptor Subtypes and Selectivity of Response in Specific Psychiatric Illnesses?" British Journal of Psychiatry 155, S8 (1989): 63–69. http://dx.doi.org/10.1192/s0007125000291770.

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Identification of 5-HT receptor subtypes — 5-HT1A, 5-HT1B, 5-HT1c, 5-HT1D, 5-HT2 (possibly A and B), 5-HT3 subtypes, and possibly 5-HT4 — has encouraged the manufacture of 5-HT receptor inhibitors with greater subtype specificity. However, it appears that the receptors interact, and drugs initially thought to be specific may have multiple actions. For some conditions such as anxiety/depression, almost all receptors are implicated. Clinical studies provide clear evidence that manipulation of the 5-HT system has a role in treating depression, anxiety, obsessional illness, migraine, and eating di

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4

Reuter, U., S. Salomone, GW Ickenstein, and C. Waeber. "Effects of Chronic Sumatriptan and Zolmitriptan Treatment on 5-HT1 Receptor Expression and Function in Rats." Cephalalgia 24, no. 5 (2004): 398–407. http://dx.doi.org/10.1111/j.1468-2982.2004.00683.x.

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Triptans are commonly used anti-migraine drugs and show agonist action mainly at serotonin 5-HT1B/1D/1F receptors. It is not known whether frequent or long-term treatment with these drugs would alter 5-HT receptor function. We investigated the effects of protracted (14-18 days) sumatriptan and zolmitriptan treatment in rats on 5-HT1 receptor mRNA expression and function in tissues related to migraine pathophysiology. RT-PCR analysis revealed that 5-HT1B/1D/1F receptor mRNA was reduced in the trigeminal ganglion after treatment with either triptan (reduction by: sumatriptan 39% and zolmitriptan

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5

Nelson, David L., Lee A. Phebus, Kirk W. Johnson, et al. "Preclinical pharmacological profile of the selective 5-HT1F receptor agonist lasmiditan." Cephalalgia 30, no. 10 (2010): 1159–69. http://dx.doi.org/10.1177/0333102410370873.

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Introduction: Lasmiditan (also known as COL-144 and LY573144; 2,4,6-trifluoro- N-[6-[(1-methylpiperidin-4-yl)carbonyl]pyridin-2yl]benzamide) is a high-affinity, highly selective serotonin (5-HT) 5-HT1F receptor agonist. Results: In vitro binding studies show a Ki value of 2.21 nM at the 5-HT1F receptor, compared with Ki values of 1043 nM and 1357 nM at the 5-HT1B and 5-HT1D receptors, respectively, a selectivity ratio greater than 470-fold. Lasmiditan showed higher selectivity for the 5-HT1F receptor relative to other 5-HT1 receptor subtypes than the first generation 5-HT1F receptor agonist LY

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6

Lindhe, Örjan, Per Almqvist, Matts Kågedal, et al. "Autoradiographic Mapping of 5-HT1B/1D Binding Sites in the Rhesus Monkey Brain Using [carbonyl-11C]zolmitriptan." International Journal of Molecular Imaging 2011 (October 12, 2011): 1–6. http://dx.doi.org/10.1155/2011/694179.

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Zolmitriptan is a serotonin 5-HT1B/1D receptor agonist that is an effective and well-tolerated drug for migraine treatment. In a human positron emission tomography study, [11C]zolmitriptan crossed the blood-brain barrier but no clear pattern of regional uptake was discernable. The objective of this study was to map the binding of [11C]zolmitriptan in Rhesus monkey brain using whole hemisphere in vitro autoradiography with [11C]zolmitriptan as a radioligand. In saturation studies, [11C]zolmitriptan showed specific (90%) binding to a population of high-affinity binding sites (Kd 0.95–5.06 nM). T

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7

Hamel, Edith. "The Biology of Serotonin Receptors: Focus on Migraine Pathophysiology and Treatment." Canadian Journal of Neurological Sciences / Journal Canadien des Sciences Neurologiques 26, no. 3 (1999): 2–6. http://dx.doi.org/10.1017/s0317167100000123.

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Serotonin receptors are highly heterogeneous and they have been regrouped within seven different families (5-HT1 - 5-HT7). With the exception of the 5-HT3 which is a ligand-gated ion channel, all others are G-protein coupled receptors with each family sharing structural, pharmacological and transductional characteristics. 5-HT receptors have been implicated in the regulation of several psychiatric and neurological disorders related to serotonergic neurotransmission, and specific receptor subtypes have recently been associated with either the pathogenesis or the treatment of migraine headache.

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8

Olivier, B., J. Schipper, J. A. M. van der Heyden, A. van Hest, J. Mos, and M. Th M. Tulp. "Preclinical evidence for the role of serotonin receptor-subtypes in depression." Acta Neuropsychiatrica 4, no. 2 (1992): 40–45. http://dx.doi.org/10.1017/s0924270800034888.

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SummarySerotonin (5-HT) plays an important role in depression and specific 5-HT reuptake blockers appear to be clinically important antidepressants. It is unclear however, which serotonergic mechanism is involved in the antidepressant effect, certainly when regarding the existence of at least seven 5-HT receptor subtypes. By testing different 5-HT ligands in two animal models of depression (forced swimming and DRL72-S test) and comparison with data from literature, evidence is provided for potential antidepressant qualities of 5-HT1A receptor-agonists and 5-HT1C receptor-antagonists. Compounds

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9

Cowen, P. J. "Serotonin Receptor Subtypes: Implications for Psychopharmacology." British Journal of Psychiatry 159, S12 (1991): 7–14. http://dx.doi.org/10.1192/s0007125000296190.

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Serotonin (5-HT) interacts with multiple brain 5-HT receptor subtypes to influence a wide range of behaviours. Three main families of 5-HT receptors (5-HT1, 5-HT2 and 5-HT3) have been described which differ in their binding affinity for selective ligands, their receptor-effector coupling mechanisms, and the behavioural processes they regulate. Nevertheless, manipulation of several different 5-HT receptor subtypes (5-HT1A, 5-HT1c, 5-HT2 and 5-HT3) may produce anxiolytic effects; 5-HT1A and 5-HT2 receptors may be involved in the aetiology of major depression and the therapeutic effects of antide

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10

Ghavami, A., K. L. Stark, M. Jareb, S. Ramboz, L. Segu, and R. Hen. "Differential addressing of 5-HT1A and 5-HT1B receptors in epithelial cells and neurons." Journal of Cell Science 112, no. 6 (1999): 967–76. http://dx.doi.org/10.1242/jcs.112.6.967.

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The 5-HT1A and 5-HT1B serotonin receptors are expressed in a variety of neurons in the central nervous system. While the 5-HT1A receptor is found on somas and dendrites, the 5-HT1B receptor has been suggested to be localized predominantly on axon terminals. To study the intracellular addressing of these receptors, we have used in vitro systems including Madin-Darby canine kidney (MDCK II) epithelial cells and primary neuronal cultures. Furthermore, we have extended these studies to examine addressing in vivo in transgenic mice. In epithelial cells, 5-HT1A receptors are found on both apical and

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11

Alland, Lucas, and Solomon H. Jacobson. "QSAR Modeling and Prediction of Triptan Binding Affinities." International Journal of Quantitative Structure-Property Relationships 6, no. 2 (2021): 19–28. http://dx.doi.org/10.4018/ijqspr.2021040102.

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The purpose of this study was to use quantitative structure-activity relationships (QSARs) to identify new triptan molecules that selectively bind to h 5-HT1B and h 5-HT1D to a greater extent than to the similar h 5-HT1A receptor in order to identify novel compounds that could lead to an alternative and potentially superior migraine relief drug. Due to its possibility in migraine abortive properties, binding affinities to h 5-HT1F were also modeled. Binding affinities for 12 different triptan drugs and structurally similar substances were compiled from the literature, and descriptors were gene

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12

Villalón, Carlos M., Anton H. Bom, Jan P. C. Heiligers, Marien O. Den Boer, and Pramod R. Saxena. "Constriction of porcine arteriovenous anastomoses by indorenate is unrelated to 5-HT1A, 5-HT1B, 5-HT1C or 5-HT1D receptor." European Journal of Pharmacology 190, no. 1-2 (1990): 167–76. http://dx.doi.org/10.1016/0014-2999(90)94123-f.

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13

Saracheva, Kremena, Petar Hrischev, Liliya Vasileva, Mariyan Topolov, Julia Nikolova, and Damianka Getova. "Effects of new generation triptans – frovatriptan and almotriptan – on hemodynamic parameters in intact male and female rats." Acta Pharmaceutica 70, no. 2 (2020): 239–47. http://dx.doi.org/10.2478/acph-2020-0005.

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AbstractThe introduction of the second generation triptans in clinical and experimental practice was a major progress in the pharmacotherapy of migraine. Frovatriptan is a second generation triptan with strong 5-HT1B/1D serotonergic agonism and low 5-HT1A/7 receptor affinity, while almotriptan possesses not only the typical 5-HT1B/1D receptor agonist activity, but shows an affinity to the 5-HT1F receptor. The aim of our study was to assess the impact of frovatriptan and almotriptan on hemodynamics in male and female rats. We used a non-invasive “tail-cuff” method to measure the arterial blood

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14

Feldman, P. D., and F. J. Galiano. "Cardiovascular effects of serotonin in the nucleus of the solitary tract." American Journal of Physiology-Regulatory, Integrative and Comparative Physiology 269, no. 1 (1995): R48—R56. http://dx.doi.org/10.1152/ajpregu.1995.269.1.r48.

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The cardiovascular regulatory role of serotonin [5-hydroxytryptamine (5-HT)] in the solitary tract nucleus (NTS) was investigated in urethan-anesthetized Wistar rats. Unilateral microinjection of 5-HT (5 nmol in 50 nl) into the NTS evoked depressions of both arterial pressure (-20 +/- 1 mmHg) and heart rate (-43 +/- 6 beats/min). Induction of bradycardia and hypotension was repeatable and consistently obtained with injections into the NTS but not into neighboring structures. Microinjection of the nonselective 5-HT receptor antagonist methiothepin or the 5-HT1A/5-HT1B antagonist pindolol preven

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15

Ueno, M., T. Ishine, and T. J. Lee. "A novel 5-HT1-like receptor subtype mediates cAMP synthesis in porcine pial vein." American Journal of Physiology-Heart and Circulatory Physiology 268, no. 4 (1995): H1383—H1389. http://dx.doi.org/10.1152/ajpheart.1995.268.4.h1383.

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The 5-hydroxytryptamine (5-HT) receptor subtype mediating 5-HT inhibition of spontaneous rhythmic contractions (SRC) in the porcine pial vein was characterized. Results from pharmacological studies using in vitro tissue bath techniques indicated that the inhibitory effects of 5-HT on SRC were qualitatively and quantitatively mimicked by 5-HT1-like agonists 5-methoxytryptamine (5-MT) and 5-carboxamidotryptamine (5-CT). 5-HT-, 5-MT-, and 5-CT-induced inhibitions of SRC were attenuated in a concentration-dependent manner by methysergide, which yielded similar pA2 values against these three agonis

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16

Boers, PM, C. Donaldson, AS Zagami, and GA Lambert. "Naratriptan Has a Selective Inhibitory Effect on Trigeminovascular Neurones at Central 5-HT1A and 5-HT1B/1D Receptors in the Cat: Implications for Migraine Therapy." Cephalalgia 24, no. 2 (2004): 99–109. http://dx.doi.org/10.1111/j.1468-2982.2004.00636.x.

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The triptans are agonists at serotonin(5-HT) 1B/1D receptors; however, they are also active at 5-HT1A and 5-HT1F receptors. We conducted this series of experiments to further elucidate the site of action of naratriptan using a well-established animal model of trigeminovascular stimulation. Following electrical stimulation of the superior sagittal sinus of the cat, single cell responses ( n = 83) were recorded in the trigeminal nucleus caudalis. Most cells (91%) also responded to electrical and mechanical stimulation of cutaneous or mucosal facial receptive fields. The micro-iontophoretic appli

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17

Tack, J. F., J. Janssens, G. Vantrappen, and J. D. Wood. "Actions of 5-hydroxytryptamine on myenteric neurons in guinea pig gastric antrum." American Journal of Physiology-Gastrointestinal and Liver Physiology 263, no. 6 (1992): G838—G846. http://dx.doi.org/10.1152/ajpgi.1992.263.6.g838.

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Intracellular recording methods were used to study the actions of 5-hydroxytryptamine (5-HT) on 257 myenteric neurons in the guinea pig gastric antrum. Application of 5-HT caused three types of postsynaptic responses. A fast-activating depolarizing response was accompanied by a decreased input resistance and desensitized quickly to repeated applications. It was mediated by a 5-HT3 receptor. A slowly activating depolarization, accompanied by an increase in the input resistance and enhancement of the excitability, was mainly observed in after hyperpolarizing/type 2 neurons. It was suppressed by

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18

Umemiya, M., and A. J. Berger. "Presynaptic inhibition by serotonin of glycinergic inhibitory synaptic currents in the rat brain stem." Journal of Neurophysiology 73, no. 3 (1995): 1192–201. http://dx.doi.org/10.1152/jn.1995.73.3.1192.

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1. With the use of a thin brain stem slice preparation, we recorded in visualized neonatal rat hypoglossal motoneurons unitary glycinergic inhibitory postsynaptic currents (IPSCs) that were evoked by extracellular stimulation of nearby interneurons. We found that 10 microM serotonin (5-HT) presynaptically inhibited this glycinergic synaptic transmission by 85.5%. 2. In the somata of presynaptic interneurons, 5-HT1A receptor activation potentiated inwardly rectifying K+ channels and inhibited voltage-activated calcium channels. 3. In contrast, the 5-HT1B receptor was primarily responsible for i

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Meiyanti, Meiyanti. "The role of triptans in the management of migraine." Universa Medicina 28, no. 1 (2016): 49–58. http://dx.doi.org/10.18051/univmed.2009.v28.49-58.

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Migraine is one of the most prevalent disorders seen in clinical practice today and also a major cause of disability in the workplace. The prevalence of migraine is highest during the years of peak productivity, ie, between the ages of 25 and 55 years. The triptans are a group of selective 5-hydroxtriptamine (HT)1 serotonin receptor agonists that activate the 5-HT1B/1D receptor and possibly also the 5-HT1A dan 5-HT1F receptors. To date 7 subclasses of serotonin receptors have been identified, namely subclasses 5-HT1 to 5-HT7. Triptan causes cranial vasoconstriction, inhibits peripheral trigemi

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Bovetto, S., C. Rouillard, and D. Richard. "Role of CRH in the effects of 5-HT-receptor agonists on food intake and metabolic rate." American Journal of Physiology-Regulatory, Integrative and Comparative Physiology 271, no. 5 (1996): R1231—R1238. http://dx.doi.org/10.1152/ajpregu.1996.271.5.r1231.

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Two series of experiments were conducted to investigate the role of corticotropin-releasing hormone (CRH) in the effects of 5-hydroxytryptamine (5-HT) on energy intake and energy expenditure. The first set of experiments was carried out to confirm the influence of 5-HT1A-, 5-HT1B-, 5-HT2A/2C-receptor agonists on the activation of the hypothalamic-pituitary-adrenal axis. Plasma corticosterone levels were measured, and a double-immunolabeling procedure was used to determine whether the neuronal activity marker, c-Fos protein (Fos), could be found within brain neurons containing CRH after treatme

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Virk, Michael S., Yotam Sagi, Lucian Medrihan, Jenny Leung, Michael G. Kaplitt, and Paul Greengard. "Opposing roles for serotonin in cholinergic neurons of the ventral and dorsal striatum." Proceedings of the National Academy of Sciences 113, no. 3 (2016): 734–39. http://dx.doi.org/10.1073/pnas.1524183113.

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Little is known about the molecular similarities and differences between neurons in the ventral (vSt) and dorsal striatum (dSt) and their physiological implications. In the vSt, serotonin [5-Hydroxytryptamine (5-HT)] modulates mood control and pleasure response, whereas in the dSt, 5-HT regulates motor behavior. Here we show that, in mice, 5-HT depolarizes cholinergic interneurons (ChIs) of the dSt whereas hyperpolarizing ChIs from the vSt by acting on different 5-HT receptor isoforms. In the vSt, 5-HT1A (a postsynaptic receptor) and 5-HT1B (a presynaptic receptor) are highly expressed, and sy

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Cohen, Zvi, Isabelle Bouchelet, André Olivier, et al. "Multiple Microvascular and Astroglial 5-Hydroxytryptamine Receptor Subtypes in Human Brain: Molecular and Pharmacologic Characterization." Journal of Cerebral Blood Flow & Metabolism 19, no. 8 (1999): 908–17. http://dx.doi.org/10.1097/00004647-199908000-00010.

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Physiologic and anatomic evidence suggest that 5-hydroxytryptamine (5-HT) neurons regulate local cerebral blood flow and blood-brain barrier permeability. To evaluate the possibility that some of these effects occur directly on the blood vessels, molecular and/or pharmacologic approaches were used to assess the presence of 5-HT receptors in human brain microvascular fractions, endothelial and smooth muscle cell cultures, as well as in astroglial cells which intimately associate with intraparenchymal blood vessels. Isolated microvessels and' capillaries consistently expressed messages for the h

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Kaswan, Nur Khalisah, Noor Aishah Mohammed Idzham, Tengku Azam Shah Tengku Mohamad, Mohd Roslan Sulaiman, and Enoch Kumar Perimal. "Cardamonin Modulates Neuropathic Pain through the Possible Involvement of Serotonergic 5-HT1A Receptor Pathway in CCI-Induced Neuropathic Pain Mice Model." Molecules 26, no. 12 (2021): 3677. http://dx.doi.org/10.3390/molecules26123677.

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Cardamonin, a naturally occurring chalcone isolated from Alpinia species has shown to possess strong anti-inflammatory and anti-nociceptive activities. Previous studies have demonstrated that cardamonin exerts antihyperalgesic and antiallodynic properties in chronic constriction injury (CCI)-induced neuropathic pain animal model. However, the mechanisms underlying cardamonin’s effect have yet to be fully understood. The present study aims to investigate the involvement of the serotonergic system in cardamonin induced antihyperalgesic and antiallodynic effects in CCI-induced neuropathic pain mi

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Watson, J., C. Roberts, C. Scott, et al. "SB-272183, a selective 5-HT1A , 5-HT1B and 5-HT1D receptor antagonist in native tissue." British Journal of Pharmacology 133, no. 6 (2001): 797–806. http://dx.doi.org/10.1038/sj.bjp.0704133.

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Burnat, Grzegorz, Piotr Brański, Joanna Solich, et al. "The functional cooperation of 5-HT1A and mGlu4R in HEK-293 cell line." Pharmacological Reports 72, no. 5 (2020): 1358–69. http://dx.doi.org/10.1007/s43440-020-00114-1.

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Abstract Background The serotonin 5-HT1A receptor (5-HT1AR) and metabotropic glutamate receptor 4 (mGlu4) have been implicated as sites of antipsychotic drug action. 5-HT1AR belongs to the A class of G protein-coupled receptors (GPCRs); mGlu4 is a representative of class C GPCRs. Both receptors preferentially couple with Gi protein to inhibit cAMP formation. The present work aimed to examine the possibility of mGlu4 and 5-HT1A receptor cross-talk, the phenomenon that could serve as a molecular basis of the interaction of these receptor ligands observed in behavioral studies. Methods First, in

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Calogero, A. E., G. Bagdy, M. L. Moncada, and R. D'Agata. "Effect of selective serotonin agonists on basal, corticotrophin-releasing hormone- and vasopressin-induced ACTH release in vitro from rat pituitary cells." Journal of Endocrinology 136, no. 3 (1993): 381–87. http://dx.doi.org/10.1677/joe.0.1360381.

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ABSTRACT The present study was undertaken to evaluate the serotonin (5-HT) receptor subtype(s) by which 5-HT acts on the pituitary to stimulate ACTH secretion. We tested the effects of the 5-HT1A receptor agonist 8-hydroxy-2-(di-n-propylamino)-tetralin (8-OH-DPAT), the 5-HT1C receptor agonist metachloro-phenylpiperazine (m-CPP), which also binds to other 5-HT receptors with lower affinity, and the 5-HT2/1C receptor agonist 1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane (DOI) on basal, corticotrophin-releasing hormone (CRH) and arginine vasopressin (AVP)-stimulated ACTH release from primary rat

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Smith, D., RG Hill, L. Edvinsson, and J. Longmore. "An Immunocytochemical Investigation of Human Trigeminal Nucleus Caudalis: Cgrp, Substance P and 5-Ht1D-Receptor Immunoreactivities Are Expressed by Trigeminal Sensory Fibres." Cephalalgia 22, no. 6 (2002): 424–31. http://dx.doi.org/10.1046/j.1468-2982.2002.00378.x.

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5-HT1D (but not 5-HT1B)-receptor immunoreactivity (i.r.) can be detected on trigeminal fibres within the spinal trigeminal tract of the human brainstem. The present study used immunohistochemical and morphometric techniques to determine the proportions of trigeminal fibres expressing substance P, CGRP or 5-HT1D-receptor immunoreactivities. Co-localization studies between 5-HT1D-receptor and substance P- or CGRP-i.r. were also performed. Brainstem material was obtained with consent (four donors) and the total number of immunoreactive fibres within the trigeminal tract was estimated using random

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Body, S., T. H. C. Cheung, G. Bezzina, et al. "New Findings on the Sensitivity of Free-Operant Timing Behaviour to 5-Hydroxytryptamine Receptor Stimulation." Timing & Time Perception 2, no. 2 (2014): 210–32. http://dx.doi.org/10.1163/22134468-00002024.

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Timing performance maintained under the free-operant psychophysical procedure (FOPP) is sensitive to 5-hydroxytryptamine (5-HT)1A and 5-HT2A receptor stimulation. Agonists of these receptors displace the psychometric function towards shorter durations, reducing , the index of central tendency of timing. Here we report the effects of Ro-600175, a selective 5-HT2C receptor agonist, and mCPP, a 5-HT receptor agonist with high affinity for 5-HT2C receptors and lower affinity for 5-HT1A, 5-HT1B and 5-HT2A receptors, on timing behaviour. Rats were trained under the FOPP to press two levers (A and B)

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Borroto-Escuela, Dasiel O., Patrizia Ambrogini, Barbara Chruścicka, et al. "The Role of Central Serotonin Neurons and 5-HT Heteroreceptor Complexes in the Pathophysiology of Depression: A Historical Perspective and Future Prospects." International Journal of Molecular Sciences 22, no. 4 (2021): 1927. http://dx.doi.org/10.3390/ijms22041927.

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Serotonin communication operates mainly in the extracellular space and cerebrospinal fluid (CSF), using volume transmission with serotonin moving from source to target cells (neurons and astroglia) via energy gradients, leading to the diffusion and convection (flow) of serotonin. One emerging concept in depression is that disturbances in the integrative allosteric receptor–receptor interactions in highly vulnerable 5-HT1A heteroreceptor complexes can contribute to causing major depression and become novel targets for the treatment of major depression (MD) and anxiety. For instance, a disruptio

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Graf, S., and S. K. Sarna. "5-HT-induced jejunal motor activity: enteric locus of action and receptor subtypes." American Journal of Physiology-Gastrointestinal and Liver Physiology 270, no. 6 (1996): G992—G1000. http://dx.doi.org/10.1152/ajpgi.1996.270.6.g992.

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The role of 5-hydroxytryptamine (5-HT), its enteric locus of action, and receptor subtypes involved in the regulation of jejunal contractions were investigated by close intra-arterial infusions in conscious dogs. Close intra-arterial infusions of 5-HT in short segments of the jejunum stimulated phasic contractions that were blocked completely by atropine, partially by tetrodotoxin, and not affected by hexamethonium. This response was also blocked significantly by 5-HT2A and 5-HT2C receptor antagonists but was not affected by 5-HT1A/5-HT1B, 5-HT3, and 5-HT4 receptor antagonists. Spontaneous pha

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Whale, Richard, and Philip J. Cowen. "Probing the Function of 5-HT1B/1D Receptors in Psychiatric Patients." CNS Spectrums 3, no. 8 (1998): 40–45. http://dx.doi.org/10.1017/s1092852900006325.

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AbstractPharmacological challenge tests provide a method of assessing the functional responsiveness of serotonin (5-HT) receptor subtypes in the human brain. A number of selective agonist ligands for the 5-HT1B/1D receptor are available for human use; however, these compounds do not distinguish between 5-HT1B and 5-HT1D receptors, which is somewhat of a disadvantage. Acute administration of sumatriptan, rizatriptan, and zolmitriptan all increase plasma growth hormone in healthy subjects, possibly via activation of postsynaptic 5-HT1D receptors. This response is blunted in major depression. Sum

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Sugimoto, Kotaro, Naoki Ichikawa-Tomikawa, Keisuke Nishiura, et al. "Serotonin/5-HT1A Signaling in the Neurovascular Unit Regulates Endothelial CLDN5 Expression." International Journal of Molecular Sciences 22, no. 1 (2020): 254. http://dx.doi.org/10.3390/ijms22010254.

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We previously reported that site-selective claudin-5 (CLDN5) breakdown and protein kinase A (PKA) activation are observed in brain microvessels of schizophrenia, but the underlying molecular basis remains unknown. The 5-HT1 receptors decline the intracellular cAMP levels and inactivate the major downstream PKA, and the 5-HT1A receptor is a promising target for schizophrenia. Therefore, we elucidated the involvement of serotonin/5-HT1A signaling in the endothelial CLDN5 expression. We demonstrate, by immunohistochemistry using post-mortem human brain tissue, that the 5-HT1A receptor is expresse

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Levitt, Erica S., Barbara J. Hunnicutt, Sharon J. Knopp, John T. Williams, and John M. Bissonnette. "A selective 5-HT1a receptor agonist improves respiration in a mouse model of Rett syndrome." Journal of Applied Physiology 115, no. 11 (2013): 1626–33. http://dx.doi.org/10.1152/japplphysiol.00889.2013.

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Rett syndrome is a neurological disorder caused by loss of function mutations in the gene that encodes the DNA binding protein methyl-CpG-binding protein 2 (Mecp2). A prominent feature of the syndrome is disturbances in respiration characterized by frequent apnea and an irregular interbreath cycle. 8-Hydroxy-2-dipropylaminotetralin has been shown to positively modulate these disturbances (Abdala AP, Dutschmann M, Bissonnette JM, Paton JF, Proc Natl Acad Sci U S A 107: 18208–18213, 2010), but the mode of action is not understood. Here we show that the selective 5-HT1a biased agonist 3-chloro-4-

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Rhoades, R. W., C. A. Bennett-Clarke, M. Y. Shi, and R. D. Mooney. "Effects of 5-HT on thalamocortical synaptic transmission in the developing rat." Journal of Neurophysiology 72, no. 5 (1994): 2438–50. http://dx.doi.org/10.1152/jn.1994.72.5.2438.

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1. Recent immunocytochemical and receptor binding data have demonstrated a transient somatotopic patterning of serotonin (5-HT)-immunoreactive fibers in the primary somatosensory cortex of developing rats and a transient expression of 5-HT1B receptors on thalamocortical axons from the ventral posteromedial thalamic nucleus (VPM). 2. These results suggest that 5-HT should strongly modulate thalamocortical synaptic transmission for a limited time during postnatal development. This hypothesis was tested in intracellular recording experiments carried out in thalamocortical slice preparations that

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Kaya, Namik, Tiansheng Shen, Shao-gang Lu, Fang-li Zhao, and Scott Herness. "A paracrine signaling role for serotonin in rat taste buds: expression and localization of serotonin receptor subtypes." American Journal of Physiology-Regulatory, Integrative and Comparative Physiology 286, no. 4 (2004): R649—R658. http://dx.doi.org/10.1152/ajpregu.00572.2003.

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Recent advances in peripheral taste physiology now suggest that the classic linear view of information processing within the taste bud is inadequate and that paracrine processing, although undemonstrated, may be an essential feature of peripheral gustatory transduction. Taste receptor cells (TRCs) express multiple neurotransmitters of unknown function that could potentially participate in a paracrine role. Serotonin is expressed in a subset of TRCs with afferent synapses; additionally, TRCs respond physiologically to serotonin. This study explored the expression and cellular localization of se

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Cumberbatch, Michael J., Raymond G. Hill, and Richard J. Hargreaves. "The effects of 5-HT1A, 5-HT1B and 5-HT1D receptor agonists on trigeminal nociceptive neurotransmission in anaesthetized rats." European Journal of Pharmacology 362, no. 1 (1998): 43–46. http://dx.doi.org/10.1016/s0014-2999(98)00764-x.

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van den Broek, RWM, P. Bhalla, A. MaassenVanDenBrink, R. de Vries, HS Sharma, and PR Saxena. "Characterization of Sumatriptan-Induced Contractions in Human Isolated Blood Vessels Using Selective 5-HT1B and 5-HT1D Receptor Antagonists and In Situ Hybridization." Cephalalgia 22, no. 2 (2002): 83–93. http://dx.doi.org/10.1046/j.1468-2982.2002.00295.x.

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The 5-HT1B/1D receptor agonist sumatriptan is effective in aborting acute attacks of migraine and is known to cause constriction of cranial arteries as well as some peripheral blood vessels. The present study set out to investigate whether 5-HT1B and/or 5-HT1D receptors mediate contractions of the human isolated middle meningeal and temporal arteries (models for anti-migraine efficacy) and coronary artery and saphenous vein (models for side-effect potential). Concentration-response curves were made with sumatriptan (1 nM-100 μM) in blood vessels in the absence or presence of selective antagoni

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Okada, Motohiro, Ruri Okubo, and Kouji Fukuyama. "Vortioxetine Subchronically Activates Serotonergic Transmission via Desensitization of Serotonin 5-HT1A Receptor with 5-HT3 Receptor Inhibition in Rats." International Journal of Molecular Sciences 20, no. 24 (2019): 6235. http://dx.doi.org/10.3390/ijms20246235.

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Vortioxetine is a novel, multimodal antidepressant with unique targets, including the inhibition of the serotonin transporter (SET), of serotonin 5-HT3 (5-HT3R), and of 5-HT7 (5-HT7R) receptors and partial agonism to serotonin 5-HT1A (5-HT1AR) receptors in humans. Vortioxetine has a lower affinity to 5-HT1AR and 5-HT7R in rats compared with humans, but several behavior studies have demonstrated its powerful antidepressant-like actions. In spite of these efforts, detailed effects of the subchronic administration of vortioxetine on serotonergic transmission remain to be clarified. This study exa

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Toschi, Andrea, Giorgia Galiazzo, Andrea Piva, et al. "Cannabinoid and Cannabinoid-Related Receptors in the Myenteric Plexus of the Porcine Ileum." Animals 11, no. 2 (2021): 263. http://dx.doi.org/10.3390/ani11020263.

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An important piece of evidence has shown that molecules acting on cannabinoid receptors influence gastrointestinal motility and induce beneficial effects on gastrointestinal inflammation and visceral pain. The aim of this investigation was to immunohistochemically localize the distribution of canonical cannabinoid receptor type 1 (CB1R) and type 2 (CB2R) and the cannabinoid-related receptors transient potential vanilloid receptor 1 (TRPV1), transient potential ankyrin receptor 1 (TRPA1), and serotonin receptor 5-HT1a (5-HT1aR) in the myenteric plexus (MP) of pig ileum. CB1R, TRPV1, TRPA1, and

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Hashimoto, Kenji, and Hitoshi Kita. "Serotonin Activates Presynaptic and Postsynaptic Receptors in Rat Globus Pallidus." Journal of Neurophysiology 99, no. 4 (2008): 1723–32. http://dx.doi.org/10.1152/jn.01143.2007.

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Although recent histological, behavioral, and clinical studies suggest that serotonin (5-HT) plays significant roles in the control of pallidal activity, only little is known about the physiological action of 5-HT in the pallidum. Our recent unit recording study in monkeys suggested that 5-HT provides both presynaptic and postsynaptic modulations of pallidal neurons. The present study using rat brain slice preparations further explored these presynaptic and postsynaptic actions of 5-HT. Bath application of 5-HT or the 5-HT1A/1B/1D/5/7 receptor (R) agonist 5-carboxamidotryptamine maleate (5-CT)

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Murray, Katherine C., Marilee J. Stephens, Michelle Rank, Jessica D'Amico, Monica A. Gorassini, and David J. Bennett. "Polysynaptic excitatory postsynaptic potentials that trigger spasms after spinal cord injury in rats are inhibited by 5-HT1B and 5-HT1F receptors." Journal of Neurophysiology 106, no. 2 (2011): 925–43. http://dx.doi.org/10.1152/jn.01011.2010.

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Sensory afferent transmission and associated spinal reflexes are normally inhibited by serotonin (5-HT) derived from the brain stem. Spinal cord injury (SCI) that eliminates this 5-HT innervation leads to a disinhibition of sensory transmission and a consequent emergence of unusually long polysynaptic excitatory postsynaptic potentials (EPSPs) in motoneurons. These EPSPs play a critical role in triggering long polysynaptic reflexes (LPRs) that initiate muscles spasms. In the present study we examined which 5-HT receptors modulate the EPSPs and whether these receptors adapt to a loss of 5-HT af

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Vidal, Benjamin, Elise Levigoureux, Sarah Chaib, et al. "Different Alterations of Agonist and Antagonist Binding to 5-HT1A Receptor in a Rat Model of Parkinson’s Disease and Levodopa-Induced Dyskinesia: A MicroPET Study." Journal of Parkinson's Disease 11, no. 3 (2021): 1257–69. http://dx.doi.org/10.3233/jpd-212580.

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Background: The gold-standard treatment for Parkinson’s disease is L-DOPA, which in the long term often leads to levodopa-induced dyskinesia. Serotonergic neurons are partially responsible for this, by converting L-DOPA into dopamine leading to its uncontrolled release as a “false neurotransmitter”. The stimulation of 5-HT1A receptors can reduce involuntary movements but this mechanism is poorly understood. Objective: This study aimed to investigate the functionality of 5-HT1A receptors using positron emission tomography in hemiparkinsonian rats with or without dyskinesia induced by 3-weeks da

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Bruinvels, A. T., B. Landwehrmeyer, E. L. Gustafson та ін. "Localization of 5-HT1B, 5-HT1Dα, 5-HT1E and 5-HT1F receptor messenger RNA in rodent and primate brain". Neuropharmacology 33, № 3-4 (1994): 367–86. http://dx.doi.org/10.1016/0028-3908(94)90067-1.

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Okada, Fukuyama, Okubo, Shiroyama, and Ueda. "Lurasidone Sub-Chronically Activates Serotonergic Transmission via Desensitization of 5-HT1A and 5-HT7 Receptors in Dorsal Raphe Nucleus." Pharmaceuticals 12, no. 4 (2019): 149. http://dx.doi.org/10.3390/ph12040149.

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Lurasidone is an atypical mood-stabilizing antipsychotic agent with unique receptor-binding profile, including 5-HT7 receptor (5-HT7R) antagonism. Effects of 5-HT7R antagonism on transmitter systems of schizophrenia and mood disorders, however, have not been well clarified. Thus, this study examined the mechanisms underlying the clinical effects of lurasidone by measuring mesocortical serotonergic transmission. Following systemic and local administrations of lurasidone, MK801 and 5-HT receptor modulators, we determined releases of 5-HT in dorsal raphe nucleus (DRN), mediodorsal thalamic nucleu

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Pauwels, Petrus J., та Christiane Palmier. "Functional effects of the 5-HT1D receptor antagonist GR 127,935 at human 5-HT1Dα, 5-HT1Dβ, 5-HT1A and opposum 5-HT1B receptors". European Journal of Pharmacology: Molecular Pharmacology 290, № 2 (1995): 95–103. http://dx.doi.org/10.1016/0922-4106(95)90021-7.

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Wade, P. R., G. M. Mawe, T. A. Branchek, and M. D. Gershon. "Use of stereoisomers of zacopride to analyze actions of 5-hydroxytryptamine on enteric neurons." American Journal of Physiology-Gastrointestinal and Liver Physiology 260, no. 1 (1991): G80—G90. http://dx.doi.org/10.1152/ajpgi.1991.260.1.g80.

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Two subtypes of excitatory 5-hydroxytryptamine (5-HT) receptor, 5-HT1P and 5-HT3, are found on type 2-AH neurons of the guinea pig myenteric plexus. The 5-HT1P receptor mediates a slow and the 5-HT3 receptor a fast depolarization of these cells, however, the role of these receptors in the physiology of the gut is unknown. Renzapride (BRL 24924), a substituted benzamide, has previously been found to antagonize responses of myenteric neurons mediated by both 5-HT1P and 5-HT3 receptors. The effects on myenteric type 2-AH neurons of a structurally similar benzamide, zacopride, which unlike renzapr

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Zhu, Chen, Xinwei Li, Weiqing Peng, and Wei Fu. "Discovery of Novel Indolealkylpiperazine Derivatives as Potent 5-HT1A Receptor Agonists for the Potential Future Treatment of Depression." Molecules 25, no. 21 (2020): 5078. http://dx.doi.org/10.3390/molecules25215078.

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Depression is a severe psychiatric disorder that affects over 100 million people worldwide. 5-HT1A receptor agonists have been implicated in the treatment of a variety of central nervous system diseases, especially depression. In this study, based on FW01, a selective potent 5-HT1AR agonist discovered via dynamic pharmacophore-based virtual screening, a series of indolealkylpiperazine derivatives with a benzamide moiety were designed and synthesized by the modification of the amide tail group as well as indole head group of FW01. Among all tested compounds, 13m displayed potent agonistic activ

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Ramadan, NM, V. Skljarevski, LA Phebus, and KW Johnson. "5-HT1F Receptor Agonists in Acute Migraine Treatment: A Hypothesis." Cephalalgia 23, no. 8 (2003): 776–85. http://dx.doi.org/10.1046/j.1468-2982.2003.00525.x.

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Serotonin-1F receptor (5-HT1F) agonists may relieve acute migraine without vasoconstriction. We conducted a review of preclinical and clinical data that assessed the potential link between migraine and 5-HT1F activation. (i) A high correlation exists between the potency of various 5-HT1 receptor agonists in the guinea pig dural plasma protein extravasation assay and their 5-HT1F receptor binding affinity. (ii) 5-HT1F receptors are on the trigeminal system, and may participate in blocking migraine pain transmission through the trigeminal ganglion and nucleus caudalis. (iii) 5-HT1F receptors are

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Centurión, David, Araceli Sánchez-López, Peter De Vries, Pramod R. Saxena, and Carlos M. Villalón. "The GR127935-sensitive 5-HT1 receptors mediating canine internal carotid vasoconstriction: resemblance to the 5-HT1B , but not to the 5-HT1D or 5-ht1F , receptor subtype." British Journal of Pharmacology 132, no. 5 (2001): 991–98. http://dx.doi.org/10.1038/sj.bjp.0703913.

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Harrington, Melissa A., Andrew J. Sleight, Josef Pitha, and Stephen J. Peroutka. "Structural determinants of 5-HT1A versus 5-HT1D receptor binding site selectivity." European Journal of Pharmacology 194, no. 1 (1991): 83–90. http://dx.doi.org/10.1016/0014-2999(91)90127-c.

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