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Journal articles on the topic 'Serotonin (5-HT) receptors'

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Published: 3 June 2025

Last updated: 31 July 2025

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1

Neumann, Joachim, Britt Hofmann, Stefan Dhein, and Ulrich Gergs. "Cardiac Roles of Serotonin (5-HT) and 5-HT-Receptors in Health and Disease." International Journal of Molecular Sciences 24, no. 5 (2023): 4765. http://dx.doi.org/10.3390/ijms24054765.

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Serotonin acts solely via 5-HT4-receptors to control human cardiac contractile function. The effects of serotonin via 5-HT4-receptors lead to positive inotropic and chronotropic effects, as well as arrhythmias, in the human heart. In addition, 5-HT4-receptors may play a role in sepsis, ischaemia, and reperfusion. These presumptive effects of 5-HT4-receptors are the focus of the present review. We also discuss the formation and inactivation of serotonin in the body, namely, in the heart. We identify cardiovascular diseases where serotonin might play a causative or additional role. We address th

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Saxena, Pramod R., and Michel D. Ferrari. "From Serotonin Receptor Classification to the Antimigraine Drug Sumatriptan." Cephalalgia 12, no. 4 (1992): 187–96. http://dx.doi.org/10.1046/j.1468-2982.1992.1204187.x.

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After the synthetic serotonin 5-hydroxytryptamine (5-HT) became available in the early 1950s, attempts were soon under way to study the nature of 5-HT receptors. Using the guinea-pig isolated ileum, Gaddum and Picarelli (1957) suggested that 5-HT-induced contractions were mediated by a morphine-sensitive “M” receptor located on the parasympathetic ganglion and a dibenzyline-sensitive “D” receptor located on the smooth muscle. Though this classification was used during the next three decades, it was realized that some effects of serotonin, for example vasoconstriction within the carotid vascula

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Lychkova, Alla Eduard. "Serotonin Receptors Mediate Contractile Activity of Rat's Esophagus in-vivo." Archive of Organ Transplantation 2, no. 1 (2017): 019–22. https://doi.org/10.17352/aot.000007.

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<strong>Background: </strong>Serotonin (5-hydroxytryptamine, 5-HT) is a regulatory and biologically active neurotransmitter and a hormone in the CNS and many organs, including the esophagus. It is known that serotonin as well as acetylcholine stimulates contractile activity of the esophageal muscles. However, role of different serotonin receptors in the 5-HT contractile activity of the esophagus is insufficiently known.

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Amidfar, Meysam, and Yong-Ku Kim. "Recent Developments on Future Antidepressant-related Serotonin Receptors." Current Pharmaceutical Design 24, no. 22 (2018): 2541–48. http://dx.doi.org/10.2174/1381612824666180803111240.

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Conventional serotonin-enhancing antidepressants including selective serotonin reuptake inhibitors (SSRIs) and serotonin and norepinephrine reuptake inhibitors (SNRIs) have shown effectiveness in the treatment of major depression, but their significant limitations such as slowness of action have led to intensive research efforts to develop new antidepressants. Increased synaptic neurotransmission of serotonin (5-hdroxytryptamine; 5-HT) through orchestration of stimulation and blockade of various subtypes of 5-HT receptors is involved in the mechanisms of action of SSRIs. Agonists at the 5-HT1A

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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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Kostowski, W. "Ethanol and serotonin 5-HT-5 receptors." Pharmacological Research 31 (January 1995): 36. http://dx.doi.org/10.1016/1043-6618(95)86402-4.

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7

Schmitz, Dietmar, Tengis Gloveli, Ruth M. Empson, and Uwe Heinemann. "Serotonin Reduces Polysynaptic Inhibition via 5-HT1A Receptors in the Superficial Entorhinal Cortex." Journal of Neurophysiology 80, no. 3 (1998): 1116–21. http://dx.doi.org/10.1152/jn.1998.80.3.1116.

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Schmitz, Dietmar, Tengis Gloveli, Ruth M. Empson, and Uwe Heinemann. Serotonin reduces polysynaptic inhibition via 5-HT1A receptors in the superficial entorhinal cortex. J. Neurophysiol. 80: 1116–1121, 1998. The superficial cells of the entorhinal cortex (EC), main input to the hippocampus, receive a serotonergic input from the raphe nuclei and express 5-hydroxytryptamine creatine sulfate complex (5-HT) receptors at high density. With the use of intracellular recordings, we investigated the effects of serotonin on synaptic inhibition of layer II and III neurons of the EC. Serotonin reduced bot

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8

Puzikov, A. M. "Esophagus: serotoninerdgic regulation." Experimental and Clinical Gastroenterology, no. 7 (September 27, 2020): 137–42. http://dx.doi.org/10.31146/1682-8658-ecg-179-7-137-142.

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Introduction: Serotonin (5-hydroxytryptamine, 5-HT) is a regulatory neurotransmitter and a hormone in the CNS and hole organs, the esophagus including. It is known that serotonin, activating its own receptors, stimulates contractile activity of the esophageal muscles. However, role of different type receptors in the 5-HT induced contractile activity of the esophagus is insufficiently known.The aim: — to determine which type of 5-HT receptors mediate serotonin dependent contractile activity of the esophagus.Material and methods: This is a electromyography study of rat esophagus contractile acti

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9

Frieling, T., H. J. Cooke, and J. D. Wood. "Serotonin receptors on submucous neurons in guinea pig colon." American Journal of Physiology-Gastrointestinal and Liver Physiology 261, no. 6 (1991): G1017—G1023. http://dx.doi.org/10.1152/ajpgi.1991.261.6.g1017.

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Intracellular microelectrodes were used to investigate the neuropharmacology of 5-hydroxytryptamine (5-HT) in the submucous plexus of the distal colon of the guinea pig. Three effects resulted from application of 5-HT to submucous neurons. Two of the effects were components of a biphasic depolarization mediated by receptors on the neuronal cell body. The third was suppression of acetylcholine release at nicotinic synapses on the cell bodies and was mediated by presynaptic 5-HT receptors. The initial component of the biphasic depolarization was a rapidly activating response characterized by inc

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10

Cheng, Yuan Shan, Yuan Sheng Liu, Godfrey ChiFung Chan, Jie Yu Ye, Yu Lung Lau, and Mo Yang. "Effects of Serotonin on Proplatelet Formation and F-actin Reorganization in Human Megakaryocytes." Blood 110, no. 11 (2007): 2108. http://dx.doi.org/10.1182/blood.v110.11.2108.2108.

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Abstract We previously reported that serotonin (5-HT) is a growth factor for hematopoietic stem cells and megakaryocytic progenitor (Yang et al, Stem Cells, 2007). We further proposed a possible role of serotonin on megakaryocyte differentiation and platelet formation. The effect of serotonin on proplatelet formation and F-actin reorganization in human megakaryocytes (MKs) was investigated in this study. Our results showed that: There was a stimulating effect of serotonin on proplatelet formation in human bone marrow megakaryocytes. Human BM MK progenitors cultured in serum free medium with ei

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11

Mo, Yang, Su-yi Li, En-yu Liang, Qi-zhou Lian, and Fan-yi Meng. "The Expression of Functional Dopamine and Serotonin Receptors on Megakaryocytes." Blood 124, no. 21 (2014): 4205. http://dx.doi.org/10.1182/blood.v124.21.4205.4205.

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Abstract Monoamine dopamine (DA) and serotonin (5-HT) can affect the functions of many cells including platelets. Our previous studies have shown that 5-HT has potent effects on promoting megakaryopoiesis and platelet formation (Yang et al, Stem Cells, 2007; 2014). In this study, our hypothesis is that both DA and 5-HT receptors may have the development expression on platelets, megakaryocytes (MK) and hematopoietic stem cells (HSCs). The expression of DA receptors: DA1, DA2 and 5-HT receptors: 5-HT2A, 2B and 2C on these hematopoietic cells, and the effect of DA and 5-HT on the cell proliferati

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Lucas-Osma, Ana M., Yaqing Li, Katie Murray, et al. "5-HT1D receptors inhibit the monosynaptic stretch reflex by modulating C-fiber activity." Journal of Neurophysiology 121, no. 5 (2019): 1591–608. http://dx.doi.org/10.1152/jn.00805.2018.

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The monosynaptic stretch reflex (MSR) plays an important role in feedback control of movement and posture but can also lead to unstable oscillations associated with tremor and clonus, especially when increased with spinal cord injury (SCI). To control the MSR and clonus after SCI, we examined how serotonin regulates the MSR in the sacrocaudal spinal cord of rats with and without a chronic spinal transection. In chronic spinal rats, numerous 5-HT receptor agonists, including zolmitriptan, methylergonovine, and 5-HT, inhibited the MSR with a potency highly correlated to their binding affinity to

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Yatham, Lakshmi N., Peter F. Liddle, Jonathan Erez, et al. "Brain serotonin-2 receptors in acute mania." British Journal of Psychiatry 196, no. 1 (2010): 47–51. http://dx.doi.org/10.1192/bjp.bp.108.057919.

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BackgroundAlthough 5-hydroxytryptamine (5-HT) has been implicated in mania, the precise alterations in the 5-HT system remain elusive.AimsTo assess brain 5-HT2 receptors in drug-free individuals experiencing a manic episode in comparison with healthy volunteers using positron emission tomography (PET).MethodParticipants (n = 10) with DSM–IV bipolar I disorder – manic episode and healthy controls (n = 10) underwent [18F]- setoperone scans. The differences in 5-HT2 receptor binding potential between the two groups were determined using statistical parametric mapping (SPM) analysis.ResultsAge was

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Nebigil, C. G., N. Etienne, B. Schaerlinger, P. Hickel, J. ‐M Launay, and L. Maroteaux. "Developmentally regulated serotonin 5‐HT 2B receptors." International Journal of Developmental Neuroscience 19, no. 4 (2001): 365–72. http://dx.doi.org/10.1016/s0736-5748(01)00022-3.

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15

Peroutka, Stephen J. "Molecular biology of serotonin (5-HT) receptors." Synapse 18, no. 3 (1994): 241–60. http://dx.doi.org/10.1002/syn.890180310.

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16

Shih, Jean C., Wu Yang, Kevin Chen, and Tim Gallaher. "Molecular biology of serotonin (5-HT) receptors." Pharmacology Biochemistry and Behavior 40, no. 4 (1991): 1053–58. http://dx.doi.org/10.1016/0091-3057(91)90125-l.

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17

Zhang, Yan, Yu Han, Rui Yang, et al. "Effect of Serotonin (5-Hydroxytryptamine) on Follicular Development in Porcine." International Journal of Molecular Sciences 25, no. 17 (2024): 9596. http://dx.doi.org/10.3390/ijms25179596.

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5-Hydroxytryptamine (5-HT) is an inhibitory neurotransmitter widely distributed in mammalian tissues, exerting its effects through binding to various receptors. It plays a crucial role in the proliferation of granulosa cells (GCs) and the development of follicles in female animals, however, its effect on porcine follicle development is not clear. The aim of this study is to investigate the expression of 5-HT and its receptors in various parts of the pig ovary, as well as the effect of 5-HT on porcine follicular development by using ELISA, quantitative real-time PCR (qPCR) and EdU assays. First

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18

Hasséssian, Haroutioun, Philippe Poulat, Edith Hamel, Tomás A. Reader, and Réjean Couture. "Spinai cord serotonin receptors in cardiovascular regulation and potentiation of the pressor response to intrathecal substance P after serotonin depletion." Canadian Journal of Physiology and Pharmacology 71, no. 7 (1993): 453–64. http://dx.doi.org/10.1139/y93-067.

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The aim of this study was to characterize, in conscious rats, the spinal cord 5-hydroxytryptamine (5-HT) receptors involved in mean arterial pressure (MAP) and heart rate (HR) regulation as well as to examine the influence of bulbospinal 5-HT fibers on cardiovascular responses to intrathecal (i.t.) substance P (SP). The i.t. injection of 5-HT or 5-carboxamidotryptamine (5-CT) (5-HT1A, 1B, 1D agonist) reduced MAP and increased HR in a dose-dependent manner. In contrast, the agonists 8-hydroxy-2-(di-n-propylamino)tetraiin (8-OH-DPAT, 5-HT1A agonist) and α-CH3-5-HT (5-HT1C and 5-HT2) only caused

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Guzel, Tomasz, and Dagmara Mirowska-Guzel. "The Role of Serotonin Neurotransmission in Gastrointestinal Tract and Pharmacotherapy." Molecules 27, no. 5 (2022): 1680. http://dx.doi.org/10.3390/molecules27051680.

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5-Hydroxytryptamine (5-HT, serotonin) is a neurotransmitter in both the central nervous system and peripheral structures, acting also as a hormone in platelets. Although its concentration in the gut covers >90% of all organism resources, serotonin is mainly known as a neurotransmitter that takes part in the pathology of mental diseases. Serotonin modulates not only CNS neurons, but also pain transmission and platelet aggregation. In the periphery, 5-HT influences muscle motility in the gut, bronchi, uterus, and vessels directly and through neurons. Serotonin synthesis starts from hydroxylat

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Tolloczko, B., Y. L. Jia, and J. G. Martin. "Serotonin-evoked calcium transients in airway smooth muscle cells." American Journal of Physiology-Lung Cellular and Molecular Physiology 269, no. 2 (1995): L234—L240. http://dx.doi.org/10.1152/ajplung.1995.269.2.l234.

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Serotonin (5-HT) is an important mediator of allergic airway narrowing in several animal species. The present study was designed to characterize the receptor subtypes that mediate 5-HT-induced airway responses in the rat. To do this, we measured Ca2+ transients and adenosine 3',5'-cyclic monophosphate (cAMP) production evoked by 5-HT in cultured rat tracheal smooth muscle cells as well as 5-HT-induced contractions of isolated tracheal rings. 5-HT (10(-6) to 10(-4) M) triggered a rapid increase in intracellular Ca2+ concentration ([Ca2+]i) followed by a second phase of sustained, elevated, and

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Beliveau, Vincent, Melanie Ganz, Ling Feng, et al. "A High-Resolution In Vivo Atlas of the Human Brain's Serotonin System." Journal of Neuroscience 37, no. 1 (2017): 120–28. https://doi.org/10.1523/JNEUROSCI.2830-16.2016.

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<strong>Abstract</strong> The serotonin (5-hydroxytryptamine, 5-HT) system modulates many important brain functions and is critically involved in many neuropsychiatric disorders. Here, we present a high-resolution, multidimensional, in vivo atlas of four of the human brain's 5-HT receptors (5-HT<sub>1A</sub>, 5-HT<sub>1B</sub>, 5-HT<sub>2A</sub>, and 5-HT<sub>4</sub>) and the 5-HT transporter (5-HTT). The atlas is created from molecular and structural high-resolution neuroimaging data consisting of positron emission tomography (PET) and magnetic resonance imaging (MRI) scans acquired in a

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Delaney, Cassidy, Jason Gien, Theresa R. Grover, Gates Roe, and Steven H. Abman. "Pulmonary vascular effects of serotonin and selective serotonin reuptake inhibitors in the late-gestation ovine fetus." American Journal of Physiology-Lung Cellular and Molecular Physiology 301, no. 6 (2011): L937—L944. http://dx.doi.org/10.1152/ajplung.00198.2011.

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Maternal use of selective serotonin (5-HT) reuptake inhibitors (SSRIs) is associated with an increased risk for persistent pulmonary hypertension of the newborn (PPHN), but little is known about 5-HT signaling in the developing lung. We hypothesize that 5-HT plays a key role in maintaining high pulmonary vascular resistance (PVR) in the fetus and that fetal exposure to SSRIs increases 5-HT activity and causes pulmonary hypertension. We studied the hemodynamic effects of 5-HT, 5-HT receptor antagonists, and SSRIs in chronically prepared fetal sheep. Brief infusions of 5-HT (3–20 μg) increased P

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Eberle-Wang, K., B. T. Braun, and K. J. Simansky. "Serotonin contracts the isolated rat pylorus via a 5-HT2-like receptor." American Journal of Physiology-Regulatory, Integrative and Comparative Physiology 266, no. 1 (1994): R284—R291. http://dx.doi.org/10.1152/ajpregu.1994.266.1.r284.

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Serotonin (5-HT) produced concentration-dependent contractions of the isolated rat pylorus in vitro. Serotonergic contractions were antagonized by the calcium L-channel blocker, diltiazem, but not by tetrodotoxin or atropine. Three drugs that block 5-HT2 receptors, ketanserin, xylamidine, and methysergide, unsurmountably inhibited contractions to 5-HT. In contrast, antagonists of 5-HT3, 5-HT1A/1B, beta-adrenergic, or alpha 1-adrenergic receptors did not alter the response to 5-HT. Devazepide, an antagonist of cholecystokinin (CCK) type-A receptors, blocked contraction produced by CCK-8 but not

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Yu, H. J., and A. Yamaguchi. "5-HT2C-Like Receptors in the Brain of Xenopus laevis Initiate Sex-Typical Fictive Vocalizations." Journal of Neurophysiology 102, no. 2 (2009): 752–65. http://dx.doi.org/10.1152/jn.90469.2008.

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Vocalizations of male and female African clawed frogs ( Xenopus laevis) are generated by brain stem central pattern generators. Serotonin (5-HT) is likely important for vocal initiation because, when applied in vitro, sex-typical fictive vocalizations are evoked from isolated brains. To explore the mechanisms underlying vocal initiation, we identified the types of serotonin receptors mediating vocal activation pharmacologically using a whole brain, fictive preparation. The results showed that 5-HT2C–like receptors are important for activation of fictive vocalizations in the sexes. 5-HT2C recep

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Voronova, Irina P. "5-HT Receptors and Temperature Homeostasis." Biomolecules 11, no. 12 (2021): 1914. http://dx.doi.org/10.3390/biom11121914.

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The present review summarizes the data concerning the influence of serotonin (5-HT) receptors on body temperature in warm-blooded animals and on processes associated with its maintenance. This review includes the most important part of investigations from the first studies to the latest ones. The established results on the pharmacological activation of 5-HT1A, 5-HT3, 5-HT7 and 5-HT2 receptor types are discussed. Such activation of the first 3 type of receptors causes a decrease in body temperature, whereas the 5-HT2 activation causes its increase. Physiological mechanisms leading to changes in

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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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Ishine, Takaaki, Isabelle Bouchelet, Edith Hamel, and Tony J. F. Lee. "Serotonin 5-HT7 receptors mediate relaxation of porcine pial veins." American Journal of Physiology-Heart and Circulatory Physiology 278, no. 3 (2000): H907—H912. http://dx.doi.org/10.1152/ajpheart.2000.278.3.h907.

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Isolated porcine pial veins in the presence of active muscle tone have been shown to exhibit rhythmic contractions (RC) that are inhibited by serotonin (5-HT) in a concentration-dependent manner. The 5-HT inhibition of RC is mediated by an as yet unidentified 5-HT receptor subtype located on the vascular smooth muscle. 5-carboxamidotryptamine, which is a potent but nonselective agonist at 5-HT7receptors, has been shown to be the most potent inhibitor of RC in porcine pial veins. Therefore, the present study was designed to determine if the 5-HT-mediated inhibition of RC in pial veins is mediat

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Akhmetova, М. Zh, G. М. Tykezhanova, F. А. Mindubaeva, and R. R. Nigmatullina. "Serotonin: biological properties and its receptors." Bulletin of the Karaganda University “Biology medicine geography Series” 94, no. 2 (2019): 71–79. https://doi.org/10.31489/2019bmg2/71-79.

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In the last decade, much attention has been paid to the study of the serotonergic system. The molecular and cellular mechanisms of the synthesis of serotonin, its metabolism and receptor interaction are well studied. The wide range of serotonin effects is explained by the presence of a wide variety of serotonin receptors. The serotonin (5-hydroxytryptamine, 5-HT) is the main mediator of the serotonergic system. In human the role of 5-HT in the central nervous system (CNS) is best characterized, where the amine remain in force as a neuro-transmitter in neural synapses and participates in the fo

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Coccaro, Emil F. "Central Serotonin and Impulsive Aggression." British Journal of Psychiatry 155, S8 (1989): 52–62. http://dx.doi.org/10.1192/s0007125000291769.

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The role of central serotonergic (5-HT) system dysfunction in the regulation of aggression in both animals and man has been investigated for more than the past two decades. Evidence for reduced central 5-HT in the mediation of aggression comes from both behavioural and correlative studies. Functional reduction and augmentation of 5-HT activity is respectively associated with increased and decreased aggression in various animal models of aggression. While similar studies in man have not been performed, strong and consistent associations between indices reflecting reduced pre-synaptic 5-HT activ

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Garattini, S., T. Mennini, and R. Samanin. "Reduction of Food Intake by Manipulation of Central Serotonin Current Experimental Results." British Journal of Psychiatry 155, S8 (1989): 41–51. http://dx.doi.org/10.1192/s0007125000291757.

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Serotonergic anorectics are correctly defined only if they enhance 5-HT transmission and have their anorectic effects inhibited by drugs that block 5-HT receptors. Fenfluramine, the prototype indirect 5-HT agonist, and its metabolite, norfenfluramine, act as 5-HT releasers and uptake inhibitors and are both more effective in the dextro form. They lack the stimulant activity and do not cause hyperthermia or stereotypical behaviour as is characteristic of amphetamines. The anorectic effect of those drugs is attenuated by metergoline, a 5-HT receptor antagonist, in animals and man; 5-HT uptake in

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Fujinoki, Masakatsu. "Serotonin-enhanced hyperactivation of hamster sperm." REPRODUCTION 142, no. 2 (2011): 255–66. http://dx.doi.org/10.1530/rep-11-0074.

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The effects of serotonin on reproductive function were examined using hamster spermatozoa. When serotonin at concentrations from 1 fmol/l to 1 μmol/l was added to modified Tyrode's albumin lactate pyruvate (mTALP) medium, hyperactivation was significantly enhanced. Agonists and antagonists of 5-hydroxytryptamine hydrochloride (5-HT) receptors (5-HT2 and 5-HT4 receptors) were added to the medium. Both 5-HT2 and 5-HT4 receptor agonists significantly enhanced hyperactivation, although the effect was greater than the former. However, both 5-HT2 and 5-HT4 receptor antagonists significantly suppress

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Zhang, B., and R. M. Harris-Warrick. "Multiple receptors mediate the modulatory effects of serotonergic neurons in a small neural network." Journal of Experimental Biology 190, no. 1 (1994): 55–77. http://dx.doi.org/10.1242/jeb.190.1.55.

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The gastropyloric receptor (GPR) cells are a set of cholinergic/serotonergic mechanosensory neurons that modulate the activity of neural networks in the crab stomatogastric ganglion (STG). Stimulation of these cells evokes a variety of slow modulatory responses in different STG neurons that are mimicked by exogenously applied serotonin (5-HT); these responses include tonic inhibition, tonic excitation and induction of rhythmic bursting. We used pharmacological agonists and antagonists to show that these three classes of modulatory response in the STG neurons are mediated by distinct 5-HT recep

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Dobbins, David E. "Receptor mechanisms of serotonin-induced prenodal lymphatic constriction in the canine forelimb." American Journal of Physiology-Heart and Circulatory Physiology 274, no. 2 (1998): H650—H654. http://dx.doi.org/10.1152/ajpheart.1998.274.2.h650.

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Numerous endogenous vasoactive agents have been shown to cause lymphatic smooth muscle contraction. In this study, we assessed the ability of serotonin (5-HT) to alter lymphatic smooth muscle activity and elucidated the receptor mechanisms of 5-HT’s actions. Both intralymphatic and intra-arterial administration of 5-HT significantly increased lymphatic smooth muscle activity in lymphatics perfused at constant flow, as indicated by an increase in lymphatic perfusion pressure. The 5-HT-induced increase in lymphatic perfusion pressure is attenuated but not blocked by the intra-arterial infusion o

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Dumitriu, Bogdan, Jonathan E. Cohen, Qin Wan, Andreea M. Negroiu, and Thomas W. Abrams. "Serotonin Receptor Antagonists Discriminate Between PKA- and PKC-Mediated Plasticity in Aplysia Sensory Neurons." Journal of Neurophysiology 95, no. 4 (2006): 2713–20. http://dx.doi.org/10.1152/jn.00642.2005.

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Highly selective serotonin (5-hydroxytryptamine, 5-HT) receptor antagonists developed for mammals are ineffective in Aplysia due to the evolutionary divergence of neurotransmitter receptors and because the higher ionic strength of physiological saline for marine invertebrates reduces antagonist affinity. It has therefore been difficult to identify antagonists that specifically block individual signaling cascades initiated by 5-HT. We studied two broad-spectrum 5-HT receptor antagonists that have been characterized biochemically in Aplysia CNS: methiothepin and spiperone. Methiothepin is highly

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Chen, Wenbo, Xiaoyan Gao, Huixin Wang, et al. "Identification and Pharmacological Characterization of Two Serotonin Type 7 Receptor Isoforms from Mythimna separata." International Journal of Molecular Sciences 24, no. 1 (2022): 655. http://dx.doi.org/10.3390/ijms24010655.

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Serotonin (5-hydroxytryptamine, 5-HT) is an important neuroactive molecule, as neurotransmitters regulate various biological functions in vertebrates and invertebrates by binding and activating specific 5-HT receptors. The pharmacology and tissue distribution of 5-HT receptors have been investigated in several model insects, and these receptors are recognized as potential insecticide targets. However, little is known about the pharmacological characterization of the 5-HT receptors in important agricultural pests. In this study, we investigated the sequence, pharmacology, and tissue distributio

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Yang, Mo, Karen Kwar Har Li, C. K. Y. Chuen, Ki Wai Chick, Nga Hin Pong, and Tai Fai Fok. "An Alternative Growth Factor for Hematopoietic Stem Cells and Megakaryocytopoiesis." Blood 104, no. 11 (2004): 2060. http://dx.doi.org/10.1182/blood.v104.11.2060.2060.

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Abstract The role of serotonin (5-hydroxytryptamine, 5-HT) on the regulation of blood stem cell proliferation and thrombopoiesis has not been recognized until 1996, when we reported that serotonin has a mitogenic effect on murine megakaryocytopoiesis via 5-HT2 receptors (Yang et al, Blood Coagul Fibrin 1996). Our study also indicated that the uptake ability of serotonin is well established in human megakaryoblasts (Yang et al, Int J Hematol, 1996). 5-HT 2A, 2B and 2C receptors were identified on human megakaryocytes and serotonin also promoted human megakaryocytopoiesis via these receptors (Ya

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Ikarashi, Yasushi, Kyoji Sekiguchi, and Kazushige Mizoguchi. "Serotonin Receptor Binding Characteristics of Geissoschizine Methyl Ether, an Indole Alkaloid in Uncaria Hook." Current Medicinal Chemistry 25, no. 9 (2018): 1036–45. http://dx.doi.org/10.2174/0929867324666170320114713.

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Background: Geissoschizine methyl ether (GM) is one of the indole alkaloids in Uncaria hook, and an active ingredient of yokukansan (YKS) that improves behavioral and psychological symptoms of dementia (BPSD) in patients with several types of dementia. The pharmacological action of GM has been related to various serotonin (5-HT) receptor subtypes. Objective: The aim of this article is to review the binding characteristics of GM to the 5-HT receptor subtypes in the brains using our own data and previous findings. Method: Competitive receptor-binding and agonist/antagonist activity assays for se

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Launay, J. M., D. Bondoux, M. J. Oset-Gasque, et al. "Increase of human platelet serotonin uptake by atypical histamine receptors." American Journal of Physiology-Regulatory, Integrative and Comparative Physiology 266, no. 2 (1994): R526—R536. http://dx.doi.org/10.1152/ajpregu.1994.266.2.r526.

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Histamine and the guanosine 3',5'-cyclic monophosphate (cGMP)-inducing agent sodium nitroprusside both increased serotonin (5-HT) uptake and cGMP levels in isolated human platelets in vitro. Histaminergic stimulation was observed at concentrations ranging from 10 nM to 0.25 microM [mean effective concentration (EC50) = 0.1 microM histamine]. The inhibition produced by the H2-receptor antagonists tiotidine, metiamide, and cimetidine was 10-10(5) times more potent on histamine receptors regulating 5-HT uptake and cGMP generation in human platelets than on the histaminergic receptors H1, HIC, H2,

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Whale, Richard, Elizabeth M. Clifford, Zubin Bhagwagar, and Philip J. Cowen. "Decreased sensitivity of 5-HT1D receptors in melancholic depression." British Journal of Psychiatry 178, no. 5 (2001): 454–57. http://dx.doi.org/10.1192/bjp.178.5.454.

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BackgroundBrain serotonin (5-HT) function is abnormal in major depression, but the involvement of different 5-HT receptor subtypes has been little studied. The availability of selective ligands now makes it possible to test the sensitivity of 5-HT1D receptors in patients with depression.AimsThe aim of the study was to use the 5-HT1D receptor agonist, zolmitriptan, to test the sensitivity of 5-HT1D receptors in patients with depression before and after treatment with selective serotonin reuptake inhibitors (SSRIs).MethodWe measured the growth hormone response to zolmitriptan (5 mg orally) in pa

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Meek, Autumn R., Alexander Morzycki, Michael D. Carter, Christopher Barden, and Donald F. Weaver. "Serotonin as a drug receptor for Li+: a computational study." Canadian Journal of Chemistry 96, no. 7 (2018): 694–702. http://dx.doi.org/10.1139/cjc-2017-0665.

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Although Li+ is widely used to treat bipolar disorder, its antidepressant pharmacological mechanism of action remains unelucidated. Herein, based on molecular modelling studies, we present the novel hypothesis that one possible receptor for Li+ is serotonin (5-hydroxytryptamine, 5-HT), a small molecule neurotransmitter rather than a large macromolecular protein. The resulting Li+/5-HT drug–receptor complex subsequently interacts with “upstream” macromolecular receptors such as the 5-HT1A receptor differently than 5-HT alone, producing an enhanced antidepressant effect. The notion that a neurot

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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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Alsip, N. L., and P. D. Harris. "Receptor mediation of microvascular responses to serotonin in striated muscle." American Journal of Physiology-Heart and Circulatory Physiology 261, no. 5 (1991): H1525—H1533. http://dx.doi.org/10.1152/ajpheart.1991.261.5.h1525.

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Serotonin constricts large arterioles and dilates small arterioles in striated muscle. Our study aimed to identify the receptors that mediate this differential response. Rats were anesthetized with pentobarbital sodium, and the cremaster muscle was prepared for videomicroscopy. Serotonin, applied topically, caused a constriction of large (A1) arterioles that was attenuated by cyproheptadine, methysergide, and LY 53857 but not by MDL 7222, phentolamine, propranolol, or diphenhydramine. The 5-hydroxytryptamine (5-HT)-induced constriction of A1 arterioles was mimicked by alpha-CH3-5-HT but not by

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Fukushima, Teruyuki, Toshiki Ohtsubo, Masayuki Tsuda, Yuchio Yanagawa, and Yuuichi Hori. "Facilitatory Actions of Serotonin Type 3 Receptors on GABAergic Inhibitory Synaptic Transmission in the Spinal Superficial Dorsal Horn." Journal of Neurophysiology 102, no. 3 (2009): 1459–71. http://dx.doi.org/10.1152/jn.91160.2008.

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Analgesic effects of serotonin (5-hydroxytryptamine [5-HT]) type 3 (5-HT3) receptors may involve the release of γ-aminobutyric acid (GABA) in the spinal dorsal horn. However, the precise synaptic mechanisms for 5-HT3 receptor-mediated spinal analgesia are not clear. In this study, we investigated whether GABAergic neurons in the superficial dorsal horn (SDH) express functional 5-HT3 receptors and how these 5-HT3 receptors affect GABAergic inhibitory synaptic transmission in the SDH, by using slice preparations from adult glutamate decarboxylase 67–green fluorescent protein (GAD67-GFP) knock-in

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Ghafir El Idrissi, Imane, Angela Santo, Enza Lacivita, and Marcello Leopoldo. "Multitarget-Directed Ligands Hitting Serotonin Receptors: A Medicinal Chemistry Survey." Pharmaceuticals 17, no. 9 (2024): 1238. http://dx.doi.org/10.3390/ph17091238.

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Serotonin (5-hydroxytryptamine, 5-HT) is a ubiquitous neurotransmitter in the human body. In the central nervous system, 5-HT affects sleep, pain, mood, appetite, and attention, while in the peripheral nervous system, 5-HT modulates peristalsis, mucus production, and blood vessel dilation. Fourteen membrane receptors mediate 5-HT activity. In agreement with the crucial roles played by 5-HT, many drugs target 5-HT receptors (5-HTRs). Therefore, it is unsurprising that many efforts have been devoted to discovering multitarget-directed ligands (MTDLs) capable of engaging one or more 5-HTRs plus a

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Majeed, Zana R., Charles D. Nichols, and Robin L. Cooper. "5-HT stimulation of heart rate in Drosophila does not act through cAMP as revealed by pharmacogenetics." Journal of Applied Physiology 115, no. 11 (2013): 1656–65. http://dx.doi.org/10.1152/japplphysiol.00849.2013.

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The fruit fly, Drosophila melanogaster, is a good experimental organism to study the underlying mechanism of heart rate (HR) regulation. It is already known that many neuromodulators (serotonin, dopamine, octopamine, acetylcholine) change the HR in Drosophila melanogaster larvae. In this study, we investigated the role of cAMP-PKA signaling pathway in HR regulation and 5-HT positive chronotropic action. In order to obtain insight into the 5-HT mechanism of action in larvae cardiomyocytes, genetic and pharmacological approaches were used. We used transgenic flies that expressed the hM4Di recept

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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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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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Borsini, Franco. "Pharmacology of 5-HT1A Receptors: Critical Aspects." CNS Spectrums 3, no. 10 (1998): 17–38. http://dx.doi.org/10.1017/s1092852900006635.

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AbstractMyriad difficulties exist in analyzing the pharmacology of the serotonin 1A (5-HT1A) receptor. The receptor may demonstrate a different activity depending on the tissue or species used for analysis, the agent used, laboratory conditions, and differences between in vitro and in vivo effects of compounds. Affinity for 5-HT receptors also varies widely, presenting difficulties in drawing definitive conclusions on affinity values for various compounds. At least two possibilities exist to explain the diversity of pharmacology of 5-HT receptors. First, it is possible that different 5-HT1A re

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Watts, Stephanie W., Kathryn W. Schenck, and Marlene L. Cohen. "Selectlve desensitization of 5-hydroxytryptamine 2A receptor mediated contraction in guinea pig trachea." Canadian Journal of Physiology and Pharmacology 72, no. 5 (1994): 463–70. http://dx.doi.org/10.1139/y94-067.

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5-Hydroxytryptamine (serotonin, 5-HT) contracts the guinea pig trachea through stimulation of 5-HT2A receptors, an effect previously reported to rapidly desensitize. The present studies were designed to examine further the putative desensitization to serotonin. In vitro studies investigating functional desensitization of the guinea pig tracheal 5-HT2A receptor documented that 5-HT (3 × 10−7 M) significantly (50%) but incompletely reduced subsequent tracheal maximal contraction to 5-HT. In contrast, an equieffective concentration of carbamylcholine (3 × 10−8 M) did not reduce guinea pig trachea

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Rademacher, David J., Sachin Patel, W. S. Vanessa Ho, et al. "U-46619 but not serotonin increases endocannabinoid content in middle cerebral artery: evidence for functional relevance." American Journal of Physiology-Heart and Circulatory Physiology 288, no. 6 (2005): H2694—H2701. http://dx.doi.org/10.1152/ajpheart.00978.2004.

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Cerebral vascular smooth muscle cells express the CB1 cannabinoid receptor, and CB1 receptor agonists produce vasodilation of cerebral arteries. The purpose of this study was to determine whether vasoconstriction of rat middle cerebral artery (MCA) results in the local formation of endocannabinoids (eCBs), which, via activation of CB1 receptors, oppose the vasoconstriction in a feedback manner. The thromboxane A2 (TXA2) mimetic U-46619 significantly increased N-arachidonylethanolamine (AEA) and 2-arachidonylglycerol (2-AG) content of isolated MCA, whereas 5-hydroxytrypamine (5-HT) decreased AE

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