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*  5-HT receptor
The 7 general serotonin receptor classes include a total of 14 known serotonin receptors. The specific types have been ... Rubenstein LA, Lanzara RG (2005-02-16). "Activation of G protein-coupled receptors entails cysteine modulation of agonist ... The serotonin receptors are activated by the neurotransmitter serotonin, which acts as their natural ligand. The serotonin ... The genes coding for serotonin receptors are expressed across the mammalian brain. Genes coding for different receptors types ...
*  5-HT2C receptor agonist
Later, animal studies showed that serotonin receptor agonists might act as a mediator of satiety. Serotonin has been implicated ... In the late 1960s, non-selective serotonin receptor antagonists demonstrated a relationship between serotonin receptors and ... The serotonin receptor agonist mCPP has a significant affinity for 5-HT2C receptors. mCPP patients experience multiple side ... Bray, Jenelle K.; Goddard, William A. (2008). "The structure of human serotonin 2c G-protein-coupled receptor bound to agonists ...
*  Milnacipran
... exerts no significant actions on H1, α1, D1, D2, and mACh receptors, nor on benzodiazepine and opioid binding sites ... Lopez-Ibor J, Guelfi JD, Pletan Y, Tournoux A, Prost JF (1996). "Milnacipran and selective serotonin reuptake inhibitors in ... MAOIs - hyperserotonergia (serotonin syndrome), potentially lethal hypertensive crisis 5-HT1 receptor agonists - coronary ... Papakostas GI, Fava M (2007). "A meta-analysis of clinical trials comparing milnacipran, a serotonin--norepinephrine reuptake ...
*  Eletriptan
... is a serotonin receptor agonist, specifically an agonist of certain 5-HT1 family receptors. Eletriptan binds with ... This is due to the unusual side effect of coronary vasoconstriction due to serotonin 5HT1B antagonism, which can precipitate a ... receptors. It has a modest affinity to the 5-HT[1A, 1E, 2B, 7] receptors, and little to no affinity at the 5-HT[2A, 2C, 3, 4, ... 5A, 6] receptors. Eletriptan has no significant affinity or pharmacological activity at adrenergic α1, α2, or β; dopaminergic ...
*  RU-28306
... is a tricyclic tryptamine derivative which acts as a serotonin receptor agonist, with selectivity for 5-HT1 and 5-HT2 ... 4,5-DHP-DMT Bay R 1531 RU-24,969 Taylor EW, Nikam S, Weck B, Martin A, Nelson D. Relative selectivity of some conformationally ... 5-HT1A and 5-HT2 recognition sites. Life Sciences. 1987 Oct 19;41(16):1961-9. PMID 3657392. ... though with relatively higher affinity for 5-HT2 subtypes and lower for 5-HT1. ...
*  5-HT1E receptor
This receptor is unique among the serotonin receptors in that it is not known to be expressed by rats or mouse species, all of ... Both receptors are Gi-coupled (inhibit adenylate cyclase activity) and both receptors have high affinities for 5-HT and low ... Gi-coupled serotonin receptor). The human gene is denoted as HTR1E. The function of the 5-HT1E receptor is unknown due to the ... serotonin) 1E receptor (5-HT1E) is a highly expressed human G-protein coupled receptor that belongs to the 5-HT1 receptor ...
*  Naratriptan
... serotonin) agonists. A meta-analysis of 53 clinical trials has shown that all triptans are effective for treating migraine at ... Medline Plus Drug Information for Naratriptan Accessed 6 August 2009 Triptans (serotonin, 5-HT1B/1D agonists) in migraine: ... It is a selective 5-HT1 receptor subtype agonist. Naratriptan is used for the treatment of the acute migraine attacks and the ... 4997841, Alexander W. Oxford, et al., Indole Derivatives, March 5, 1991 DeArment, Alaric (2010-07-09). "Roxane launches generic ...
*  5-HT1F receptor
Amlaiky N, Ramboz S, Boschert U, Plassat JL, Hen R (Oct 1992). "Isolation of a mouse "5HT1E-like" serotonin receptor expressed ... serotonin) receptor 1F, also known as HTR1F is a 5-HT1 receptor protein and also denotes the human gene encoding it. 5-n- ... serotonin) receptor 1F". Adham N, Kao HT, Schecter LE, Bard J, Olsen M, Urquhart D, Durkin M, Hartig PR, Weinshank RL, Branchek ... "Assignment of the human serotonin 1F receptor gene (HTR1F) to the short arm of chromosome 3 (3p13-p14.1)". Molecular Membrane ...
*  5-Methoxytryptamine
Wu PH, Gurevich N, Carlen PL (1988). "Serotonin-1A receptor activation in hippocampal CA1 neurons by 8-hydroxy-2-(di-n- ... Roth, Brian (2006). The serotonin receptors. Humana Press. p. 133. ISBN 978-1-58829-568-2. S. Nigra / Domenech T, et al., 1997 ... Glennon RA, Dukat M, Westkaemper RB (2000-01-01). "Serotonin Receptor Subtypes and Ligands". American College of ... Measured affinity for some receptors (not a complete list): 5-HT1B receptors (Ki = 35 nM) 5-HT1D receptors (Ki = 7.3 nM) 5-HT1E ...
*  5-HT7 receptor
Agonists mimic the effects of the endogenous ligand, which is serotonin at the 5-HT7 receptor (↑cAMP). 5-Carboxamidotryptamine ... bind the receptor and have no intrinsic activity but will block the activity of agonists or inverse agonists. Inverse agonists ... Bard JA, Zgombick J, Adham N, Vaysse P, Branchek TA, Weinshank RL (November 1993). "Cloning of a novel human serotonin receptor ... role of G protein-coupled receptor kinases and arrestins in receptor desensitization and resensitization". Receptors & Channels ...
*  5-HT5A receptor
When selective activation of this receptor is desired in scientific research, the non-selective serotonin receptor agonist 5- ... Marazziti D, Ori M, Nardini M, Rossi A, Nardi I, Cassano GB (2001). "mRNA expression of serotonin receptors of type 2C and 5A ... serotonin) receptor 5A, also known as HTR5A, is a protein that in humans is encoded by the HTR5A gene. The gene described in ... It also appears to serve as a presynaptic serotonin autoreceptor. The neurotransmitter serotonin (5-hydroxytryptamine, 5-HT) ...
*  5-HT1D receptor
Bremner, D. H.; Ringan, N. S.; Wishart, G. (1997). "Modeling of the agonist binding site of serotonin human 5-HT1A, 5-HT1Dα and ... serotonin) receptor 1D". Millan, M.J., et al., Signaling at G-protein-coupled serotonin receptors: recent advances and future ... "Chromosomal mapping of A1 and A2 adenosine receptors, VIP receptor, and a new subtype of serotonin receptor". Genomics. 11 (1 ... Weinshank, R. L.; Zgombick, J. M.; Macchi, M. J.; Branchek, T. A.; Hartig, P. R. (1992). "Human Serotonin-1d Receptor Is ...
*  5-HT1B receptor
Tsai SJ, Wang YC, Chen JY, Hong CJ (2003). "Allelic variants of the tryptophan hydroxylase (A218C) and serotonin 1B receptor (A ... inverse agonist) SB-236,057 (inverse agonist) In humans the protein is coded by the gene HTR1B. A genetic variant in the ... Weinshank RL, Zgombick JM, Macchi MJ, Branchek TA, Hartig PR (Apr 1992). "Human serotonin 1D receptor is encoded by a subfamily ... Hasegawa Y, Higuchi S, Matsushita S, Miyaoka H (Apr 2002). "Association of a polymorphism of the serotonin 1B receptor gene and ...
*  5-HT3 receptor
These agents are not agonists at the receptor, but increase the affinity or efficacy of the receptors for an agonist: Indole ... or serotonin) receptors which are G protein-coupled receptors. This ion channel is cation-selective and mediates neuronal ... 1000x selectivity over other serotonin receptors SR-57227 Varenicline YM-31636 Antagonists for the receptor (sorted by their ... When the receptor is activated to open the ion channel by agonists, the following effects are observed: CNS: nausea and ...
*  5-HT4 receptor
This gene is a member of the family of human serotonin receptors, which are G protein-coupled receptors that stimulate cAMP ... BIMU-8 Cisapride CJ-033,466 - partial agonist ML-10302 Mosapride Prucalopride Renzapride RS-67506 RS-67333 - partial agonist ... Cichon S, Kesper K, Propping P, Nöthen MM (1998). "Assignment of the human serotonin 4 receptor gene (HTR4) to the long arm of ... Norum JH, Hart K, Levy FO (January 2003). "Ras-dependent ERK activation by the human G(s)-coupled serotonin receptors 5-HT4(b) ...
*  5-HT6 receptor
The 5HT6 receptor is a subtype of 5HT receptor that binds the endogenous neurotransmitter serotonin (5-hydroxytryptamine, 5HT ... Full agonist at human 5HT6 receptors E-6801 E-6837 - partial agonist at rat 5-HT6 receptors. Orally active in rats, and caused ... IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. serotonin 6 receptor at ... serotonin) receptor 6". Woolley ML, Marsden CA, Fone KC (Feb 2004). "5HT6 receptors". Current Drug Targets. CNS and ...
*  Rizatriptan
... acts as an agonist at serotonin 5-HT1B and 5-HT1D receptors. Like the other triptans sumatriptan and zolmitriptan, ... Rizatriptan (trade name Maxalt) is a 5-HT1 receptor agonist of the triptan class of drugs developed by Merck & Co. for the ... It is available in strengths of 5 and 10 mg as tablets and orally disintegrating tablets (Maxalt-MLT). Maxalt obtained approval ...
*  5-Carboxamidotryptamine
Glennon RA, Dukat M, Westkaemper RB (2000-01-01). "Serotonin Receptor Subtypes and Ligands". American College of ... high-affinity full agonist at the 5-HT1A, 5-HT1B, 5-HT1D, 5-HT5A, and 5-HT7 receptors, as well as at the 5-HT2, 5-HT3, 5-HT6 ... a selective agonist of 5-HT1 receptors". Archives Internationales de Pharmacodynamie et de Thérapie. 277 (2): 235-52. PMID ... is a tryptamine derivative closely related to the neurotransmitter serotonin. 5-CT acts as a non-selective, ...
*  Serotonin receptor antagonist
... and many other organs and has been used in hypertension and psychosis Serotonin receptor agonist Lindley, C.; Blower, P. (2000 ... A serotonin antagonist, or serotonin receptor antagonist, is a drug used to inhibit the action at serotonin (5-HT) receptors. ... "Oral serotonin type 3-receptor antagonists for prevention of chemotherapy-induced emesis". American Journal of Health-System ... dopamine receptors D1 and D2, histamine receptor H1, and A1 adrenoreceptors. Ketanserin Antihypertensive. Blocks 5-HT2A, 5-HT2C ...
*  5-HT2A receptor
Schmid CL, Raehal KM, Bohn LM (January 2008). "Agonist-directed signaling of the serotonin 2A receptor depends on beta-arrestin ... Serotonin receptors were split into two classes by Gaddum and Picarelli when it was discovered that some of the serotonin- ... Design and Synthesis of Selective Serotonin Receptor Agonists for Positron Emission Tomography Imaging of the Brain. University ... Feng J, Cai X, Zhao J, Yan Z (September 2001). "Serotonin receptors modulate GABA(A) receptor channels through activation of ...
*  BRL-54443
McKune CM, Watts SW (April 2001). "Characterization of the serotonin receptor mediating contraction in the mouse thoracic aorta ... BRL-54443 is a drug which acts as a selective agonist for the 5-HT1E and 5-HT1F serotonin receptor subtypes. ... Janssen P, Tack J, Sifrim D, Meulemans AL, Lefebvre RA (May 2004). "Influence of 5-HT1 receptor agonists on feline stomach ...
*  Triptan
Goadsby, P. J. (1998). "Serotonin 5HT1B/1D receptor agonists in migraine - Comparative pharmacology and its therapeutic ... doi:10.1111/j.1526-4610.2010.01691.x. Gillman (2010). "Triptans, serotonin agonists, and serotonin syndrome (serotonin toxicity ... The drugs of this class act as agonists for serotonin 5-HT1B and 5-HT1D receptors at blood vessels and nerve endings in the ... Their action is attributed to their agonist effects on serotonin 5‑HT1B and 5‑HT1D receptors in blood vessels (causing their ...
*  List of investigational anxiolytics
... mGluR2 and mGluR3 agonist [13] Tianeptine oxalate (TNX-601) - atypical μ-opioid receptor agonist [14] Verucerfont (GSK-561679, ... and α1-adrenergic receptor antagonist [12] Midomafetamine (MDMA; "ecstasy") - serotonin-norepinephrine-dopamine releasing agent ... Agomelatine (AGO-178; Valdoxan) - melatonin MT1 and MT2 receptor agonist, 5-HT2C receptor antagonist[1] Riluzole sublingual ( ... D2 and D3 receptor partial agonist and 5-HT2A, 5-HT2B, 5-HT7, α1-adrenergic, α2-adrenergic, and H1 receptor antagonist [10] ...
*  Methysergide
Serotonin was found to be among the candidate agents to be included. In the same period, serotonin was isolated (1948) and, ... It is known to have partial agonist effects on some of the other 5-HT receptors as well. Methysergide is metabolised into ... receptors. Its therapeutic effect in migraine prophylaxis has been associated with its antagonism at the 5-HT2B receptor. It is ... Based on the possible involvement of serotonin in migraine attacks, it was introduced in 1959 by Sicuteri as a preventive drug ...
*  5-HT1A receptor
The serotonin 1A receptor is encoded by the HTR1A gene. The 5-HT1A receptor is the most widespread of all the 5-HT receptors. ... Some of the atypical antipsychotics like lurasidone and aripiprazole are also partial agonists at the 5-HT1A receptor and are ... The serotonin 1A receptor (or 5-HT1A receptor) is a subtype of serotonin receptor (5-HT receptor) that binds the ... Parks CL, Shenk T (1996). "The serotonin 1a receptor gene contains a TATA-less promoter that responds to MAZ and Sp1". J. Biol ...
*  Zolmitriptan
... is a selective serotonin receptor agonist of the 1B and 1D subtypes. It is a triptan, used in the acute treatment ... is a histamine H2-receptor antagonist that inhibits the production of acid in the stomach. ""2008 Top 200 generic drugs by ... Zolmitriptan is available as a swallowable tablet, an oral disintegrating tablet, and a nasal spray, in doses of 2.5 and 5 mg. ... 5): 433-439. doi:10.1046/j.1365-2125.1998.00809.x. MacGregor, E.A. (1998). "Zolmitriptan clinical studies". Drugs Today. 34 (12 ...