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Receptor, Serotonin, 5-HT2A

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Definition: A serotonin receptor subtype found widely distributed in peripheral tissues where it mediates the contractile responses of variety of tissues that contain SMOOTH MUSCLE. Selective 5-HT2A receptor antagonists include KETANSERIN. The 5-HT2A subtype is also located in BASAL GANGLIA and CEREBRAL CORTEX of the BRAIN where it mediates the effects of HALLUCINOGENS such as LSD.      Other names Receptors, Serotonin 2A; Receptor, 5-HT2A; 5 HT2A Receptor; 2A Receptors, Serotonin; 2A Receptor, Serotonin; Serotonin 2A Receptors; Receptor, Serotonin 2A; 5-HT2A Receptor; 5-HT(2A) Receptor; Serotonin 2A Receptor
 
SubstanceCAS Registry & nameCategoriesSourceDrugs*
2-(4-iodo-2,5-dimethoxyphenyl)-N-(2-methoxybenzyl)ethanamine  0   *Benzylamines *Phenethylamines Carbon Radioisotopes Ligands Receptor, Serotonin, 5-HT2A. J Nucl Med 2010 Nov;51(11):1763-70
1-(2,4-difluorophenethyl)-4-(4-fluorophenylsulfinyl)piperidine  0   *Piperidines *Sulfoxides Fluorine Radioisotopes Receptor, Serotonin, 5-HT2A. Nucl Med Biol 2010 Jul;37(5):605-14
1-(2,4-difluorophenethyl)-4-(4-fluorophenylsulfonyl)piperidine  0   *Piperidines *Sulfones Fluorine Radioisotopes Receptor, Serotonin, 5-HT2A. Nucl Med Biol 2010 Jul;37(5):605-14
2-(4-(4-chloro-1-methyl-1H-pyrazole-3-carbonyl)piperazin-1-yl)-1-(4-fluorophenyl)ethanone  0   *Piperazines *Pyrazoles Receptor, Serotonin, 5-HT2A. J Med Chem 2010 Aug 12;53(15):5696-706
2-(4-(4-bromo-1-methyl-1H-pyrazole-3-carbonyl)piperazin-1-yl)-1-(4-fluorophenyl)ethanone  0   *Piperazines *Pyrazoles Receptor, Serotonin, 5-HT2A. J Med Chem 2010 Aug 12;53(15):5696-706
5-(((4-benzo(a)isothiazol-3-yl)piperazin-1-yl)methyl)-6-chloroindolin-2-one  0   *Indoles *Thiazoles Receptor, Serotonin, 5-HT2A/antagonists & inhibitors. Pharmacol Biochem Behav 2010 Jan;94(3):363-73
APD791  0   *Benzamides *Morpholines *Pyrazoles Receptor, Serotonin, 5-HT2A/antagonists & inhibitors. J Pharmacol Exp Ther. 2009 Oct;331(1):96-103
AR 246686  0   *Phenylurea Compounds Receptor, Serotonin, 5-HT2A/antagonists & inhibitors. Eur J Pharmacol 2008 May 31;586(1-3):234-43
N-(2-(4-(1,2-benzisothiazol-3-yl)-1-piperazinylmethyl)-1-cyclohexylmethyl)-2,3-bicyclo(2.2.1)heptanedicarboximide  0   *Thiazoles *Isoindoles Receptors, Dopamine D2/antagonists & inhibitors Receptor, Serotonin, 5-HT2A/antagonists & inhibitors. Eur J Pharmacol 2007 Oct 31;572(2-3):160-70LATUDA
YKP 1358  0   *Alkaloids Receptors, Dopamine D2/antagonists & inhibitors Receptor, Serotonin, 5-HT2A/antagonists & inhibitors. Clin Pharmacol Ther 2007 Feb;81(2):252-8
(4-bromo-3,6-dimethoxybenzocyclobuten-1-yl)methylamine  0   *Bicyclo Compounds *Methylamines Receptor, Serotonin, 5-HT2A. J Med Chem 2006 Sep 21;49(19):5794-803
C-(4,5,6-trimethoxyindan-1-yl)methanamine  0   *Indans *Methylamines Receptor, Serotonin, 5-HT2A/agonists. J Med Chem 2006 Jul 13;49(14):4269-74
N-(4-fluorophenylmethyl)-N-(1-methylpiperidin-4-yl)-N'-(4-(2-methylpropyloxy)phenylmethyl)carbamide  0   *Piperidines Urea/*analogs & derivatives Receptor, Serotonin, 5-HT2A/agonists. J Pharmacol Exp Ther 2006 May;317(2):910-8
2-(4-methoxyphenyl)-N-(4-methylbenzyl)-N-(1-methylpiperidin-4-yl)acetamide  0   *Benzamides *Piperidines Receptor, Serotonin, 5-HT2A/antagonists & inhibitors. J Pharmacol Exp Ther 2004 Sep;310(3):943-51
9-(4-methylpiperazin-1-yl)pyrrolo(2,1-b)benzothiazepine  0   *Pyrroles *Thiazepines Receptors, Dopamine D2/antagonists & inhibitors Receptor, Serotonin, 5-HT2A/antagonists & inhibitors. J Med Chem 2004 Jan 1;47(1):143-57

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Sources: NLM Medical Subject Headings, NIH UMLS, Drugs@FDA, FDA AERS original data copyright United States Government. No endorsement implied. Last modified 6/6/2012
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