Novel agonists of 5HT2C receptors. Synthesis and biological evaluation of substituted 2-(indol-1-yl)-1-methylethylamines and 2-(indeno[1,2-b]pyrrol-1-yl)-1-methylethylamines. Improved therapeutics for obsessive compulsive disorder.

Abstract	The syntheses of a series of substituted 2-(indol-1-yl)-1-methylethylamines and 2-(indeno[1,2- b]pyrrol-1-yl)-1-methylethylamines are reported. The binding affinities of the compounds at 5HT2C and 5HT2A receptors (79% homology in the transmembrane domain) were determined. The ligands displayed selectivity for 5HT2C receptors relative to 5HT2A receptors. Compounds were functionally characterized both in vitro and in vivo as 5HT2C receptor agonists. 5f, 5l, 5n, 5o, 5q, 14c, 14f, 14k, and 14m exhibited anticompulsive activity in an animal model of obsessive compulsive disorder.
Authors	M Bös, F Jenck, J R Martin, J L Moreau, A J Sleight, J Wichmann, U Widmer
Journal	Journal of medicinal chemistry (J Med Chem) Vol. 40 Issue 17 Pg. 2762-9 (Aug 15 1997) ISSN: 0022-2623 [Print] United States
PMID	9276022 (Publication Type: Journal Article)
Chemical References	Ethylamines Ligands Receptor, Serotonin, 5-HT2A Receptor, Serotonin, 5-HT2C Receptors, Serotonin Serotonin Receptor Agonists Serotonin
Topics	3T3 Cells Animals Ethylamines (chemical synthesis, chemistry, therapeutic use) Female Humans Ligands Male Mice Obsessive-Compulsive Disorder (drug therapy) Penile Erection (drug effects) Rats Receptor, Serotonin, 5-HT2A Receptor, Serotonin, 5-HT2C Receptors, Serotonin (metabolism) Serotonin (metabolism) Serotonin Receptor Agonists (chemical synthesis, chemistry, therapeutic use) Thirst (drug effects)

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