Cycloalkyl[b][1,4]benzodiazepinoindoles are agonists at the human 5-HT2C receptor |
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Authors: | Sabb Annmarie L Vogel Robert L Welmaker Gregory S Sabalski Joan E Coupet Joseph Dunlop John Rosenzweig-Lipson Sharon Harrison Boyd |
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Institution: | Chemical and Screening Sciences, Wyeth Research, CN 8000, Princeton, NJ 08543-8000, USA. sabba@wyeth.com |
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Abstract: | Evaluation of selected compounds from our Corporate Compound Library in a human 5-HT(2C) receptor binding assay led to the discovery of WAY-629, a cyclohexylb]1,4]benzodiazepinoindole (K(i) 56 nM, E(max) 90%), which is selective for the 5-HT(2C) receptor versus other serotonin receptor subtypes, and dopamine, histamine, adrenergic, and muscarinic receptors. In addition, WAY-629 was active in vivo in a rat model of feeding behavior. An SAR study based on WAY-629 led to compound 11 (K(i) 13 nM, E(max) 102%). |
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