Cycloalkyl [b][1, 4] benzodiazepinoindoles are agonists at the human 5-HT 2C receptor

…, J Dunlop, S Rosenzweig-Lipson, B Harrison

文献索引：Sabb, Annmarie L.; Vogel, Robert L.; Welmaker, Gregory S.; Sabalski, Joan E.; Coupet, Joseph; Dunlop, John; Rosenzweig-Lipson, Sharon; Harrison, Boyd Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 10 p. 2603 - 2607

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被引用次数: 36

摘要

Evaluation of selected compounds from our Corporate Compound Library in a human 5- HT2C receptor binding assay led to the discovery of WAY-629, a cyclohexyl [b][1, 4] benzodiazepinoindole (Ki 56nM, Emax 90%), which is selective for the 5-HT2C 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 ...