2. Academic Validation
  3. Cycloalkyl[b][1,4]benzodiazepinoindoles are agonists at the human 5-HT2C receptor

Cycloalkyl[b][1,4]benzodiazepinoindoles are agonists at the human 5-HT2C receptor

  • Bioorg Med Chem Lett. 2004 May 17;14(10):2603-7. doi: 10.1016/j.bmcl.2004.02.100.
Annmarie L Sabb 1,  Robert L Vogel,  Gregory S Welmaker,  Joan E Sabalski,  Joseph Coupet,  John Dunlop,  Sharon Rosenzweig-Lipson,  Boyd Harrison
Affiliations

Affiliation

  • 1 Chemical and Screening Sciences, Wyeth Research, CN 8000, Princeton, NJ 08543-8000, USA. [email protected]
PMID: 15109661 DOI: 10.1016/j.bmcl.2004.02.100
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 cyclohexyl[b][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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