Binding of beta-carbolines at 5-HT(2) serotonin receptors

  • Bioorg Med Chem Lett. 2003 Dec 15;13(24):4421-5. doi: 10.1016/j.bmcl.2003.09.027.
Brian Grella  1 ,  Milt Teitler ,  Carol Smith ,  Katharine Herrick-Davis ,  R A Glennon
Affiliations
  • 1. Department of Medicinal Chemistry, School of Pharmacy, Virginia Commonwealth University, Richmond, VA 23298-0540, USA.
PMID: 14643338 DOI: 10.1016/j.bmcl.2003.09.027
Abstract

A series of ring-substituted (i.e., methoxy and bromo) 3,4-dihydro- and 1,2,3,4-tetrahydro-beta-carbolines was examined at 5-HT(2A) and 5-HT(2C) serotonin receptors. Whereas most of the methoxy-substituted derivatives typically displayed affinities similar to their unsubstituted parents, certain (particularly 8-substituted) bromo derivatives displayed enhanced affinity. A binding profile was obtained for selected beta-carbolines.

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