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Bioorg Med Chem Lett. 2001 Aug 20;11(16):2133-6.

5-HT(3)R binding of lerisetron: an interdisciplinary approach to drug-Receptor interactions.

Author information

1
Department of Basic Pharmaceutical Sciences, College of Pharmacy, The University of Louisiana at Monroe, 700 University Avenue, Monroe, LA 71209, USA.

Abstract

The design, synthesis, and use of lerisetron-based molecular probes to investigate the 5-HT(3)R binding site are described. A SAR study, which involved distance and electronic parameter modifications of lerisetron's N-benzyl group, resulted in the discovery of a partial agonist.

PMID:
11514154
DOI:
10.1016/s0960-894x(01)00417-6
[Indexed for MEDLINE]

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