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

H S Parihar; A Suryanarayanan; C Ma; P Joshi; P Venkataraman; M K Schulte; K S Kirschbaum

doi:10.1016/s0960-894x(01)00417-6

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

Bioorg Med Chem Lett. 2001 Aug 20;11(16):2133-6. doi: 10.1016/s0960-894x(01)00417-6.

Authors

H S Parihar¹, A Suryanarayanan, C Ma, P Joshi, P Venkataraman, M K Schulte, K S Kirschbaum

Affiliation

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

PMID: 11514154
DOI: 10.1016/s0960-894x(01)00417-6

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.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Benzimidazoles / chemical synthesis
Benzimidazoles / chemistry
Benzimidazoles / pharmacology*
Drug Design
Piperidines / chemical synthesis
Piperidines / chemistry
Piperidines / pharmacology*
Receptors, Serotonin / drug effects
Receptors, Serotonin / metabolism*
Receptors, Serotonin, 5-HT3
Serotonin Antagonists / chemical synthesis
Serotonin Antagonists / chemistry
Serotonin Antagonists / pharmacology*
Structure-Activity Relationship

Substances

Benzimidazoles
Piperidines
Receptors, Serotonin
Receptors, Serotonin, 5-HT3
Serotonin Antagonists
lerisetron