Identification and Characterization of M4 Selective Muscarinic Antagonists

Overview

Journal Bioorg Med Chem Lett

Specialty Biochemistry

Date 1999 Jan 5

PMID 9873472

Citations 8

Authors

C E Augelli-Szafran

J C Jaen

D W Moreland

C B Nelson

R D Schwarz

Affiliations

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Abstract

Our interest in the area of m4 muscarinic antagonists had led us to study a series of benzoxazine isoquinolines. One of the most potent and selective compounds of this series is example 1 with an IC50 value of 90.7 nM at m4 receptors, and 72-fold (m1), 38-fold (m2), 10-fold (m3), and 82-fold (m5) more selective compared to the other receptors. The synthesis and receptor binding affinity of analogs of 1 are reported.

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