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Identification and characterization of m4 selective muscarinic antagonists
C E Augelli-Szafran1, J C Jaen, D W Moreland
1Department of Medicinal Chemistry, Parke-Davis Pharmaceutical Research, Ann Arbor, Michigan 48105, USA.
Bioorganic & Medicinal Chemistry Letters
|January 5, 1999
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.