Identification and characterization of m4 selective muscarinic antagonists

CE Augelli-Szafran, JC Jaen, DW Moreland…

Index: Augelli-Szafran, Corinne E.; Jaen, Juan C.; Moreland, David W.; Nelson, Carrie B.; Penvose-Yi, Jan R.; Schwarz, Roy D. Bioorganic and Medicinal Chemistry Letters, 1998 , vol. 8, # 15 p. 1991 - 1996

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Citation Number: 25

Abstract

Our interest in the area of m4 muscarinic antagonists has 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.