2. Academic Validation
  3. Identification and characterization of m4 selective muscarinic antagonists

Identification and characterization of m4 selective muscarinic antagonists

  • Bioorg Med Chem Lett. 1998 Aug 4;8(15):1991-6. doi: 10.1016/s0960-894x(98)00351-5.
C E Augelli-Szafran 1,  J C Jaen,  D W Moreland,  C B Nelson,  J R Penvose-Yi,  R D Schwarz
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, Parke-Davis Pharmaceutical Research, Ann Arbor, Michigan 48105, USA.
PMID: 9873472 DOI: 10.1016/s0960-894x(98)00351-5
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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