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Investigating the interaction of McN-A-343 with the M muscarinic receptor using its nitrogen mustard derivative and ACh mustard.

Authors
  • Figueroa, K W
  • Suga, H
  • Ehlert, F J
Type
Published Article
Journal
British Journal of Pharmacology
Publisher
Wiley (Blackwell Publishing)
Publication Date
Jul 01, 2010
Volume
160
Issue
6
Pages
1534–1549
Identifiers
DOI: 10.1111/j.1476-5381.2010.00810.x
PMID: 20590642
Source
Medline
License
Unknown

Abstract

Our results suggest that McN-A-343 and its nitrogen mustard derivative interact competitively with ACh and N-methylscopolamine at the orthosteric site on the M(1) muscarinic receptor. Measuring how drugs modulate the kinetics of receptor alkylation by an irreversible ligand is a powerful approach for distinguishing between negative allosteric modulators and competitive inhibitors.

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