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Design and synthesis of piperidinyl piperidine analogues as potent and selective M2 muscarinic receptor antagonists.

Authors
  • Wang, Y
  • Chackalamannil, S
  • Hu, Z
  • Clader, J W
  • Greenlee, W
  • Billard, W
  • Binch, H
  • Crosby, G
  • Ruperto, V
  • Duffy, R A
  • McQuade, R
  • Lachowicz, J E
Type
Published Article
Journal
Bioorganic & Medicinal Chemistry Letters
Publisher
Elsevier
Publication Date
Oct 16, 2000
Volume
10
Issue
20
Pages
2247–2250
Identifiers
PMID: 11055330
Source
Medline
License
Unknown

Abstract

Identification of a number of highly potent M2 receptor antagonists with >100-fold selectivity against the M1 and M3 receptor subtypes is described. In the rat microdialysis assay, this series of compounds showed pronounced enhancement of brain acetylcholine release after oral administration.

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