Airway smooth muscle selectivity of the muscarinic antagonist DAC 5945 in vivo

We investigated the M3/M2 antagonist selectivity of [N-iminomethyl-N'-[(2-hydroxy-2-phenyl-2-cyclohexyl)-ethyl] piperazine HCI (DAC 5945) in vivo. ED50 values for reversal of methacholine-induced bronchoconstriction and bradycardia by muscarinic antagonists were determined in anesthetized and v...

Full description

Saved in:
Bibliographic Details
Published inEuropean journal of pharmacology Vol. 196; no. 3; p. 323
Main Authors Howell, R E, Laemont, K D, Noronha-Blob, L
Format Journal Article
LanguageEnglish
Published Netherlands 24.04.1991
Subjects
Animals
Bronchoconstriction - drug effects
Bronchoconstriction - physiology
Female
Guinea Pigs
Methacholine Chloride - pharmacology
Muscarinic Antagonists
Muscle, Smooth - drug effects
Muscle, Smooth - physiology
Piperazines - pharmacology
Propranolol - pharmacology
Trachea - drug effects
Trachea - physiology
Online AccessGet more information

Cover

More Information
Summary:We investigated the M3/M2 antagonist selectivity of [N-iminomethyl-N'-[(2-hydroxy-2-phenyl-2-cyclohexyl)-ethyl] piperazine HCI (DAC 5945) in vivo. ED50 values for reversal of methacholine-induced bronchoconstriction and bradycardia by muscarinic antagonists were determined in anesthetized and ventilated guinea pigs. Atropine, ipratopium, pirenzepine and diphenyl-acetoxy-4-methylpiperidine methiodide (4-DAMP) were non-selective, whereas methoctramine was cardioselective. In contrast, DAC 5945 was a more potent muscarinic antagonist in the airways than in the heart, demonstrating M3/M2 selectivity in vivo.
ISSN:0014-2999
DOI:10.1016/0014-2999(91)90447-X