Stereoselectivity of the enantiomers of trihexyphenidyl and its methiodide at muscarinic receptor subtypes.

Abstract:

:High stereoselectivity was observed for the enantiomers of trihexyphenidyl and trihexyphenidyl methiodide at muscarinic M1-receptors in field-stimulated rabbit vas deferens and at M2 alpha- and M2 beta-receptors in guinea-pig atrium and ileum, respectively. Considerably higher affinities (up to 1700-fold) were found for the (R)-(-)-enantiomers. The stereochemical demands made by the muscarinic receptor subtypes were most stringent at the M1-receptors. The (R)-(-)-enantiomers were found to be potent M1-selective antagonists (pA2 = 10.1/10.6). They showed a 91- and 45-fold selectivity for M1- over M2 alpha-receptors, respectively.

journal_name

Eur J Pharmacol

authors

Lambrecht G,Feifel R,Moser U,Aasen AJ,Waelbroeck M,Christophe J,Mutschler E

doi

10.1016/0014-2999(88)90417-7

subject

Has Abstract

pub_date

1988-10-11 00:00:00

pages

167-70

issue

1-2

eissn

0014-2999

issn

1879-0712

pii

0014-2999(88)90417-7

journal_volume

155

pub_type

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