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 Pharmacoljournal_title
European journal of pharmacologyauthors
Lambrecht G,Feifel R,Moser U,Aasen AJ,Waelbroeck M,Christophe J,Mutschler Edoi
10.1016/0014-2999(88)90417-7subject
Has Abstractpub_date
1988-10-11 00:00:00pages
167-70issue
1-2eissn
0014-2999issn
1879-0712pii
0014-2999(88)90417-7journal_volume
155pub_type
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