Literature DB >> 3243330

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

G Lambrecht1, R Feifel, U Moser, A J Aasen, M Waelbroeck, J Christophe, E Mutschler.   

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.

Entities:  

Mesh：

Substances：

Year:  1988        PMID： 3243330     DOI： 10.1016/0014-2999(88)90417-7

Source DB:  PubMed          Journal:  Eur J Pharmacol        ISSN： 0014-2999            Impact factor:   4.432


  8 in total

1.  Stereoselective recognition of the enantiomers of phenglutarimide and of six related compounds by four muscarinic receptor subtypes.

Authors:  M Waelbroeck; S Lazareno; O Pfaff; T Friebe; M Tastenoy; E Mutschler; G Lambrecht
Journal:  Br J Pharmacol       Date:  1996-12       Impact factor: 8.739

2.  A muscarinic receptor different from the M1, M2, M3 and M4 subtypes mediates the contraction of the rabbit iris sphincter.

Authors:  I T Bognar; U Altes; C Beinhauer; I Kessler; H Fuder
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1992-06       Impact factor: 3.000

3.  Different muscarine receptors mediate the prejunctional inhibition of [3H]-noradrenaline release in rat or guinea-pig iris and the contraction of the rabbit iris sphincter muscle.

Authors:  H Fuder; J Schöpf; J Unckell; M T Wesner; C Melchiorre; R Tacke; E Mutschler; G Lambrecht
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1989-12       Impact factor: 3.000

4.  Thermodynamics of antagonist binding to rat muscarinic M2 receptors: antimuscarinics of the pridinol, sila-pridinol, diphenidol and sila-diphenidol type.

Authors:  M Waelbroeck; J Camus; M Tastenoy; G Lambrecht; E Mutschler; M Kropfgans; J Sperlich; F Wiesenberger; R Tacke; J Christophe
Journal:  Br J Pharmacol       Date:  1993-06       Impact factor: 8.739

5.  Prejunctional muscarine receptors in the rabbit ear artery differ from M1, M2 and M3 muscarine receptors.

Authors:  S A Darroch; L K Choo; F Mitchelson
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1992-03       Impact factor: 3.000

6.  Stereoselective inhibition of muscarinic receptor subtypes by the enantiomers of hexahydro-difenidol and acetylenic analogues.

Authors:  R Feifel; M Wagner-Röder; C Strohmann; R Tacke; M Waelbroeck; J Christophe; E Mutschler; G Lambrecht
Journal:  Br J Pharmacol       Date:  1990-03       Impact factor: 8.739

7.  Antagonism by (R)- and (S)-trihexyphenidyl of muscarinic stimulation of adenylyl cyclase in rat olfactory bulb and inhibition in striatum and heart.

Authors:  P Onali; A J Aasen; M C Olianas
Journal:  Br J Pharmacol       Date:  1994-11       Impact factor: 8.739

8.  Characterization of the prejunctional muscarinic receptors mediating inhibition of evoked release of endogenous noradrenaline in rabbit isolated vas deferens.

Authors:  U Grimm; H Fuder; U Moser; H G Bümert; E Mutschler; G Lambrecht
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1994-01       Impact factor: 3.000
  8 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.