Literature DB >> 3393229

Chiral muscarinic agonists possessing a 1,3-oxathiolane nucleus: enantio- and tissue-selectivity on isolated preparations of guinea-pig ileum and atria and of rat urinary bladder.

P Angeli1, L Brasili, M Giannella, F Gualtieri, M T Picchio, E Teodori.   

Abstract

Racemate and corresponding enantiomers of muscarinic agonists carrying a 1,3-oxathiolane nucleus were studied on isolated preparations of guinea-pig ileum and atria and of rat urinary bladder. The efficacy of these agonists were determined according to the method of Furchgott and Bursztyn (1967) and enantio-selectivity and tissue-selectivity were investigated. The enantio-selectivities of the most potent compounds studied (expressed as the ratio of potencies or affinities of the enantiomers) vary significantly from tissue to tissue, supporting the view that M2 receptors are not homogeneous. In particular, the data all indicate that the ileal receptors are different to the atrial and bladder ones.

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Year:  1988        PMID： 3393229     DOI： 10.1007/bf00168833

Source DB:  PubMed          Journal:  Naunyn Schmiedebergs Arch Pharmacol        ISSN： 0028-1298            Impact factor:   3.000


  13 in total

Review 1.  Muscarinic receptor subtypes: a critique of the current classification and a proposal for a working nomenclature.

Authors:  R M Eglen; R L Whiting
Journal:  J Auton Pharmacol       Date:  1986-12

2.  The cardio-selectivity of himbacine: a muscarine receptor antagonist.

Authors:  S Anwar-ul; H Gilani; L B Cobbin
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1986-01       Impact factor: 3.000

3.  Alpha-adrenoreceptor reagents. 4. Resolution of some potent selective prejunctional alpha 2-adrenoreceptor antagonists.

Authors:  A P Welbourn; C B Chapleo; A C Lane; P L Myers; A G Roach; C F Smith; M R Stillings; I F Tulloch
Journal:  J Med Chem       Date:  1986-10       Impact factor: 7.446

4.  Different steric characteristics of beta 1- and beta 2-adrenoceptors.

Authors:  T H Morris; A J Kaumann
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1984-09       Impact factor: 3.000

5.  Muscarinic receptor subtypes: M1 and M2 biochemical and functional characterization.

Authors:  R Hammer; A Giachetti
Journal:  Life Sci       Date:  1982-12-27       Impact factor: 5.037

6.  Resolution, absolute configuration, and cholinergic enantioselectivity of (+)- and (-)-cis-2-methyl-5-[(dimethylamino)methyl]-1,3-oxathiolane methiodide.

Authors:  E Teodori; F Gualtieri; P Angeli; L Brasili; M Giannella; M Pigini
Journal:  J Med Chem       Date:  1986-09       Impact factor: 7.446

7.  Resolution, absolute configuration, and cholinergic enantioselectivity of (-)- and (+)-c-2-methyl-r-5-[(dimethylamino)methyl]-1,3-oxathiolane t-3-oxide methiodide and related sulfones.

Authors:  E Teodori; F Gualtieri; P Angeli; L Brasili; M Giannella
Journal:  J Med Chem       Date:  1987-10       Impact factor: 7.446

8.  Action of agonists and antagonists at muscarinic receptors present on ileum and atria in vitro.

Authors:  R U Clague; R M Eglen; A C Strachan; R L Whiting
Journal:  Br J Pharmacol       Date:  1985-09       Impact factor: 8.739

9.  Multiple agonist binding sites of muscarinic acetylcholine receptors and their relation to the negative inotropic action of agonists in guinea-pig heart.

Authors:  A Mizushima; S Uchida; K Matsumoto; T Osugi; T Kagiya; X M Zhou; H Higuchi; H Yoshida
Journal:  Eur J Pharmacol       Date:  1985-12-17       Impact factor: 4.432

10.  Determination of dissociation constants and relative efficacies of some potent muscarinic agonists at postjunctional muscarinic receptors.

Authors:  E Grana; A Lucchelli; F Zonta; C Boselli
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1987-01       Impact factor: 3.000
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  2 in total

1.  Determination of muscarinic agonist potencies at M1 and M2 muscarinic receptors in a modified pithed rat preparation.

Authors:  P Angeli; L Brasili; F Cantalamessa; G Marucci; J Wess
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1990-12       Impact factor: 3.000

2.  The action of (+/-)L-660,863 [(+/-)3-(3-amino-1,2,4-oxadiazole-5-yl)-quinuclidine] at muscarinic receptor subtypes in vitro.

Authors:  R M Eglen; G C Harris; A P Ford; E H Wong; J R Pfister; R L Whiting
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1992-04       Impact factor: 3.000
  2 in total

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