Literature DB >> 3754814

The enantiomers of the dihydropyridine derivative H 160/51 show opposite effects of stimulation and inhibition.

P Gjörstrup, H Hårding, R Isaksson, C Westerlund.   

Abstract

H 160/51 is a calcium agonistic 1,4-dihydropyridine. Its optical isomers were now found to have opposing actions in the cat papillary muscle and rat portal vein. The inhibitory (+)-enantiomer had potencies of the same order as those of the stimulatory (-)-enantiomer. However the racemate and the (-)-enantiomer had approximately the same potencies and intrinsic activities. A model is presented to account for the fact that the effects of the inhibitory (+)-enantiomer can be concealed in the effects of the racemate of H 160/51.

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Year:  1986        PMID: 3754814     DOI: 10.1016/0014-2999(86)90417-6

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


  6 in total

1.  Molecular level model for the agonist/antagonist selectivity of the 1,4-dihydropyridine calcium channel receptor.

Authors:  D A Langs; Y W Kwon; P D Strong; D J Triggle
Journal:  J Comput Aided Mol Des       Date:  1991-04       Impact factor: 3.686

2.  The dihydropyridine derivative 202-791: interpretation of the effects of the racemate considering inverse agonistic enantiomers.

Authors:  M Damarowsky; H Lüllmann; U Ravens
Journal:  Br J Pharmacol       Date:  1988-12       Impact factor: 8.739

3.  Ca-agonists: a new class of inotropic drugs.

Authors:  M Bechem; R Gross; S Hebisch; M Schramm
Journal:  Basic Res Cardiol       Date:  1989       Impact factor: 17.165

4.  Opposite cardiac actions of the enantiomers of Bay K 8644 at different membrane potentials in guinea-pig papillary muscles.

Authors:  U Ravens; H P Schöpper
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1990-03       Impact factor: 3.000

5.  A molecular graphics study on structure-action relationships of calcium-antagonistic and agonistic 1,4-dihydropyridines.

Authors:  H D Höltje; S Marrer
Journal:  J Comput Aided Mol Des       Date:  1987-04       Impact factor: 3.686

6.  The effects of the cardiotonic dihydropyridine derivatives Bay k 8644 and H160/51 on post-rest adaptation of guinea-pig papillary muscles.

Authors:  T Beyer; N Gansohr; P Gjörstrup; U Ravens
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1986-12       Impact factor: 3.000

  6 in total

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