Literature DB >> 3801761

Stereospecific inhibition of 5-HT-induced increase of intracellular free calcium by (+)- and (-)-desmethoxyverapamil in human platelets.

C Bruns, D Marmé, H Osswald.   

Abstract

The concentration of intracellular free calcium [Ca2+]i in human platelets was measured by the quin-2 method. 5-Hydroxytryptamine (5-HT) at 10(-5) M induced a rapid transient increase of [Ca2+]i which was antagonized by 10(-7) M ketanserin or cyproheptadine. The verapamil derivative, desmethoxyverapamil (D888), showed stereospecific inhibition of the 5-HT-induced [Ca2+]i increase. The IC50 for (-)-D888 was approx. 2 X 10(-8) M; (+)-D888 was almost 50 times less potent.

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Year:  1986        PMID： 3801761      PMCID： PMC1916576          DOI： 10.1111/j.1476-5381.1986.tb10188.x

Source DB:  PubMed          Journal:  Br J Pharmacol        ISSN： 0007-1188            Impact factor:   8.739


  7 in total

1.  Inhibition of [3H]spiperone binding to 5-HT2 receptors of rat cerebral cortex by the calcium antagonists verapamil and D600.

Authors:  J E Taylor; F V Defeudis
Journal:  Eur J Pharmacol       Date:  1984-10-30       Impact factor: 4.432

2.  Calcium homeostasis in intact lymphocytes: cytoplasmic free calcium monitored with a new, intracellularly trapped fluorescent indicator.

Authors:  R Y Tsien; T Pozzan; T J Rink
Journal:  J Cell Biol       Date:  1982-08       Impact factor: 10.539

3.  (-)-[3H]Desmethoxyverapamil, a novel Ca2+ channel probe. Binding characteristics and target size analysis of its receptor in skeletal muscle.

Authors:  A Goll; D R Ferry; J Striessnig; M Schober; H Glossmann
Journal:  FEBS Lett       Date:  1984-10-29       Impact factor: 4.124

4.  Verapamil, an antagonist at 5-hydroxytryptamine receptors of human blood platelets.

Authors:  H Affolter; W P Burkard; A Pletscher
Journal:  Eur J Pharmacol       Date:  1985-01-22       Impact factor: 4.432

5.  Rapid intracellular release of calcium in human platelets by stimulation of 5-HT2-receptors.

Authors:  P Erne; A Pletscher
Journal:  Br J Pharmacol       Date:  1985-02       Impact factor: 8.739

6.  Inhibition of human platelet functions by verapamil.

Authors:  Y Ikeda; M Kikuchi; K Toyama; K Watanabe; Y Ando
Journal:  Thromb Haemost       Date:  1981-04-30       Impact factor: 5.249

7.  Effect of the calcium-entry blocking agent nifedipine on activation of human platelets and comparison with verapamil.

Authors:  P Han; C Boatwright; N G Ardlie
Journal:  Thromb Haemost       Date:  1983-08-30       Impact factor: 5.249
  7 in total

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