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Stereospecific inhibition of 5‐HT‐induced increase of intracellular free calcium by (+)‐ and (−)‐desmethoxyverapamil in human platelets
Author(s) -
Bruns Christian,
Marmé Dieter,
Osswald Hartmut
Publication year - 1986
Publication title -
british journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1111/j.1476-5381.1986.tb10188.x
Subject(s) - verapamil , platelet , calcium , chemistry , intracellular , ketanserin , cyproheptadine , calcium in biology , endocrinology , 5 ht receptor , medicine , serotonin , pharmacology , biophysics , biochemistry , receptor , biology , organic chemistry
The concentration of intracellular free calcium [Ca 2+ ] 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 [Ca 2+ ] i which was antagonized by 10 −7 M ketanserin or cyproheptadine. The verapamil derivative, desmethoxyverapamil (D 888), showed stereospecific inhibition of the 5‐HT‐induced [Ca 2+ ] i increase. The IC 50 for (−)‐D 888 was approx. 2 × 10 −8 M; (+)‐D 888 was almost 50 times less potent.