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CaM‐Inhibitory Actions of Ca Antagonists
Author(s) -
Mannhold Raimund,
Kramer Andreas,
Schäfer Wolfgang,
Schramm Petra
Publication year - 1987
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.19873200804
Subject(s) - potency , chemistry , diltiazem , pharmacology , lipophilicity , flunarizine , verapamil , nifedipine , inhibitory postsynaptic potential , dihydropyridine , calcium , stereochemistry , medicine , biochemistry , in vitro , organic chemistry
We have tested the calmodulin (CaM) inhibitory potency of some Ca antagonists and of calmidazolium and aprindine in the phosphodiesterase (PDE) assay. Also we have compared the dependence on lipophilicity of the CaM inhibitory potency and of functional properties of Ca antagonists. The CaM inhibitory potency of Ca antagonists, with the exception of nifedipine, correlates with their lipophilicity (r = 0.96). Negative inotropic potency of a subgroup of Ca antagonists (prenylamine, fendiline, bencyclane, perhexiline) interrelates with their CaM inhibitory potency and exhibits a similar dependence on lipophilicity. CaM inhibition seems to contribute to vasodilator potency only for the most liophilic Ca antagonists. On the basis of their CaM‐inhibitory properties, three groups of Ca antagonists are distinguished: a) verapamil and diltiazem, b) dihydropyridine derivatives and c) lipophilic Ca antagonists (perhexiline, flunarizine, prenylamine, fendiline).