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Importance of nitrile substitution for the Ca antagonistic action of Verapamil
Author(s) -
Mannhold Raimund,
Höltje HansDieter,
Koke Volker
Publication year - 1986
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.19863191107
Subject(s) - verapamil , nitrile , substituent , chemistry , steric effects , stereochemistry , inotrope , calcium , medicine , organic chemistry
The effects of verapamil congeners, a) obtained by exchange of the nitrile substituent and b) a structural isomer, on the contractile activity were investigated in isotonically contracting cat papillary muscle. Results indicate that the nitrile substituent is essential for the negative inotropic action of verapamil. Investigations with an ortho disubstituted structural isomer of verapamil showed an unchanged mode of action, while potency is decreased. These findings can be explained on the basis of differences in the steric and electronic properties of the molecules under consideration.