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Chiral aspects of drug action at ion channels: A commentary on the stereoselectivity of drug actions at voltage‐gated ion channels with particular reference to verapamil actions at the Ca 2+ channel
Author(s) -
Kwon YongWha,
Triggle David J.
Publication year - 1991
Publication title -
chirality
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.43
H-Index - 77
eISSN - 1520-636X
pISSN - 0899-0042
DOI - 10.1002/chir.530030504
Subject(s) - chemistry , stereoselectivity , verapamil , ion channel , enantiomer , stereochemistry , drug action , drug , voltage gated ion channel , biophysics , receptor , calcium , pharmacology , biochemistry , organic chemistry , medicine , biology , catalysis
Ion channels may be considered as pharmacological receptors possessing specific drug binding sites with defined structure‐activity relationships. Accordingly drug binding to ion channels is stereoselective. Interpretation of this stereoselectivity may be complex because of the existence of differences in affinity and access to different channel states. Such state‐dependent interactions may give rise to quantitative and qualitative differences in stereoselectivity. The implications of such differences are reviewed for drug action at Na + , K + and Ca 2+ channels. Detailed attention is paid to the actions of verapamil enantiomers in the cardiovascular system where activities differ in vascular and cardiac tissues because of state‐dependent interactions and stereoselective first‐oass metabolism.