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Specific inhibition of Ca‐activated K channels in red cells by selected dihydropyridine derivatives
Author(s) -
Ellory J.C.,
Culliford S.J.,
Smith P.A.,
Wolowyk M.W.,
Knaus E.E.
Publication year - 1994
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.1476-5381.1994.tb14823.x
Subject(s) - nitrendipine , dihydropyridine , chemistry , potassium channel , pharmacology , biophysics , biochemistry , stereochemistry , calcium , biology , organic chemistry
1 Thirty two dihydropyridine derivatives were screened as potential inhibitors of the Ca‐activated K‐channel in human red cells. 2 Three derivatives (26, 29, 32 see Tables 1 and 2) with high activity were then characterized in detail, and also tested against the smooth muscle Ca‐channel and shown to have varying potencies. 3 One of the more potent derivatives (32) and nitrendipine were also tested on the Ca‐activated K‐channel, Maxi‐K channel, from mouse pancreatic beta‐cells. 4 We conclude from our results that it may be possible to develop selective Gardos‐channel inhibitors based on these molecules, which may be of benefit in the treatment of sickle cell disease.