Calphostin C, a widely used protein kinase C inhibitor, directly and potently blocks L-type Ca channels.
Calphostin C is a widely used inhibitor of protein kinase C; in the past 4 years at least 350 articles have been published using this drug as a selective inhibitor of protein kinase C. In this paper, we show that calphostin C also potently inhibits cardiac L-type Ca channels by a mechanism that does not involve changes in adenosine 3',5'-cyclic monophosphate levels or dephosphorylation. The inhibition requires illumination by visible light during exposure to calphostin C. The Ca current (ICa) that remains after partial inhibition of ICa has the same voltage-dependent characteristics as the control current.
Hartzell
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HC
Department of Anatomy and Cell Biology, Emory University School of Medicine, Atlanta, Georgia 30322, USA.
Rinderknecht
A
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D000818:Animals; D002121:Calcium Channel Blockers / Q000494:pharmacology*; D015220:Calcium Channels / Q000187:drug effects* / Q000502:physiology / Q000528:radiation effects; D005576:Colforsin / Q000494:pharmacology; D000242:Cyclic AMP / Q000378:metabolism; D008027:Light; D009281:Naphthalenes / Q000494:pharmacology*; D018408:Patch-Clamp Techniques; D010766:Phosphorylation / Q000187:drug effects; D011493:Protein Kinase C / Q000037:antagonists & inhibitors*; D011892:Rana catesbeiana; D013110:Sphingosine / Q000494:pharmacology
D002121:Calcium Channel Blockers; D015220:Calcium Channels; D009281:Naphthalenes; D005576:Colforsin; D000242:Cyclic AMP; D011493:Protein Kinase C; C058819:calphostin C; D013110:Sphingosine