New drug binding sites in Ca2+ channels.
New classes of drugs modifying Ca2+ channel activity have become available, this may enlarge the clinical utilities that have been associated with established Ca2+ channel antagonists such as the dihydropyridines (for example, nifedipine). Two such classes are reviewed by Michael Spedding, Barry Kenny and Pierre Chatelain. Fantofarone is a non-dihydropyridine with a novel site of action in the L-type Ca2+ channel that appears to yield a distinct cardiovascular profile. In contrast, fluspirilene and related Na+ and Ca2+ channel inhibitors have a distinct site of action in Ca2+ channels, which is not specific for one channel type. The utility of Na+ and Ca2+ channel inhibitors in ischaemic stroke is compared with new and more selective Na+ channel inhibitors.
Spedding
M
M
Institut de Recherche Servier, Croissy sur Seine, France.
Kenny
B
B
Chatelain
P
P
D000818:Animals; D001665:Binding Sites / Q000502:physiology; D002121:Calcium Channel Blockers / Q000378:metabolism*; D005484:Fluspirilene / Q000378:metabolism*; D006801:Humans; D007212:Indolizines / Q000378:metabolism*; D010627:Phenethylamines / Q000378:metabolism*
D002121:Calcium Channel Blockers; D007212:Indolizines; D010627:Phenethylamines; D005484:Fluspirilene; C059901:fantofarone