Chemistry of calcium antagonists
Meyer, H.; Bossert, F.; Wehinger, E.; Towart, R.; Bellemann, P.
Hypertension 5(4 Pt 2): II2-II7
1983
ISSN/ISBN: 0194-911X PMID: 6345372 Document Number: 210965
A brief review describes nonspecific and specific chemical structures that inhibit calcium (Ca) entry into cells through the slow Ca channel in cell membranes. Nonspecific Ca antagonists include: magnesium, lanthanum, diazoxide, beta-2 receptor agonists, certain aminoglycoside and polyether antibiotics, methadone, and SKF 525A. Specific Ca antagonists include prenylamine, fendiline, verapamil, gallopamil, tiapamil, bencyclan, cinnarizine, and diltiazem. The chemical structures of all these drugs contain an aryl portion, with a basic alkyl or aralkyl side chain as an essential active structure. However, a new, highly-active Ca antagonist (similar to a 4-aryl-dihydropyridine) lacks this side chain. The first drug used in the 4-aryl-dihydropyridine series was nifedipine (an antianginal and antihypertensive agent). Other dihydropyridines usually contain an asymmetric carbon atom, and occur as optical isomers with different Ca antagonist effects. The chemical structures and stereochemistry of the various organic Ca antagonists are illustrated. (wz)