Stereoselectivity of NC-1100, a Ca-entry blocker.
1. Stereoselectivity of NC-1100 in Ca-entry blocking activity was tested in the guinea pig taenia caecum. 2. Racemic, (-)- and (+)-NC-1100 shifted the contraction-response curve of CaCl2 towards higher concentration in a parallel manner suggesting a competition. 3. (-)-NC-1100 was about 3 times as potent as (+)-NC-1100. 4. Potency of racemic NC-1100 was intermediate between those of (-)- and (+)-NC-1100.
Miyake
N
N
Department of Chemical Pharmacology, Toho University School of Pharmaceutical Sciences, Chiba, Japan.
Takayanagi
I
I
D000818:Animals; D002121:Calcium Channel Blockers / Q000494:pharmacology*; D002122:Calcium Chloride / Q000494:pharmacology; D002432:Cecum / Q000187:drug effects; D006168:Guinea Pigs; D066298:In Vitro Techniques; D008297:Male; D009131:Muscle, Smooth, Vascular / Q000187:drug effects; D010879:Piperazines / Q000494:pharmacology*; D011189:Potassium Chloride / Q000494:pharmacology; D013237:Stereoisomerism; D014665:Vasodilator Agents / Q000494:pharmacology*
D002121:Calcium Channel Blockers; D010879:Piperazines; D014665:Vasodilator Agents; C050134:tamolarizine; D011189:Potassium Chloride; D002122:Calcium Chloride