Ca-blocking action of stereoisomers of CI-951, (+)-CI-951 (NC-1500) and (-)-CI-951 in the isolated muscle preparations.
1. Stereoselectivity of CI-951 in Ca-entry blocking activity was tested in guinea pig taenia caecum and urinary bladder and rabbit thoracic aorta and basilar artery. 2. NC-1500 ((+)-CI-951) and (-)-CI-951 had a selectivity to the basilar artery. 3. NC-1500 ((+)-CI-951) was about 6-16 times as potent as (-)-CI-951. 4. These results suggest that NC-1500 ((+)-CI-951) may be considered a cerebral vasodilator and have potential usefulness as a therapeutic drug.
Koike
K
K
Department of Chemical Pharmacology, Toho University School of Pharmaceutical Sciences, Chiba, Japan.
Takayanagi
I
I
Takiguchi
S
S
Urita
Y
Y
Miyake
N
N
D000818:Animals; D002118:Calcium / Q000378:metabolism; D002121:Calcium Channel Blockers / Q000494:pharmacology*; D002122:Calcium Chloride / Q000494:pharmacology; D006168:Guinea Pigs; D066298:In Vitro Techniques; D008297:Male; D009130:Muscle, Smooth / Q000187:drug effects*; D009131:Muscle, Smooth, Vascular / Q000187:drug effects; D009287:Naphthyridines / Q000494:pharmacology*; D011188:Potassium / Q000494:pharmacology; D011817:Rabbits; D013237:Stereoisomerism; D014665:Vasodilator Agents / Q000494:pharmacology
D002121:Calcium Channel Blockers; D009287:Naphthyridines; D014665:Vasodilator Agents; C062630:CI 951; D002122:Calcium Chloride; D011188:Potassium; D002118:Calcium