[Effects of 1, 4-bis-(3-(3, 4, 5-trimethoxy benzoyl oxy)-propyl) perhydro-1, 4-diazepine (dilazep) on the isolated smooth muscles].
The effects of a new coronary vasodilator (dilazep) on isolated intestine, taenia coli, trachea, vas deferens, uter, aorta and coronary arteries were investigated in rats, guinea pigs, rabbits and dogs. Dilazep showed relaxant effects on isolated smooth muscle in a concentration of 10(-5) 3 X 10(-4) M and non-competitive inhibition on contraction induced by agonists (pD'2: 4.405.05). In guinea pig taenia coli, dilazep had a relaxant effect on K-contracture. The effect was qualitatively similar to that of papaverine. In guinea pig taenia coli, dilazep showed a Ca++ antagonistic effect in a concentration as high as 3 X 10(-6)M. The potency was stronger than dipyridamole, NaNO2 and aminophylline and equalled that of papaverine and hexobendine. In guinea pig taenia coli, dilazip potentiated relaxant effects induced by adenosine and adenine nucleotides in a concentration as high as 10(-8)M. The potency was stronger than that of dipyridamole. From these results, it is suggested that the potentiating effect of both adenosine and adenine nucleotides and Ca++ antagonistic effect of dilazep may play an important role in producing the coronary vasodilating effect.
D000227:Adenine Nucleotides / Q000494:pharmacology; D000241:Adenosine / Q000494:pharmacology; D000818:Animals; D001011:Aorta / Q000187:drug effects; D002118:Calcium / Q000502:physiology; D004109:Dilazep / Q000494:pharmacology*; D004285:Dogs; D004305:Dose-Response Relationship, Drug; D005260:Female; D006168:Guinea Pigs; D066298:In Vitro Techniques; D007422:Intestines / Q000187:drug effects; D008297:Male; D009119:Muscle Contraction / Q000187:drug effects; D009130:Muscle, Smooth / Q000187:drug effects*; D010208:Papaverine / Q000494:pharmacology; D011188:Potassium / Q000502:physiology; D011817:Rabbits; D051381:Rats; D014599:Uterus / Q000187:drug effects; D014649:Vas Deferens / Q000187:drug effects
D000227:Adenine Nucleotides; D010208:Papaverine; D004109:Dilazep; D000241:Adenosine; D011188:Potassium; D002118:Calcium