[Pharmacological studies of 2-(5H-[1]benzopyrano[2,3-b]pyridin-7-yl) propionic acid (Y-8004) (II). General pharmacological action].
This anti-inflammatory agent proved to have a therapeutic margin wider than that of indomethacin. Y-8004 exhibited little effect on the central nervous system, somatic and autonomic nervous system. On the cardiovascular system in dogs, Y-8004 induced a slight transient fall in blood pressure followed by a pressor response, increase in heart rate and coronary vasodilation at a dose of 30 mg/kg given intravenously, but no remarkable change was seen on the electrocardiogram. Y-8004 showed no effect on isolated smooth muscles such as vas deferens, ileum and atria, but inhibited gastrointestinal propulsion at a dose of 100 mg/kg given orally in mice and spontaneous contractions of the pregnant uterus of rats at a concentration of more than 10(-6)M. This agent also decreased urine volume and electrolytes in rats. This property was considered to be common to other acidic nonsteroidal anti-inflammatory agents. On the other hand, in guinea pigs, Y-8004 inhibited the bradykinin-induced bronchoconstriction and the collagen-induced platelet aggregation to a greater extent than did indomethacin. These findings suggest that Y-8004 is an active compound with properties similar to acidic non-steroidal anti-inflammatory agents such as indomethacin.
D000818:Animals; D001341:Autonomic Nervous System / Q000187:drug effects; D001777:Blood Coagulation / Q000187:drug effects; D002490:Central Nervous System / Q000187:drug effects; D004285:Dogs; D005260:Female; D005342:Fibrinolysis / Q000187:drug effects; D005769:Gastrointestinal Motility / Q000187:drug effects; D006168:Guinea Pigs; D006439:Hemodynamics / Q000187:drug effects; D066298:In Vitro Techniques; D008297:Male; D051379:Mice; D009126:Muscle Relaxation / Q000187:drug effects; D010974:Platelet Aggregation / Q000187:drug effects; D011422:Propionates / Q000494:pharmacology*; D011725:Pyridines / Q000494:pharmacology*; D011817:Rabbits; D051381:Rats; D012119:Respiration / Q000187:drug effects; D014590:Uterine Contraction / Q000187:drug effects
D011422:Propionates; D011725:Pyridines