A comparative study of PGI2 and two analogues (FCE 21292 and FCE 21258) in vitro and in vivo.
Two analogues of PGI2, FCE 21258 (5E-13,14-didehydro-carboprostacyclin) and FCE 21292 (5E-13,14-didehydro-20-methyl-carboprostacyclin) have been evaluated in comparison with PGI2 in different in vitro and in vivo screening tests. The rank order of potency was PGI2 greater than FCE 21292 greater than FCE 21258 in the following tests: potentiation of bradykinin-induced increased plasma protein extravasation in the guinea pig skin, inhibition of guinea pig platelet aggregation in vivo where the duration of action of FCE 21292 was longer than that of PGI2, lowering of mean systemic arterial pressure in conscious normotensive and spontaneously hypertensive rats and inhibition of rabbit platelet aggregation in vitro. In the relaxation of bovine coronary artery in vitro the rank order of potency was FCE 21292 greater than PGI2 greater than FCE 21258.
D000818:Animals; D001158:Arteries / Q000502:physiology; D001794:Blood Pressure / Q000187:drug effects*; D001798:Blood Proteins / Q000378:metabolism; D001920:Bradykinin / Q000494:pharmacology; D002417:Cattle; D004357:Drug Synergism; D011464:Epoprostenol / Q000494:pharmacology* / Q000031:analogs & derivatives; D006168:Guinea Pigs; D008297:Male; D009126:Muscle Relaxation / Q000187:drug effects; D010974:Platelet Aggregation / Q000187:drug effects*; D011817:Rabbits; D051381:Rats; D012867:Skin / Q000378:metabolism
D001798:Blood Proteins; C039191:FCE 21258; C039192:13,14-didehydro-20-methylcarboprostacyclin; D011464:Epoprostenol; D001920:Bradykinin