dl-9a-deoky-9a-methylene PGI2 (a stable prostacyclin derivative): Preliminary pharmacological data

Abstract Carboprostacyclin (dl-9a-deoxy-9a-methylena-PGI 2 ), a new stable PGI 2 analogue, has been studied in vitro and in vivo . This analogue relaxes bovine coronary artery (potency ratio to PGI 2 = 0.17), inhibits human PRP aggregation induced by ADP (IC 50 = 12.5 nM5, deaggregates platelet clumps in cat heparinized blood (ED 50 = 10.4 μg/kg) and raises cAMP content in human PRP, but is less potent than PGI 2 . It is less potent (about 30 times) than PGI 2 in lowering blood pressure in anaesthetized rats, inhibits basal gastric secretion in the rat and is 8 and 6 times less potent than PGE 2 in protecting rat gastric mucosa from the lesions induced by stress and ASA, respectively, and about half as potent as PGE 2 in protecting intestinal mucosa from damage by indomethacin.