Effects of TRK-100, a stable prostacyclin analogue, on regulation of cyclic AMP metabolism in platelets.
TRK-100 is a chemically stable analogue of prostacyclin and effective in inhibiting platelet aggregation when orally administered in experimental animals. In the present study we compared the potency of TRK-100 with those of PGI2 and PGE1 to cause an activation of adenylate cyclase activity in rat and human platelet membranes. TRK-100 was half as effective as PGI2, and 10 times more effective than PGE1 in both platelet membranes. TRK-100 also induced an activation of phosphodiesterase activity when directly added to intact platelets probably as a feedback mechanism of intracellular cAMP level like PGI2 did. TRK-100 would mimic PGI2 in the regulation of cAMP metabolism.
Nogimori
K
K
Central Research Laboratories, Kaken Pharmaceutical Co. Ltd., Kyoto, Japan.
Kajikawa
N
N
Nishio
S
S
Yajima
M
M
D015105:3',5'-Cyclic-AMP Phosphodiesterases / Q000097:blood; D000262:Adenylyl Cyclases / Q000097:blood; D000527:Alprostadil / Q000494:pharmacology; D000818:Animals; D001792:Blood Platelets / Q000187:drug effects* / Q000378:metabolism; D000242:Cyclic AMP / Q000097:blood*; D004789:Enzyme Activation / Q000187:drug effects; D011464:Epoprostenol / Q000494:pharmacology* / Q000031:analogs & derivatives; D006801:Humans; D066298:In Vitro Techniques; D010975:Platelet Aggregation Inhibitors / Q000494:pharmacology*; D051381:Rats; D011919:Rats, Inbred Strains
D010975:Platelet Aggregation Inhibitors; C048081:beraprost; D011464:Epoprostenol; D000242:Cyclic AMP; D015105:3',5'-Cyclic-AMP Phosphodiesterases; D000262:Adenylyl Cyclases; D000527:Alprostadil