The putative prostacyclin receptor antagonist (FCE-22176) is a full agonist on human platelets and NCB-20 cells.
The action of FCE-22176 on prostacyclin receptors of human platelets and the NCB-20 cell line have been examined. FCE-22176 is a full agonist in both systems, mediating activation of adenylate cyclase. The concentration required for half-maximum enzyme activation was 174 nM in platelet membranes and 193 nM in homogenates of NCB-20 cells. The binding of [3H]iloprost to human platelet or NCB-20 cell membranes was inhibited by FCE-22176, and Ki values of 400 and 280 nM were obtained.
D000262:Adenylyl Cyclases / Q000378:metabolism*; D001792:Blood Platelets / Q000187:drug effects*; D002460:Cell Line; D002462:Cell Membrane / Q000201:enzymology; D004789:Enzyme Activation / Q000187:drug effects; D011464:Epoprostenol / Q000378:metabolism / Q000494:pharmacology* / Q000031:analogs & derivatives; D006801:Humans; D016285:Iloprost; D066298:In Vitro Techniques; D044006:Receptors, Epoprostenol; D011982:Receptors, Prostaglandin / Q000187:drug effects*
D044006:Receptors, Epoprostenol; D011982:Receptors, Prostaglandin; C039192:13,14-didehydro-20-methylcarboprostacyclin; D011464:Epoprostenol; D000262:Adenylyl Cyclases; D016285:Iloprost