The adenylate cyclase of rheumatoid synovial fluid macrophages is more sensitive for dl-5E, 19,14-di dehydro-carbo-prostacyclin, a stable prostacyclin analogue, than for prostaglandin E2.
dl-5E, 19,14-di dehydro-carbo-prostacyclin (DDH-carbo PGI2), a stable prostacyclin (PGI2) derivative, but not prostaglandin (PG) E2, stimulated the adenylate cyclase of synovial fluid macrophages, isolated from rheumatoid patients with an active synovitis, in a dose dependent manner (10-1000 ng/ml). DDH-carbo PGI2 also stimulated synovial macrophage cAMP synthesis when injected into the knee joint. Exogenous arachidonic acid (AA) had little effect on cyclic-AMP (cAMP) formation or PGI2 release (assayed as 6ketoPGF1 alpha). It stimulated, however, the release of PGE2 and, to a lesser extent, thromboxane (Tx) A2 (measured as TxB2).
Elliott
G R
GR
Department of Pharmacology, Erasmus University Rotterdam, The Netherlands.
Swaak
A
A
Bonta
I L
IL
D000262:Adenylyl Cyclases / Q000378:metabolism*; D016718:Arachidonic Acid; D001095:Arachidonic Acids / Q000378:metabolism; D001172:Arthritis, Rheumatoid / Q000201:enzymology*; D000242:Cyclic AMP / Q000096:biosynthesis; D015232:Dinoprostone / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D011464:Epoprostenol / Q000378:metabolism / Q000494:pharmacology* / Q000031:analogs & derivatives; D006801:Humans; D008264:Macrophages / Q000187:drug effects / Q000201:enzymology*; D013582:Synovial Fluid / Q000166:cytology*
D001095:Arachidonic Acids; D016718:Arachidonic Acid; C039191:FCE 21258; D011464:Epoprostenol; D000242:Cyclic AMP; D000262:Adenylyl Cyclases; D015232:Dinoprostone