PGE1 but not PGI2 desensitizes the PGI2 receptor-adenylate cyclase complex in human foreskin fibroblasts.
In intact cells or in membranes prepared from intact cells that were preincubated with PGE1, subsequent PGI2-stimulation is attenuated. Preincubation of cells with PGI2 does not induce desensitization of PGI2-stimulated adenylate cyclase. These data suggest that HFF cells must be constantly exposed to a biologically active prostaglandin for desensitization to occur. The intrinsic chemical lability of PGI2 may be a biochemical protection mechanism against desensitization in cells that normally respond to PGI2.
D000262:Adenylyl Cyclases / Q000378:metabolism*; D002478:Cells, Cultured; D004305:Dose-Response Relationship, Drug; D004789:Enzyme Activation / Q000187:drug effects; D011464:Epoprostenol / Q000494:pharmacology* / Q000031:analogs & derivatives; D006801:Humans; D007545:Isoproterenol / Q000494:pharmacology; D008297:Male; D011453:Prostaglandins / Q000494:pharmacology*; D011458:Prostaglandins E / Q000494:pharmacology*; D011465:Prostaglandins, Synthetic / Q000494:pharmacology*; D011956:Receptors, Cell Surface / Q000187:drug effects*; D011982:Receptors, Prostaglandin / Q000187:drug effects*; D012867:Skin / Q000201:enzymology
D011453:Prostaglandins; D011458:Prostaglandins E; D011465:Prostaglandins, Synthetic; D011956:Receptors, Cell Surface; D011982:Receptors, Prostaglandin; C025006:nitriloprostaglandin I2; D011464:Epoprostenol; D000262:Adenylyl Cyclases; D007545:Isoproterenol