REV 2871 (CHBZ): a novel inhibitor of histamine release.
CHBZ is a novel, non-disodium cromoglycate (DSCG)-like, antiallergic drug in vitro. Whereas DSCG loses antisecretory activity with increasing time of preincubation with rat mast cells (RMC) before antigen challenge, and does not inhibit non-immunologically mediated release from human leukocytes, CHBZ exerts long-lived inhibition of both types of release from both types of cells. CHBZ is taken up by RMC in a saturable and time-dependent manner. It is enzymatically converted inside RMC to a DSCG-like metabolite, REV 3579, which, because of its ionic character, accumulates inside the cell. CHBZ, presumably through the action of the REV 3579 generated intracellularly, may mediate long-lived phosphorylation of the same 78 K protein which is transiently phosphorylated upon exposure of RMC to DSCG.
D000818:Animals; D001692:Biological Transport; D002250:Carbon Radioisotopes; D006634:Histamine H1 Antagonists / Q000494:pharmacology*; D006636:Histamine Release / Q000187:drug effects*; D006801:Humans; D007073:Immunoglobulin E / Q000276:immunology; D007700:Kinetics; D007962:Leukocytes / Q000187:drug effects / Q000276:immunology; D008407:Mast Cells / Q000187:drug effects / Q000276:immunology; D010080:Oxazoles / Q000378:metabolism / Q000494:pharmacology*; D011865:Radioisotope Dilution Technique; D051381:Rats; D011919:Rats, Inbred Strains; D013329:Structure-Activity Relationship
D002250:Carbon Radioisotopes; D006634:Histamine H1 Antagonists; D010080:Oxazoles; D007073:Immunoglobulin E; C049843:2-ethoxyethyl 5-chlorobenzoxazole-2-carboxylate