Detail of "83654-05-1"

Reference

RHC 80267 inhibits thyrotropin-stimulated prostaglandin release from rat thyroid lobes

RHC 80267 inhibits thyrotropin-stimulated prostaglandin release from rat thyroid lobes. Levasseur, Steven; Kostelec, Martin; Burke, Gerald (Dep. Med., Cook County Hosp., Chicago, IL 60612, USA). Prostaglandins, 27(5), 673-82 (English) 1984. CODEN: PRGLBA. ISSN: 0090-6980. DOCUMENT TYPE: Journal CA Section: 2 (Mammalian Hormones) The effect of the diglyceride lipase (DG lipase) [83137-80-8] inhibitor RHC 80267 [83654-05-1] on basal and TSH [9002-71-5]-stimulated prostaglandin (PG) release was studied in rat thyroid lobes. Further, the effects of RHC 80267 on phosphatidylinositol phospholipase C (PIPLC) [63551-76-8], DG lipase, and arachidonate cyclooxygenase [39391-18-9] activities were studied in rat thyroid cytosol, plasma membrane, and whole homogenate prepns., resp. Whereas RHC 80267 inhibited DG lipase activity in a dose-related manner from 0.5 to 10 mM (17-80% inhibition), it failed to inhibit either PIPLC or arachidonate cyclooxygenase activities by more than 9% when tested at 5 and 10 mM. RHC 80267 reduced TSH-stimulated 6-keto-PGF1a [58962-34-8] and PGF2a [551-11-1] release by 100% and 57%, resp. The DG lipase inhibitor did not reduce basal release of either prostaglandin. Thus, there appears to be a PIPLC-DG lipase pathway in TSH-stimulated PG synthesis in thyroid.

Effects of (1,6-di(O-carbamoyl)cyclohexanone oxime)hexane (RHC 80267) on prostaglandin biosynthesis and accumulation of diacylglycerol and arachidonic acid in rabbit iris

Effects of (1,6-di(O-carbamoyl)cyclohexanone oxime)hexane (RHC 80267) on prostaglandin biosynthesis and accumulation of diacylglycerol and arachidonic acid in rabbit iris. Yousufzai, Sardar Y. K.; Abdel-Latif, Ata A. (Dep. Cell Mol. Biol., Med. Coll. Georgia, Augusta, GA 30912, USA). Biochem. Pharmacol., 34(4), 539-44 (English) 1985. CODEN: BCPCA6. ISSN: 0006-2952. DOCUMENT TYPE: Journal CA Section: 2 (Mammalian Hormones) Section cross-reference(s): 1 The effects of RHC 80267 [83654-05-1], a diacylglycerol lipase (DG lipase) [83137-80-8] inhibitor, on the DG lipase pathway and on arachidonic acid (AA) [506-32-1] metab. were investigated in the iris muscle. Incubation of the iris for 30 min at 37° resulted in a loss of AA from phosphatidylinositol, phosphatidylcholine, and phosphatidylethanolamine of 40, 25, and 32%, resp. The drug inhibited the activity of DG lipase in the iris microsomal fraction and it increased the accumulation of DG, AA, and other glycerolipids in iris muscle prelabeled with [14C]AA, presumably by inhibiting this enzyme. Under the same exptl. conditions, the drug increased the accumulation of DG and AA in the tissue in a dose- and time-dependent manner, and it inhibited the synthesis of PGE2 [363-24-6] and PGF2a [551-11-1] by iris and iris microsomes in a dose-dependent manner. Apparently, RHC 80267 has nonspecific effects on glycerolipid and AA metab. in this tissue. Whereas the drug does inhibit DG lipase in the intact iris, it increased the accumulation of glycerolipids and AA and it inhibited the biosynthesis of PGs in this tissue. Some doubt is cast on its use in studies on the mechanism of AA release from membrane phosphoinositides for PG synthesis.