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Chemical Compound Review

CHEMBL158897     (cyclohexylideneamino) N-[6...

Synonyms: AG-K-15201, BSPBio_001074, KBioGR_000414, KBioSS_000414, RHC-80267, ...
 
 
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Disease relevance of U 57908

  • In mouse neuroblastoma N18TG2 cells prelabeled with [3H]arachidonic acid ([3H]AA) the biosynthesis of 2-arachidonoylglycerol (2-AG) is induced by ionomycin in a fashion sensitive to an inhibitor of diacylglycerol (DAG) lipase, RHC 80267, but not to four different phospholipase C (PLC) blockers [1].
 

High impact information on U 57908

  • Moreover, inhibitors of phosphatidate phosphohydrolase (propranolol) and diacylglycerol lipase (RHC-80267), attenuated ET-1-induced 6-keto-PGF1 alpha formation [2].
  • Dependence of secretory responses to gonadotropin-releasing hormone on diacylglycerol metabolism. Studies with a diacylglycerol lipase inhibitor, RHC 80267 [3].
  • MAFP (a cPLA2 inhibitor) and REV 5901 (a 5-lipoxygenase inhibitor as well as a competitive antagonist of peptide leukotrienes), but not RHC 80267 (a diacylglycerol lipase inhibitor), also inhibited the UTP-induced response [4].
  • Similarly, the diacylglycerol lipase inhibitor RHC 80267 did not alter TAG synthesis from plasma membrane DAG, further supporting direct incorporation of DAG into TAG.These studies indicate that DAG derived from plasma membrane phospholipid is largely used for TAG formation, and support the view that this mechanism can terminate DAG signals [5].
  • Inclusion of RHC 80267 in the ionophore induction system also resulted in significant accelerations of the onset of exocytosis [6].
 

Biological context of U 57908

  • Lysosomal diacylglycerol hydrolysis is sensitive towards non-ionic detergents, cationic amphiphilic drugs and the lipase inhibitor RHC 80267 [7].
  • Neither the Ca2+-independent PLA2 inhibitor, HELSS [E-6-(bromomethylene)-tetrahydro-3-(1-naphthalenyl)-2H-pyran-2-one], nor DAG lipase inhibitor, RHC-80267 [1,6-bis-(cyclohexyloximino-carbonylamino)-hexane] altered EDHF-mediated vasodilation [8].
  • A DGL inhibitor, RHC-80267, inhibited DGL activity in a dose-dependent manner with an IC50 (the concentration required for 50% inhibition) of about 5 microM [9].
  • The refractory period for the generation of slow potentials evoked by depolarizing stimuli was about 8 s, and it was decreased to about 5 s by RHC-80267, with no significant alteration to the amplitude of spontaneous or evoked slow potentials [10].
  • RHC-80267 (0.3-1 microM) increased the frequency of slow potential generation, with no alteration to the amplitude of either the slow potentials or the resting membrane potential [10].
 

Anatomical context of U 57908

  • Inhibition of diacylglycerol metabolism in isolated cardiac myocytes by U-57 908 (RHC 80267), a diacylglycerol lipase inhibitor [11].
  • On the other hand, glycerol output from PC-PLC treated myocytes was effectively inhibited by a diacylglycerol lipase inhibitor (U-57908, The Upjohn Company) [12].
  • 5. The lack of effect of RHC 80267 in this situation may indicate that in the mast cell, DAG kinase is more active than DAG lipase in degrading physiological levels of DAG [13].
  • U-57 908 (RHC 80267) inhibited diacylglycerol (DG) lipase activity in soluble and microsomal subcellular fractions from cardiac myocytes isolated from adult rat hearts; half-maximal inhibition was observed at a concentration of 3.5 microM [11].
  • These results indicate that the potentiation of acetylcholine-evoked responses by RHC-80267 in rat mesenteric artery is caused by the inhibition of the cholinesterase activity in the vascular wall [14].
 

Associations of U 57908 with other chemical compounds

 

Gene context of U 57908

References

  1. Phosphatidic acid as the biosynthetic precursor of the endocannabinoid 2-arachidonoylglycerol in intact mouse neuroblastoma cells stimulated with ionomycin. Bisogno, T., Melck, D., De Petrocellis, L., Di Marzo, V. J. Neurochem. (1999) [Pubmed]
  2. Prostacyclin formation elicited by endothelin-1 in rat aorta is mediated via phospholipase D activation and not phospholipase C or A2. Wright, H.M., Malik, K.U. Circ. Res. (1996) [Pubmed]
  3. Dependence of secretory responses to gonadotropin-releasing hormone on diacylglycerol metabolism. Studies with a diacylglycerol lipase inhibitor, RHC 80267. Chang, J.P., Morgan, R.O., Catt, K.J. J. Biol. Chem. (1988) [Pubmed]
  4. Lipoxygenase metabolites as mediators of UTP-induced intracellular acidification in mouse RAW 264.7 macrophages. Lin, W.W., Chang, S.H., Wu, M.L. Mol. Pharmacol. (1998) [Pubmed]
  5. Diacylglycerol generated in CHO cell plasma membrane by phospholipase C is used for triacylglycerol synthesis. Igal, R.A., Caviglia, J.M., de Gómez Dumm, I.N., Coleman, R.A. J. Lipid Res. (2001) [Pubmed]
  6. The role of diacylglycerol in the exocytosis of the sperm acrosome. Studies using diacylglycerol lipase and diacylglycerol kinase inhibitors and exogenous diacylglycerols. Roldan, E.R., Harrison, R.A. Biochem. J. (1992) [Pubmed]
  7. Diacylglycerol hydrolysis in rat liver lysosomes. Kunze, H., Hesse, B., Löffler, B.M. FEBS Lett. (1986) [Pubmed]
  8. Calcium-dependent phospholipase A2 mediates the production of endothelium-derived hyperpolarizing factor in perfused rat mesenteric prearteriolar bed. Adeagbo, A.S., Henzel, M.K. J. Vasc. Res. (1998) [Pubmed]
  9. Purification and characterization of diacylglycerol lipase from human platelets. Moriyama, T., Urade, R., Kito, M. J. Biochem. (1999) [Pubmed]
  10. Effects of RHC-80267, an inhibitor of diacylglycerol lipase, on excitation of circular smooth muscle of the guinea-pig gastric antrum. Suzuki, H., Kito, Y., Fukuta, H., Yamamoto, Y. Journal of smooth muscle research = Nihon Heikatsukin Gakkai kikanshi. (2002) [Pubmed]
  11. Inhibition of diacylglycerol metabolism in isolated cardiac myocytes by U-57 908 (RHC 80267), a diacylglycerol lipase inhibitor. Chuang, M., Severson, D.L. J. Mol. Cell. Cardiol. (1990) [Pubmed]
  12. Phospholipid degradation in hypoxic/reoxygenated cardiomyocytes in response to phospholipase C from Bacillus cereus. Forsdahl, K., Larsen, T.S. J. Mol. Cell. Cardiol. (1995) [Pubmed]
  13. The actions of inhibitors of diacylglycerol kinase and diacylglycerol lipase on histamine release from rat peritoneal mast cells. Cantwell, M.E., Foreman, J.C. Br. J. Pharmacol. (1987) [Pubmed]
  14. The diacylglycerol lipase inhibitor RHC-80267 potentiates the relaxation to acetylcholine in rat mesenteric artery by anti-cholinesterase action. Ghisdal, P., Vandenberg, G., Hamaide, M.C., Wibo, M., Morel, N. Eur. J. Pharmacol. (2005) [Pubmed]
  15. Angiogenin activates phospholipase C and elicits a rapid incorporation of fatty acid into cholesterol esters in vascular smooth muscle cells. Moore, F., Riordan, J.F. Biochemistry (1990) [Pubmed]
  16. Accumulation of cyclic AMP elicited by vasoactive intestinal peptide is potentiated by noradrenaline, histamine, adenosine, baclofen, phorbol esters, and ouabain in mouse cerebral cortical slices: studies on the role of arachidonic acid metabolites and protein kinase C. Schaad, N.C., Schorderet, M., Magistretti, P.J. J. Neurochem. (1989) [Pubmed]
  17. Basic fibroblast growth factor-stimulated arachidonic acid release in rat pancreatic acini: sequential action of tyrosine kinase, phospholipase C, protein kinase C and diacylglycerol lipase. Hou, W., Arita, Y., Morisset, J. Cell. Signal. (1996) [Pubmed]
  18. Alpha-1A adrenergic receptor stimulation with phenylephrine promotes arachidonic acid release by activation of phospholipase D in rat-1 fibroblasts: inhibition by protein kinase A. Ruan, Y., Kan, H., Parmentier, J.H., Fatima, S., Allen, L.F., Malik, K.U. J. Pharmacol. Exp. Ther. (1998) [Pubmed]
  19. Endothelium-derived 2-arachidonylglycerol: an intermediate in vasodilatory eicosanoid release in bovine coronary arteries. Gauthier, K.M., Baewer, D.V., Hittner, S., Hillard, C.J., Nithipatikom, K., Reddy, D.S., Falck, J.R., Campbell, W.B. Am. J. Physiol. Heart Circ. Physiol. (2005) [Pubmed]
  20. The Ang II-induced growth of vascular smooth muscle cells involves a phospholipase D-mediated signaling mechanism. Freeman, E.J. Arch. Biochem. Biophys. (2000) [Pubmed]
  21. Signal transduction by the erythropoietin receptor: evidence for the activation of phospholipases A2 and C. Mason-Garcia, M., Clejan, S., Tou, J.S., Beckman, B.S. Am. J. Physiol. (1992) [Pubmed]
  22. Involvement of arachidonate metabolism in neurotensin-induced prolactin release in vitro. Canonico, P.L., Speciale, C., Sortino, M.A., Scapagnini, U. Am. J. Physiol. (1985) [Pubmed]
  23. 5-Hydroxyeicosatetraenoic acid increases prolactin release from rat anterior pituitary cells. Koike, K., Judd, A.M., MacLeod, R.M. Endocrinology (1985) [Pubmed]
  24. Inhibition of myocardial lipoprotein lipase by U-57,908 (RHC 80267). Carroll, R., Severson, D.L. Lipids (1992) [Pubmed]
 
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