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RHC 80267

CAS No. : 83654-05-1

MCE 站：RHC 80267

产品活性：RHC 80267 (U-57908) 是一种有效的选择性二酰基甘油脂酶 (DAGL) 抑制剂 (对犬血小板的 IC₅₀ 为 4 μM)。RHC 80267 抑制胆碱酯酶活性，IC₅₀ 为 4 μM，从而增强了乙酰胆碱引起的松弛。RHC 80267 还抑制 COX 活性和磷脂酰胆碱的水解。

研究领域：Metabolic Enzyme/Protease  |  Neuronal Signaling  |  GPCR/G Protein  |  Immunology/Inflammation

作用靶点：Acyltransferase  |  mAChR  |  COX  |  Phospholipase

In Vitro: The potentiation by RHC 80267 of the relaxation to acetylcholine could be caused by the inhibition of cholinesterase: (1) RHC 80267 does not affect the responses to carbachol, the carbamyl derivative of acetylcholine which only differs from acetylcholine by its resistance to hydrolysis by cholinesterase, and (2) the effect of RHC 80267 is mimicked by the inhibitor of cholinesterase neostigmine, RHC 80267 showing no additional effect in the presence of a maximally effective concentration of neostigmine. The determination of the effect of RHC 80267 on the cholinesterase activity of brain homogenate confirmed that RHC 80267 inhibits this enzyme in the same range of concentrations increasing the relaxation to acetylcholine, namely at 1-10 μM.

In Vivo: RHC 80267 (40 μM) enhances contractions induced by U46619 (a thromboxane A2 analog) in human and rat pulmonary arteries (hPAs and rPAs, respectively) and by angiotensin II (ANG II) in rPAs in an endothelium-dependent manner.

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