RHC-80267 is a potent and selective diacylglycerol lipase inhibitor with an IC50 value of 4µM for canine platelet diglyceride lipase.[1] In the circular smooth muscle isolated from the stomach antrum of guinea pig, RHC-80267 at a concentration of 0.3μM increased the slow potentials from 1.12±0.31 min–1 to 2.43±0.67 min–1. The refractory period for the generation of slow potentials in smooth muscle cells was also reduced in the presence of 0.3μM RHC-80267.[2] In rat brain homogenates, RHC-80267 inhibited cholinesterase activity in a concentration-dependent manner with a pIC50 value of 5.39±0.06 (IC50 = 4μM). Pre-incubation of rat artery rings with RHC-80267 (10-7–10-5M) resulted in a concentration-dependent leftward shift of the concentration-effect curve to acetylcholine. Pre-incubation with calphostin C (1μM) and RHC-80267 (10μM) decreased the contraction evoked by noradrenaline by 50±9%. In KCl-contracted arteries, pre-incubation with 10μM RHC-80267 led to a leftward shift of the relaxation evoked by acetylcholine.[3]
作用机制
RHC-80267 is a diacylglycerol lipase inhibitor that enhances the activity of protein kinase C by elevating the level of diacylglycerol.[2]
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