Inhibitory effects of L-arginine derivatives on endothelium-dependent vasorelaxing response to acetylcholine of the rat aorta

European Journal of Medicinal Chemistry
Guei-Jane WangChinpiao Chen

Abstract

N(omega)-nitro-L-arginine alkyl esters (A-1-A-B) and L-arginine alkyl esters (E-1-E-B) were synthesized, and the vasorelaxing effects of acetylcholine were studied in the absence or presence of these compounds in rat aortic rings with intact endothelium that was precontracted with phenylephrine. These compounds revealed that the nitro group is an essential inhibiting group of these inhibitors, and that hydrophobic functional groups can fine-tune the binding effects. Among them, A-3 is the most potent inhibitor.

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Citations

Jun 19, 2008·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Jiabo Li, Yaowu Sha

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