Inhibitory effects of L-arginine derivatives on endothelium-dependent vasorelaxing response to acetylcholine of the rat aorta.
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.
Wang
Guei-Jane
GJ
National Research Institute of Chinese Medicine, Taipei 112, Taiwan, ROC.
Lai
Tzi-Chung
TC
Chen
Chinpiao
C
D000109:Acetylcholine / Q000494:pharmacology*; D000818:Animals; D001013:Aorta, Thoracic / Q000187:drug effects*; D001120:Arginine / Q000031:analogs & derivatives* / Q000494:pharmacology*; D004730:Endothelium, Vascular / Q000187:drug effects*; D009119:Muscle Contraction / Q000187:drug effects* / Q000502:physiology*; D010656:Phenylephrine / Q000378:metabolism; D051381:Rats; D017207:Rats, Sprague-Dawley; D014665:Vasodilator Agents / Q000494:pharmacology
D014665:Vasodilator Agents; D010656:Phenylephrine; D001120:Arginine; D000109:Acetylcholine