NG-amino-L-arginine: a new potent antagonist of L-arginine-mediated endothelium-dependent relaxation.

NG-amino-L-arginine: a new potent antagonist of L-arginine-mediated endothelium-dependent relaxation.
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NG-氨基-L-精氨酸:L-精氨酸介导的内皮依赖性松弛的新型有效拮抗剂。

DOI:
10.1016/0006-291x(90)92343-x
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发表时间:
1990
影响因子:
3.1
通讯作者:
Ignarro,LJ
Ignarro,LJ
中科院分区:
生物学4区
文献类型:
--
作者:
Fukuto,JM;Wood,KS;Byrns,RE;Ignarro,LJ

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本研究检测了ng -氨基- l -精氨酸(一种新型的l -精氨酸结构类似物)对牛肺动脉分离环内皮依赖性松弛、收缩和循环GMP积累的影响。ng -氨基- l -精氨酸引起强效的立体选择性内皮依赖性收缩,这与平滑肌中环GMP基础水平的显著内皮依赖性下降有关。ng -氨基- l -精氨酸引起乙酰胆碱引起的松弛和循环GMP积累的浓度依赖性、竞争性和立体选择性拮抗。ng -氨基- l-精氨酸的效力是ng -甲基- l-精氨酸的100- 300倍,并且不抑制硝化甘油引起的内皮非依赖性松弛。这种有效的l -精氨酸抑制类似物将为研究l -精氨酸衍生的一氧化氮在体外和体内的生物合成和生物学作用提供有用的化学探针。
This study examined the influence of NG-amino-L-arginine, a novel structural analog of L-arginine, on endothelium-dependent relaxation, contraction, and cyclic GMP accumulation in isolated rings of bovine pulmonary artery. NG-Amino-L-arginine caused potent and stereoselective endothelium-dependent contraction that was associated with a marked and endothelium-dependent decline in basal levels of cyclic GMP in smooth muscle. NG-Amino-L-arginine caused concentration-dependent, competitive, and stereoselective antagonism of acetylcholine-elicited relaxation and cyclic GMP accumulation. NG-Amino-L-arginine was 100- to 300- fold more potent than NG-methyl-L-arginine and did not inhibit endothelium-independent relaxation elicited by nitroglycerin. This potent inhibitory analog of L-arginine should be a useful chemical probe for studying the biosynthesis and biological role of L-arginine-derived nitric oxide bothin vitroandin vivo.