AGMATINE - AN ENDOGENOUS CLONIDINE-DISPLACING SUBSTANCE IN THE BRAIN
AGMATINE - AN ENDOGENOUS CLONIDINE-DISPLACING SUBSTANCE IN THE BRAIN
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DOI：
10.1126/science.7906055
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发表时间：
1994-02-18
期刊：
影响因子：
56.9
通讯作者：
REIS, DJ
中科院分区：
文献类型：
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作者：
LI, G;REGUNATHAN, S;REIS, DJ
可乐定是一种抗高血压药物，可与α(2)-肾上腺素能和咪唑啉受体结合。咪唑啉受体的内源性配体可能是一种可乐定置换物质，一种从牛脑中分离出来的小分子。这种可乐定置换物质被提纯，并经质谱学鉴定为胍丁胺(脱羧化精氨酸)，目前在大脑中未检测到。胍丁胺与α(2)-肾上腺素能和咪唑啉受体结合，刺激肾上腺嗜铬细胞释放儿茶酚胺。它的生物合成酶精氨酸脱羧酶存在于大脑中。本地合成的胍丁胺是咪唑啉受体的内源性激动剂，咪唑啉受体是α(2)-肾上腺素能受体的非儿茶酚胺配体，可能起神经递质的作用。
Clonidine, an antihypertensive drug, binds to alpha(2)-adrenergic and imidazoline receptors. The endogenous ligand for imidazoline receptors may be a clonidine-displacing substance, a small molecule isolated from bovine brain. This clonidine-displacing substance was purified and determined by mass spectroscopy to be agmatine (decarboxylated arginine), here-tofore not detected in brain. Agmatine binds to alpha(2)-adrenergic and imidazoline receptors and stimulates release of catecholamines from adrenal chromaffin cells. Its biosynthetic enzyme, arginine decarboxylase, is present in brain. Agmatine, locally synthesized, is an endogenous agonist at imidazoline receptors, a noncatecholamine ligand at alpha(2)-adrenergic receptors and may act as a neurotransmitter.