Agmatine: an Endogenous Clonidine-Displacing Substance in the Brain
- 18 February 1994
- journal article
- Published by American Association for the Advancement of Science (AAAS) in Science
- Vol. 263 (5149) , 966-969
- https://doi.org/10.1126/science.7906055
Abstract
Clonidine, an antihypertensive drug, binds to α 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), heretofore not detected in brain. Agmatine binds to α 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 α 2 -adrenergic receptors and may act as a neurotransmitter.Keywords
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