Agmatine: an endogenous clonidine-displacing substance in the brain.

Article Details

Citation

Li G, Regunathan S, Barrow CJ, Eshraghi J, Cooper R, Reis DJ

Agmatine: an endogenous clonidine-displacing substance in the brain.

Science. 1994 Feb 18;263(5149):966-9.

PubMed ID
7906055 [ View in PubMed
]
Abstract

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), heretofore 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.

DrugBank Data that Cites this Article

Drugs
Drug Targets
DrugTargetKindOrganismPharmacological ActionActions
AgmatineAlpha-2C adrenergic receptorProteinHumans
Yes
Agonist
Details
AgmatineNischarinProteinHumans
Yes
Agonist
Details