Publication Date:
1994-02-18
Description:
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.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Li, G -- Regunathan, S -- Barrow, C J -- Eshraghi, J -- Cooper, R -- Reis, D J -- HL18974/HL/NHLBI NIH HHS/ -- New York, N.Y. -- Science. 1994 Feb 18;263(5149):966-9.〈br /〉〈span class="detail_caption"〉Author address: 〈/span〉Department of Neurology and Neuroscience, Cornell University Medical College, New York, NY 10021.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/7906055" target="_blank"〉PubMed〈/a〉
Keywords:
Adrenal Medulla/drug effects/metabolism
;
Agmatine/chemistry/isolation & purification/*metabolism/pharmacology
;
Animals
;
Binding Sites
;
Brain/enzymology/metabolism
;
*Brain Chemistry
;
Carboxy-Lyases/metabolism
;
Cattle
;
Cerebral Cortex/metabolism
;
Clonidine/analogs & derivatives/metabolism
;
Epinephrine/metabolism
;
Imidazoline Receptors
;
Neurotransmitter Agents/metabolism
;
Norepinephrine/metabolism
;
Rats
;
Receptors, Adrenergic, alpha/metabolism
;
Receptors, Drug/metabolism
Print ISSN:
0036-8075
Electronic ISSN:
1095-9203
Topics:
Biology
,
Chemistry and Pharmacology
,
Computer Science
,
Medicine
,
Natural Sciences in General
,
Physics
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