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Isolation and measurement of the endogenous cannabinoid receptor agonist, anandamide, in brain and peripheral tissues of human and rat
Author(s) -
Felder Christian C.,
Nielsen Amie,
Briley Eileen M.,
Palkovits Miklós,
Priller Joseph,
Axelrod Julius,
Nguyen Duy N.,
Richardson John M.,
Riggin Ralph M.,
Koppel Gary A.,
Paul Steven M.,
Becker Gerald W.
Publication year - 1996
Publication title -
febs letters
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.593
H-Index - 257
eISSN - 1873-3468
pISSN - 0014-5793
DOI - 10.1016/0014-5793(96)00891-5
Subject(s) - anandamide , cannabinoid receptor , depolarization induced suppression of inhibition , cannabinoid , endocannabinoid system , human brain , agonist , endocrinology , medicine , cannabinoid receptor type 2 , chemistry , receptor , biology , pharmacology , neuroscience
Anandamide (arachidonylethanolamide) is a novel lipid neurotransmitter first isolated from porcine brain which has been shown to be a functional agonist for the cannabinoid CB1 and CB2 receptors. Anandamide has never been isolated from human brain or peripheral tissues and its role in human physiology has not been examined. Anandamide was measured by LC/MS/MS and was found in human and rat hippocampus (and human parahippocampal cortex), striatum, and cerebellum, brain areas known to express high levels of CB1 cannabinoid receptors. Significant levels of anandamide were also found in the thalamus which expresses low levels of CB1 receptors. Anandamide was also found in human and rat spleen which expresses high levels of the CB2 cannabinoid receptor. Small amounts of anandamide were also detected in human heart and rat skin. Only trace quantities were detected in pooled human serum, plasma, and CSF. The distribution of anandamide in human brain and spleen supports its potential role as an endogenous agonist in central and peripheral tissues. The low levels found in serum, plasma, and CSF suggest that it is metabolized in tissues where it is synthesized, and that its action is probably not hormonal in nature.