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Cannabinoid receptors and their endogenous ligands
1Faculty of Pharmaceutical Sciences, Teikyo University, Sagamiko, Kanagawa 199-0195, Japan. sugiurat@pharm.teikyo-u.ac.jp
Journal of Biochemistry
|July 5, 2002
Summary
Researchers identified 2-arachidonoylglycerol as the intrinsic natural ligand for cannabinoid receptors, distinct from anandamide. This finding links cannabinoid receptor function to inositol phospholipid turnover in various tissues.
Area of Science:
- Neuroscience
- Biochemistry
- Pharmacology
Background:
- Delta9-Tetrahydrocannabinol (THC) interacts with cannabinoid receptors, producing pharmacological effects.
- Cloning of the cannabinoid receptor 1 (CB1) gene in 1990 spurred the search for endogenous ligands.
- Anandamide and 2-arachidonoylglycerol were identified as endogenous ligands with cannabimimetic activities.
Purpose of the Study:
- To determine the intrinsic natural ligand for the cannabinoid receptor.
- To elucidate the relationship between cannabinoid receptors and inositol phospholipid metabolism.
Main Methods:
- Structure-activity relationship experiments were conducted.
- Analysis of endogenous ligands isolated from biological sources.
Main Results:
- 2-arachidonoylglycerol, but not anandamide, was identified as the intrinsic natural ligand for the cannabinoid receptor.
- 2-arachidonoylglycerol is a degradation product of inositol phospholipids.
- This establishes a link between cannabinoid receptor function and enhanced inositol phospholipid turnover.
Conclusions:
- 2-arachidonoylglycerol plays a key role as the endogenous ligand for cannabinoid receptors.
- Cannabinoid receptor function is integrated with cellular signaling pathways involving inositol phospholipids.
- Further investigation into the physiological roles of cannabinoid receptors and 2-arachidonoylglycerol in mammalian tissues, including the nervous system, is warranted.