Cannabinoid pharmacology: implications for additional cannabinoid receptor subtypes

Cannabinoid pharmacology: implications for additional cannabinoid receptor subtypes Δ 9 -Tetrahydrocannabinol (Δ 9 -THC), the primary psychoactive constituent of marijuana ( Cannabis sativa ), is known to bind to two cannabinoid receptors: CB 1 receptors, located primarily in the brain, and CB 2 receptors, located primarily in the periphery. Recent research has suggested that other cannabinoids, including anandamide and WIN 55,212-2, may also act at novel non-CB 1 , non-CB 2 cannabinoid receptor(s). Anandamide produces a number of in vivo pharmacological effects in CB 1 knockout mice that are not produced by Δ 9 -THC and cannot be explained by anandamide's rapid metabolism. In addition, in vitro anandamide and WIN 55,212-2 stimulate ( 35 S)GTPγS binding in both CB 1 knockout and wildtype mice while Δ 9 -THC stimulates this binding only in wildtype mice. Although anandamide and vanilloid agonists share pharmacological effects, anandamide's actions in CB 1 knockout mice do not appear to be mediated by vanilloid VR 1 receptors. While not yet conclusive, these results suggest the possibility of additional cannabinoid receptors in the brain and periphery. http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png Chemistry and Physics of Lipids Elsevier

Cannabinoid pharmacology: implications for additional cannabinoid receptor subtypes

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Publisher
Elsevier
Copyright
Copyright © 2002 Elsevier Science Ireland Ltd
ISSN
0009-3084
eISSN
1873-2941
DOI
10.1016/S0009-3084(02)00146-9
Publisher site
See Article on Publisher Site

Abstract

Δ 9 -Tetrahydrocannabinol (Δ 9 -THC), the primary psychoactive constituent of marijuana ( Cannabis sativa ), is known to bind to two cannabinoid receptors: CB 1 receptors, located primarily in the brain, and CB 2 receptors, located primarily in the periphery. Recent research has suggested that other cannabinoids, including anandamide and WIN 55,212-2, may also act at novel non-CB 1 , non-CB 2 cannabinoid receptor(s). Anandamide produces a number of in vivo pharmacological effects in CB 1 knockout mice that are not produced by Δ 9 -THC and cannot be explained by anandamide's rapid metabolism. In addition, in vitro anandamide and WIN 55,212-2 stimulate ( 35 S)GTPγS binding in both CB 1 knockout and wildtype mice while Δ 9 -THC stimulates this binding only in wildtype mice. Although anandamide and vanilloid agonists share pharmacological effects, anandamide's actions in CB 1 knockout mice do not appear to be mediated by vanilloid VR 1 receptors. While not yet conclusive, these results suggest the possibility of additional cannabinoid receptors in the brain and periphery.

Journal

Chemistry and Physics of LipidsElsevier

Published: Dec 31, 2002

References

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  • The endogenous lipid anandamide is a full agonist at the human vanilloid receptor (hVR1)
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