Cannabinoid Receptors: Where They are and What They do

Cannabinoid Receptors: Where They are and What They do The endocannabinoid system consists of the endogenous cannabinoids (endocannabinoids), cannabinoid receptors and the enzymes that synthesise and degrade endocannabinoids. Many of the effects of cannabinoids and endocannabinoids are mediated by two G protein‐coupled receptors (GPCRs), CB1 and CB2, although additional receptors may be involved. CB1 receptors are present in very high levels in several brain regions and in lower amounts in a more widespread fashion. These receptors mediate many of the psychoactive effects of cannabinoids. CB2 receptors have a more restricted distribution, being found in a number of immune cells and in a few neurones. Both CB1 and CB2 couple primarily to inhibitory G proteins and are subject to the same pharmacological influences as other GPCRs. Thus, partial agonism, functional selectivity and inverse agonism all play important roles in determining the cellular response to specific cannabinoid receptor ligands. http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png Journal of Neuroendocrinology Wiley

Cannabinoid Receptors: Where They are and What They do

Journal of Neuroendocrinology, Volume 20 – May 1, 2008

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Publisher
Wiley
Copyright
© 2008 The Author. Journal Compilation © 2008 Blackwell Publishing Ltd
ISSN
0953-8194
eISSN
1365-2826
DOI
10.1111/j.1365-2826.2008.01671.x
pmid
18426493
Publisher site
See Article on Publisher Site

Abstract

The endocannabinoid system consists of the endogenous cannabinoids (endocannabinoids), cannabinoid receptors and the enzymes that synthesise and degrade endocannabinoids. Many of the effects of cannabinoids and endocannabinoids are mediated by two G protein‐coupled receptors (GPCRs), CB1 and CB2, although additional receptors may be involved. CB1 receptors are present in very high levels in several brain regions and in lower amounts in a more widespread fashion. These receptors mediate many of the psychoactive effects of cannabinoids. CB2 receptors have a more restricted distribution, being found in a number of immune cells and in a few neurones. Both CB1 and CB2 couple primarily to inhibitory G proteins and are subject to the same pharmacological influences as other GPCRs. Thus, partial agonism, functional selectivity and inverse agonism all play important roles in determining the cellular response to specific cannabinoid receptor ligands.

Journal

Journal of NeuroendocrinologyWiley

Published: May 1, 2008

References

  • Role of endogenous cannabinoids in synaptic signaling
    Freund, Freund; Katona, Katona; Piomelli, Piomelli
  • Cannabinoid receptors as therapeutic targets
    Mackie, Mackie
  • The complications of promiscuity: endocannabinoid action and metabolism
    Alexander, Alexander; Kendall, Kendall
  • The orphan receptor GPR55 is a novel cannabinoid receptor
    Ryberg, Ryberg; Larsson, Larsson; Sjogren, Sjogren; Hjorth, Hjorth; Hermansson, Hermansson; Leonova, Leonova; Elebring, Elebring; Nilsson, Nilsson; Drmota, Drmota; Greasley, Greasley
  • Expression of the cannabinoid receptor CB1 in distinct neuronal subpopulations in the adult mouse forebrain
    Marsicano, Marsicano; Lutz, Lutz
  • CB1 receptors: emerging evidence for central and peripheral mechanisms that regulate energy balance, metabolism, and cardiovascular health
    Cota, Cota
  • The expression of receptors for endocannabinoids in human and rodent skeletal muscle
    Cavuoto, Cavuoto; McAinch, McAinch; Hatzinikolas, Hatzinikolas; Janovska, Janovska; Game, Game; Wittert, Wittert
  • Endocannabinoid‐mediated synaptic plasticity in the CNS
    Chevaleyre, Chevaleyre; Takahashi, Takahashi; Castillo, Castillo
  • Identification of a potent and highly efficacious, yet slowly desensitizing CB1 cannabinoid receptor agonist
    Luk, Luk; Jin, Jin; Zvonok, Zvonok; Lu, Lu; Lin, Lin; Chavkin, Chavkin; Makriyannis, Makriyannis; Mackie, Mackie

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