Pharmacology of cannabinoid CB1 and CB2 receptors

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Abstract

There are at least two types of cannabinoid receptors, CB1 and CB2, both coupled to G-proteins. CB1 receptors are present in the central nervous system and CB1 and CB2 receptors in certain peripheral tissues. The existence of endogenous cannabinoid receptor agonists has also been demonstrated. These discoveries have led to the development of selective cannabinoid CB1 and CB2 receptor ligands. This review focuses on the classification, binding properties, effector systems and distribution of cannabinoid receptors. It also describes the various cannabinoid receptor agonists and antagonists now available and considers the main in vivo and in vitro bioassay methods that are generally used.

References (207)

  • D.G. Deutsch et al.

    Enzymatic synthesis and degradation of anandamide, a cannabinoid receptor agonist

    Biochem. Pharmacol.

    (1993)
  • S. Diaz et al.

    Suppression of lymphocyte adenosine 3′:5′-cyclic monophosphate (cAMP) by delta-9-tetrahydrocannabinol

    Int. J. Immunopharmacol.

    (1993)
  • V. Di Marzo

    Arachidonic acid and eicosanoids as targets and effectors in second messenger interactions

    Prostaglandins Leukot. Essent. Fatty Acids

    (1995)
  • F. Fan et al.

    Cannabinoid receptor down-regulation without alteration of the inhibitory effect of CP 55,940 on adenylyl cyclase in the cerebellum of CP 55,940-tolerant mice

    Brain Res.

    (1996)
  • C.C. Felder et al.

    Isolation and measurement of the endogenous cannabinoid receptor agonist, anandamide, in brain and peripheral tissues of human and rat

    FEBS Lett.

    (1996)
  • E. Fride et al.

    Pharmacological activity of the cannabinoid receptor agonist, anandamide, a brain constituent

    Eur. J. Pharmacol.

    (1993)
  • Y. Gareau et al.

    Structure activity relationships of tetrahydrocannabinol analogues on human cannabinoid receptors

    Bioorg. Med. Chem. Lett.

    (1996)
  • M. Glass et al.

    Loss of cannabinoid receptors in the substantia nigra in Huntington's disease

    Neuroscience

    (1993)
  • A.J. Hampson et al.

    Anandamide hydroxylation by brain lipoxygenase: metabolite structures and potencies at the cannabinoid receptor

    Biochim. Biophys. Acta

    (1995)
  • D.J. Henry et al.

    Activation of inwardly rectifying potassium channels (GIRK1) by co-expressed rat brain cannabinoid receptors in Xenopus oocytes

    Neurosci. Lett.

    (1995)
  • M. Herkenham et al.

    Neuronal localization of cannabinoid receptors and second messengers in mutant mouse cerebellum

    Brain Res.

    (1991)
  • M. Herkenham et al.

    Neuronal localization of cannabinoid receptors in the basal ganglia of the rat

    Brain Res.

    (1991)
  • C.J. Hillard et al.

    Characterization of the kinetics and distribution of N-arachidonylethanolamine (anandamide) hydrolysis by rat brain

    Biochim. Biophys. Acta

    (1995)
  • B.Y. Ho et al.

    Determination of the cannabinoid receptors in mouse x rat hybridoma NG108-15 cells and rat GH4C1 cells

    Neurosci. Lett.

    (1996)
  • A. Howlett

    Inhibition of neuroblastoma adenylate cyclase by cannabinoid and nantradol compounds

    Life Sci.

    (1984)
  • A.C. Howlett

    Cannabinoid inhibition of adenylate cyclase: relative activity of constituents and metabolites of marihuana

    Neuropharmacology

    (1987)
  • A.C. Howlett et al.

    Stereochemical effects of 11-OH-Δ8-tetrahydro-cannabinol-dimethylheptyl to inhibit adenylate cyclase and bind to the cannabinoid receptor

    Neuropharmacology

    (1990)
  • J.W. Huffman et al.

    Design, synthesis and pharmacology of cannabimimetic indoles

    Bioorg. Med. Chem. Lett.

    (1994)
  • E.M. Jansen et al.

    Distribution of cannabinoid receptors in rat brain determined with aminoalkylindoles

    Brain Res.

    (1992)
  • V. Abadji et al.

    (R)-methanandamide: a chiral novel anandamide possessing higher potency and metabolic stability

    J. Med. Chem.

    (1994)
  • I.B. Adams et al.

    Evaluation of cannabinoid receptor binding and in vivo activities for anandamide analogs

    J. Pharmacol. Exp. Ther.

    (1995)
  • R.L. Barrett et al.

    Pharmacological specificity of Δ9-tetrahydrocannabinol discrimination in rats

    Psychopharmacology

    (1995)
  • M. Bayewitch et al.

    The peripheral cannabinoid receptor: adenylate cyclase inhibition and G protein coupling

    FEBS Lett.

    (1995)
  • M. Bidaut-Russell et al.

    Cannabinoid receptor-regulated cyclic AMP accumulation in the rat striatum

    J. Neurochem.

    (1991)
  • M. Bidaut-Russell et al.

    Cannabinoid receptors and modulation of cyclic AMP accumulation in the rat brain

    J. Neurochem.

    (1990)
  • M. Bouaboula et al.

    Cannabinoid-receptor expression in human leukocytes

    Eur. J. Biochem.

    (1993)
  • M. Bouaboula et al.

    Activation of mitogen-activated protein kinases by stimulation of the central cannabinoid receptor CB1

    Biochem. J.

    (1995)
  • M. Bouaboula et al.

    Signaling pathway associated with stimulation of CB2 peripheral cannabinoid receptor. Involvement of both mitogen-activated protein kinase and induction of Krox-24 expression

    Eur. J. Biochem.

    (1996)
  • L. Caenazzo et al.

    HindIII identifies a two allele DNA polymorphism of the human cannabinoid receptor gene (CNR)

    Nucl. Acids Res.

    (1991)
  • F.M. Casiano et al.

    Putative aminoalkylindoles (AAI) antagonists

    NIDA Res. Monogr.

    (1990)
  • M.P. Caulfield et al.

    Cannabinoid receptor agonists inhibit Ca current in NG108-15 neuroblastoma cells via a pertussis toxin-sensitive mechanism

    Br. J. Pharmacol.

    (1992)
  • A. Chakrabarti et al.

    Cloning and sequencing of a cDNA encoding the mouse brain-type cannabinoid receptor protein

    DNA Seq.-J. Seq. Map.

    (1995)
  • Y.-C. Cheng et al.

    Relationship between the inhibition constant (KI) and the concentration of inhibitor which causes 50 per cent inhibition (IC50) of an enzymatic reaction

    Biochem. Pharmacol

    (1973)
  • D.R. Compton et al.

    Cannabinoid structure-activity relationships: correlation of receptor binding and in vivo activities

    J. Pharmacol. Exp. Ther.

    (1993)
  • D.R. Compton et al.

    In vivo characterization of a specific cannabinoid receptor antagonist (SR141716A): inhibition of Δ9-tetrahydrocannabinol-induced responses and apparent agonist activity

    J. Pharmacol. Exp. Ther.

    (1996)
  • A.A. Coutts et al.

    Effect of cannabinoid agonists and SR141716A on acetylcholine release from the myenteric plexus of the guinea-pig small intestine

    Br. J. Pharmacol.

    (1996)
  • A.A. Coutts et al.

    Evidence that guinea-pig small intestine contains CB1 cannabinoid receptors and possibly also a cannabinoid receptor ligand

    Br. J. Pharmacol.

    (1995)
  • Y. Daaka et al.

    Cannabinoid receptor proteins are increased in Jurkat, human T-cell line after mitogen activation

    J. Pharmacol. Exp. Ther.

    (1996)
  • S.K. Das et al.

    Cannabinoid ligand-receptor signaling in the mouse uterus

    Proc. Natl. Acad. Sci. USA

    (1995)
  • S.A. Deadwyler et al.

    Cannabinoids modulate potassium current in cultured hippocampal neurons

    Recept. Channels

    (1993)
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