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Cannabinoid receptors and their ligands.

Abstract

There are at least two types of cannabinoid receptors, CB(1) and CB(2), both coupled to G proteins. CB(1) receptors exist primarily on central and peripheral neurons, one of their functions being to modulate neurotransmitter release. CB(2) receptors are present mainly on immune cells. Their roles are proving more difficult to establish but seem to include the modulation of cytokine release. Endogenous agonists for cannabinoid receptors (endocannabinoids) have also been discovered, the most important being arachidonoyl ethanolamide (anandamide), 2-arachidonoyl glycerol and 2-arachidonyl glyceryl ether. Other endocannabinoids and cannabinoid receptor types may also exist. Although anandamide can act through CB(1) and CB(2) receptors, it is also a vanilloid receptor agonist and some of its metabolites may possess yet other important modes of action. The discovery of the system of cannabinoid receptors and endocannabinoids that constitutes the "endocannabinoid system" has prompted the development of CB(1)- and CB(2)-selective agonists and antagonists/inverse agonists. CB(1)/CB(2) agonists are already used clinically, as anti-emetics or to stimulate appetite. Potential therapeutic uses of cannabinoid receptor agonists include the management of multiple sclerosis/spinal cord injury, pain, inflammatory disorders, glaucoma, bronchial asthma, vasodilation that accompanies advanced cirrhosis, and cancer. Following their release onto cannabinoid receptors, endocannabinoids are removed from the extracellular space by membrane transport and then degraded by intracellular enzymic hydrolysis. Inhibitors of both these processes have been developed. Such inhibitors have therapeutic potential as animal data suggest that released endocannabinoids mediate reductions both in inflammatory pain and in the spasticity and tremor of multiple sclerosis. So too have CB(1) receptor antagonists, for example for the suppression of appetite and the management of cognitive dysfunction or schizophrenia.

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  • Publisher Full Text
  • Authors+Show Affiliations

    ,

    Department of Biomedical Sciences, University of Aberdeen, Foresterhill, Aberdeen AB25 2ZD, Scotland, UK. rgp@aberdeen.ac.uk

    Source

    MeSH

    Animals
    Cannabinoid Receptor Modulators
    Cannabinoids
    Eicosanoids
    Humans
    Ligands
    Receptors, Cannabinoid
    Receptors, Drug
    Signal Transduction
    Substrate Specificity
    Synaptic Transmission

    Pub Type(s)

    Journal Article
    Research Support, Non-U.S. Gov't
    Research Support, U.S. Gov't, P.H.S.
    Review

    Language

    eng

    PubMed ID

    12052030

    Citation

    Pertwee, R G., and R A. Ross. "Cannabinoid Receptors and Their Ligands." Prostaglandins, Leukotrienes, and Essential Fatty Acids, vol. 66, no. 2-3, 2002, pp. 101-21.
    Pertwee RG, Ross RA. Cannabinoid receptors and their ligands. Prostaglandins Leukot Essent Fatty Acids. 2002;66(2-3):101-21.
    Pertwee, R. G., & Ross, R. A. (2002). Cannabinoid receptors and their ligands. Prostaglandins, Leukotrienes, and Essential Fatty Acids, 66(2-3), pp. 101-21.
    Pertwee RG, Ross RA. Cannabinoid Receptors and Their Ligands. Prostaglandins Leukot Essent Fatty Acids. 2002;66(2-3):101-21. PubMed PMID: 12052030.
    * Article titles in AMA citation format should be in sentence-case
    TY - JOUR T1 - Cannabinoid receptors and their ligands. AU - Pertwee,R G, AU - Ross,R A, PY - 2002/6/8/pubmed PY - 2002/12/7/medline PY - 2002/6/8/entrez SP - 101 EP - 21 JF - Prostaglandins, leukotrienes, and essential fatty acids JO - Prostaglandins Leukot. Essent. Fatty Acids VL - 66 IS - 2-3 N2 - There are at least two types of cannabinoid receptors, CB(1) and CB(2), both coupled to G proteins. CB(1) receptors exist primarily on central and peripheral neurons, one of their functions being to modulate neurotransmitter release. CB(2) receptors are present mainly on immune cells. Their roles are proving more difficult to establish but seem to include the modulation of cytokine release. Endogenous agonists for cannabinoid receptors (endocannabinoids) have also been discovered, the most important being arachidonoyl ethanolamide (anandamide), 2-arachidonoyl glycerol and 2-arachidonyl glyceryl ether. Other endocannabinoids and cannabinoid receptor types may also exist. Although anandamide can act through CB(1) and CB(2) receptors, it is also a vanilloid receptor agonist and some of its metabolites may possess yet other important modes of action. The discovery of the system of cannabinoid receptors and endocannabinoids that constitutes the "endocannabinoid system" has prompted the development of CB(1)- and CB(2)-selective agonists and antagonists/inverse agonists. CB(1)/CB(2) agonists are already used clinically, as anti-emetics or to stimulate appetite. Potential therapeutic uses of cannabinoid receptor agonists include the management of multiple sclerosis/spinal cord injury, pain, inflammatory disorders, glaucoma, bronchial asthma, vasodilation that accompanies advanced cirrhosis, and cancer. Following their release onto cannabinoid receptors, endocannabinoids are removed from the extracellular space by membrane transport and then degraded by intracellular enzymic hydrolysis. Inhibitors of both these processes have been developed. Such inhibitors have therapeutic potential as animal data suggest that released endocannabinoids mediate reductions both in inflammatory pain and in the spasticity and tremor of multiple sclerosis. So too have CB(1) receptor antagonists, for example for the suppression of appetite and the management of cognitive dysfunction or schizophrenia. SN - 0952-3278 UR - https://www.unboundmedicine.com/medline/citation/12052030/Cannabinoid_receptors_and_their_ligands_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0952327801903412 DB - PRIME DP - Unbound Medicine ER -