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Targeting the endocannabinoid system with cannabinoid receptor agonists: pharmacological strategies and therapeutic possibilities.

Abstract

Human tissues express cannabinoid CB(1) and CB(2) receptors that can be activated by endogenously released 'endocannabinoids' or exogenously administered compounds in a manner that reduces the symptoms or opposes the underlying causes of several disorders in need of effective therapy. Three medicines that activate cannabinoid CB(1)/CB(2) receptors are now in the clinic: Cesamet (nabilone), Marinol (dronabinol; Δ(9)-tetrahydrocannabinol (Δ(9)-THC)) and Sativex (Δ(9)-THC with cannabidiol). These can be prescribed for the amelioration of chemotherapy-induced nausea and vomiting (Cesamet and Marinol), stimulation of appetite (Marinol) and symptomatic relief of cancer pain and/or management of neuropathic pain and spasticity in adults with multiple sclerosis (Sativex). This review mentions several possible additional therapeutic targets for cannabinoid receptor agonists. These include other kinds of pain, epilepsy, anxiety, depression, Parkinson's and Huntington's diseases, amyotrophic lateral sclerosis, stroke, cancer, drug dependence, glaucoma, autoimmune uveitis, osteoporosis, sepsis, and hepatic, renal, intestinal and cardiovascular disorders. It also describes potential strategies for improving the efficacy and/or benefit-to-risk ratio of these agonists in the clinic. These are strategies that involve (i) targeting cannabinoid receptors located outside the blood-brain barrier, (ii) targeting cannabinoid receptors expressed by a particular tissue, (iii) targeting upregulated cannabinoid receptors, (iv) selectively targeting cannabinoid CB(2) receptors, and/or (v) adjunctive 'multi-targeting'.

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  • Authors+Show Affiliations

    School of Medical Sciences, Institute of Medical Sciences, University of Aberdeen, Foresterhill, Aberdeen, UK. rgp@abdn.ac.uk

    Source

    MeSH

    Analgesics
    Animals
    Blood-Brain Barrier
    Cannabinoid Receptor Agonists
    Cardiovascular Diseases
    Clinical Trials as Topic
    Dronabinol
    Drug Discovery
    Endocannabinoids
    Humans
    Neurodegenerative Diseases
    Pain
    Receptor, Cannabinoid, CB1
    Receptor, Cannabinoid, CB2
    Risk Assessment

    Pub Type(s)

    Journal Article
    Review

    Language

    eng

    PubMed ID

    23108552

    Citation

    Pertwee, Roger G.. "Targeting the Endocannabinoid System With Cannabinoid Receptor Agonists: Pharmacological Strategies and Therapeutic Possibilities." Philosophical Transactions of the Royal Society of London. Series B, Biological Sciences, vol. 367, no. 1607, 2012, pp. 3353-63.
    Pertwee RG. Targeting the endocannabinoid system with cannabinoid receptor agonists: pharmacological strategies and therapeutic possibilities. Philos Trans R Soc Lond, B, Biol Sci. 2012;367(1607):3353-63.
    Pertwee, R. G. (2012). Targeting the endocannabinoid system with cannabinoid receptor agonists: pharmacological strategies and therapeutic possibilities. Philosophical Transactions of the Royal Society of London. Series B, Biological Sciences, 367(1607), pp. 3353-63. doi:10.1098/rstb.2011.0381.
    Pertwee RG. Targeting the Endocannabinoid System With Cannabinoid Receptor Agonists: Pharmacological Strategies and Therapeutic Possibilities. Philos Trans R Soc Lond, B, Biol Sci. 2012 Dec 5;367(1607):3353-63. PubMed PMID: 23108552.
    * Article titles in AMA citation format should be in sentence-case
    TY - JOUR T1 - Targeting the endocannabinoid system with cannabinoid receptor agonists: pharmacological strategies and therapeutic possibilities. A1 - Pertwee,Roger G, PY - 2012/10/31/entrez PY - 2012/10/31/pubmed PY - 2013/4/9/medline SP - 3353 EP - 63 JF - Philosophical transactions of the Royal Society of London. Series B, Biological sciences JO - Philos. Trans. R. Soc. Lond., B, Biol. Sci. VL - 367 IS - 1607 N2 - Human tissues express cannabinoid CB(1) and CB(2) receptors that can be activated by endogenously released 'endocannabinoids' or exogenously administered compounds in a manner that reduces the symptoms or opposes the underlying causes of several disorders in need of effective therapy. Three medicines that activate cannabinoid CB(1)/CB(2) receptors are now in the clinic: Cesamet (nabilone), Marinol (dronabinol; Δ(9)-tetrahydrocannabinol (Δ(9)-THC)) and Sativex (Δ(9)-THC with cannabidiol). These can be prescribed for the amelioration of chemotherapy-induced nausea and vomiting (Cesamet and Marinol), stimulation of appetite (Marinol) and symptomatic relief of cancer pain and/or management of neuropathic pain and spasticity in adults with multiple sclerosis (Sativex). This review mentions several possible additional therapeutic targets for cannabinoid receptor agonists. These include other kinds of pain, epilepsy, anxiety, depression, Parkinson's and Huntington's diseases, amyotrophic lateral sclerosis, stroke, cancer, drug dependence, glaucoma, autoimmune uveitis, osteoporosis, sepsis, and hepatic, renal, intestinal and cardiovascular disorders. It also describes potential strategies for improving the efficacy and/or benefit-to-risk ratio of these agonists in the clinic. These are strategies that involve (i) targeting cannabinoid receptors located outside the blood-brain barrier, (ii) targeting cannabinoid receptors expressed by a particular tissue, (iii) targeting upregulated cannabinoid receptors, (iv) selectively targeting cannabinoid CB(2) receptors, and/or (v) adjunctive 'multi-targeting'. SN - 1471-2970 UR - https://www.unboundmedicine.com/medline/citation/23108552/Targeting_the_endocannabinoid_system_with_cannabinoid_receptor_agonists:_pharmacological_strategies_and_therapeutic_possibilities_ L2 - https://royalsocietypublishing.org/doi/full/10.1098/rstb.2011.0381?url_ver=Z39.88-2003&rfr_id=ori:rid:crossref.org&rfr_dat=cr_pub=pubmed DB - PRIME DP - Unbound Medicine ER -