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Molecular Biology of Cannabinoid Receptors

  • Chapter
Cannabinoids

Part of the book series: Handbook of Experimental Pharmacology ((HEP,volume 168))

Abstract

To date, two cannabinoid receptors have been isolated by molecular cloning. The CB1 and CB2 cannabinoid receptors are members of the G protein-coupled receptor family. There is also evidence for additional cannabinoid receptor subtypes. The CB1 and CB2 receptors recognize endogenous and exogenous cannabinoid compounds, which fall into five structurally diverse classes. Mutagenesis and molecular modeling studies have identified several key amino acid residues involved in the selective recognition of these ligands. Numerous residues involved in receptor activation have been elucidated. Regions of the CB1 receptor mediating desensitization and internalization have also been discovered. The known genetic structures of the CB1 and CB2 receptors indicate polymorphisms and multiple exons that may be involved in tissue and species-specific regulation of these genes. The cannabinoid receptors are regulated during chronic agonist exposure, and gene expression is altered in disease states. There is a complex molecular architecture of the cannabinoid receptors that allows a single receptor to recognize multiple classes of compounds and produce an array of distinct downstream effects.

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  1. Forbes Norris MDA/ALS Research, California Pacific Medical Center, 2351 Clay St 416, San Francisco, CA, 94115, USA

    M. E. Abood

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  1. School of Medical Sciences, Institute of Medical Science, University of Aberdeen, Foresterhill, Aberdeen, AB25 2ZD, Scotland, UK

    Roger G. Pertwee

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Abood, M.E. (2005). Molecular Biology of Cannabinoid Receptors. In: Pertwee, R.G. (eds) Cannabinoids. Handbook of Experimental Pharmacology, vol 168. Springer, Berlin, Heidelberg. https://doi.org/10.1007/3-540-26573-2_3

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