کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
2565057 1128045 2012 12 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Cannabinoid receptors: nomenclature and pharmacological principles
موضوعات مرتبط
علوم زیستی و بیوفناوری علم عصب شناسی روانپزشکی بیولوژیکی
پیش نمایش صفحه اول مقاله
Cannabinoid receptors: nomenclature and pharmacological principles
چکیده انگلیسی

The CB1 and CB2 cannabinoid receptors are members of the G protein-coupled receptor (GPCR) family that are pharmacologically well defined. However, the discovery of additional sites of action for endocannabinoids as well as synthetic cannabinoid compounds suggests the existence of additional cannabinoid receptors. Here we review this evidence, as well as the current nomenclature for classifying a target as a cannabinoid receptor. Basic pharmacological definitions, principles and experimental conditions are discussed in order to place in context the mechanisms underlying cannabinoid receptor activation. Constitutive (agonist-independent) activity is observed with the overexpression of many GPCRs, including cannabinoid receptors. Allosteric modulators can alter the pharmacological responses of cannabinoid receptors. The complex molecular architecture of each of the cannabinoid receptors allows for a single receptor to recognize multiple classes of compounds and produce an array of distinct downstream effects. Natural polymorphisms and alternative splice variants may also contribute to their pharmacological diversity. As our knowledge of the distinct differences grows, we may be able to target select receptor conformations and their corresponding pharmacological responses. Importantly, the basic biology of the endocannabinoid system will continue to be revealed by ongoing investigations.


► New information on cannabinoid receptor nomenclature and pharmacological principles.
► The potential classification of GPR18 and GPR55 as cannabinoid receptor subtypes.
► Distinction among agonists, antagonists, inverse agonists and allosteric modulators.
► Practical information on binding and signal transduction for cannabinoid receptors.
► Relevance of CB1 and CB2 mutations, splice variants and polymorphisms to physiology.

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Progress in Neuro-Psychopharmacology and Biological Psychiatry - Volume 38, Issue 1, 2 July 2012, Pages 4–15
نویسندگان
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