Abstract
The cannabinoid receptors CB1 and CB2 are family A, G-protein Coupled Receptors that mediate the effects of cannabinoids, a class of compounds that are so named because the first members were isolates of the cannabis plant. In recent history, there has been much anecdotal evidence that the potent and diverse physiological responses produced by these compounds can be turned to therapeutic benefit for a wide variety of maladies. The remarkable abundance of cannabinoid receptors and the discovery of several endogenous ligands along with enzyme and transporter proteins for which they are substrates, suggests that an endogenous cannabinoid neuromodulatory system is an important mediator of biological function. For these reasons CB1 and CB2 receptors are attractive targets for the design of therapeutic ligands. The action of these receptors, however, may also be modulated by manipulating the enzymes and membrane transporters that regulate the endogenous ligands. Despite the range of physiological processes and activities that are mediated by cannabinoid receptors, it is clear that it is possible to produce ligands that result in differential responses. In this paper, we review the pharmacophoric elements that lead to these differential responses and in order to discuss them in context we present an overview of structural aspects governing cannabinoid receptor function, the cannabinergic system and its physiological functions.
Keywords: Cannabinoid, pharmacophore, aminoalkylindoles, diarylpyrazoles, endocannabinoids, receptor, selectivity, agonist, antagonist
Current Pharmaceutical Design
Title: Cannabinoid Receptors as Therapeutic Targets
Volume: 12 Issue: 14
Author(s): Alexandros Makriyannis, Spyros P. Nikas, Ganesh A. Thakur and Spiro Pavlopoulos
Affiliation:
Keywords: Cannabinoid, pharmacophore, aminoalkylindoles, diarylpyrazoles, endocannabinoids, receptor, selectivity, agonist, antagonist
Abstract: The cannabinoid receptors CB1 and CB2 are family A, G-protein Coupled Receptors that mediate the effects of cannabinoids, a class of compounds that are so named because the first members were isolates of the cannabis plant. In recent history, there has been much anecdotal evidence that the potent and diverse physiological responses produced by these compounds can be turned to therapeutic benefit for a wide variety of maladies. The remarkable abundance of cannabinoid receptors and the discovery of several endogenous ligands along with enzyme and transporter proteins for which they are substrates, suggests that an endogenous cannabinoid neuromodulatory system is an important mediator of biological function. For these reasons CB1 and CB2 receptors are attractive targets for the design of therapeutic ligands. The action of these receptors, however, may also be modulated by manipulating the enzymes and membrane transporters that regulate the endogenous ligands. Despite the range of physiological processes and activities that are mediated by cannabinoid receptors, it is clear that it is possible to produce ligands that result in differential responses. In this paper, we review the pharmacophoric elements that lead to these differential responses and in order to discuss them in context we present an overview of structural aspects governing cannabinoid receptor function, the cannabinergic system and its physiological functions.
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Cite this article as:
Makriyannis Alexandros, Nikas P. Spyros, Thakur A. Ganesh and Pavlopoulos Spiro, Cannabinoid Receptors as Therapeutic Targets, Current Pharmaceutical Design 2006; 12 (14) . https://dx.doi.org/10.2174/138161206776873743
DOI https://dx.doi.org/10.2174/138161206776873743 |
Print ISSN 1381-6128 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4286 |
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