Modulation of CB1 cannabinoid receptor by allosteric ligands: Pharmacology and therapeutic opportunities

Cannabinoid pharmacology has been intensely studied because of cannabis' pervasive medicinal and non-medicinal uses as well as for the therapeutic potential of cannabinoid-based drugs for the treatment of pain, anxiety, substance abuse, obesity, cancer and neurodegenerative disorders. The identification of allosteric modulators of the cannabinoid receptor 1 (CB$_1$) has given a new direction to the development of cannabinoid-based therapeutics due to the many advantages offered by targeting allosteric site(s). Allosteric receptor modulators hold potential to develop subtype-specific and pathway-specific therapeutics. Here we briefly discuss the first-generation of allosteric modulators of CB$_1$ receptor, their structure-activity relationships, signaling pathways and the allosteric binding site(s) on the CB$_1$ receptor. This article is part of the Special Issue entitled "A New Dawn in Cannabinoid Neurobiology".


Publication Date:
May 17 2017
Date Submitted:
Nov 21 2018
ISSN:
1873-7064
Citation:
Neuropharmacology
124
Note:
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 Record created 2018-11-21, last modified 2019-04-03


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