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

Abstract

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 (CB1) 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 CB1 receptor, their structure-activity relationships, signaling pathways and the allosteric binding site(s) on the CB1 receptor. This article is part of the Special Issue entitled "A New Dawn in Cannabinoid Neurobiology".

• Authors: Leepakshi Khurana, Ken Mackie, Daniele Piomelli, Debra A Kendall
• Journal: Neuropharmacology (Neuropharmacology) Vol. 124 Pg. 3-12 (Sep 15 2017) ISSN: 1873-7064 [Electronic] England
• PMID: 28527758 (Publication Type: Journal Article, Review)
• Copyright: Copyright © 2017 Elsevier Ltd. All rights reserved.

Chemical References

• Cannabinoid Receptor Modulators
• Ligands
• Receptor, Cannabinoid, CB1

Topics

• Allosteric Regulation (drug effects)
• Animals
• Cannabinoid Receptor Modulators (pharmacology)
• Humans
• Ligands
• Receptor, Cannabinoid, CB1 (metabolism)
• Signal Transduction (drug effects)
• Structure-Activity Relationship