Modulation of CB1 Cannabinoid Receptor by Allosteric Ligands: Pharmacology and Therapeutic Opportunities

Overview

Journal Neuropharmacology

Specialties Neurology
Pharmacology

Date 2017 May 22

PMID 28527758

Citations 35

Authors

Leepakshi Khurana

Ken Mackie

Daniele Piomelli

Debra A Kendall

Affiliations

Soon will be listed here.

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

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