Canna~Fangled Abstracts

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

By May 17, 2017No Comments
Neuropharmacology. 2017 May 17. pii: S0028-3908(17)30230-7. doi: 10.1016/j.neuropharm.2017.05.018.
[Epub ahead of print]

Abstract

pm-2-site-207Cannabinoid 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.

KEYWORDS:

Allosteric modulator; Biased signaling; CB(1); Therapeutic potential

PMID: 28527758

 

DOI: 10.1016/j.neuropharm.2017.05.018

Publication type

Publication type

twin memes II