Enantiospecific allosteric modulation of cannabinoid 1 receptor

RB Laprairie, PM Kulkarni, JR Deschamps… - ACS chemical …, 2017 - ACS Publications
… , and endogenous CB1R allosteric ligands have been identified. The paradigmatic, first-generation
CB1R allosteric modulators, Org27569 and PSNCBAM-1, paradoxically enhance the …

Allosteric modulation of cannabinoid receptor 1—Current challenges and future opportunities

S Hryhorowicz, M Kaczmarek-Ryś… - International Journal of …, 2019 - mdpi.com
… of cannabinoid receptors. In this paper, we present the latest advances in research on the
CB1R, its allosteric modulation and allosteric … essentials of the cannabinoid 1 receptor- ligand (…

Allosteric Modulators of the CB1 Cannabinoid Receptor: A Structural Update Review

P Morales, P Goya, N Jagerovic… - … and Cannabinoid …, 2016 - liebertpub.com
… a potent allosteric modulator for the cannabinoid receptor 1 (… improve allosteric parameters
for the cannabinoid receptor 1 (… Allosteric modulators of the cannabinoid 1 receptor. Patent. …

Cannabidiol is a negative allosteric modulator of the cannabinoid CB1 receptor

RB Laprairie, AM Bagher, MEM Kelly… - British journal of …, 2015 - Wiley Online Library
… In this study, the primary effect of CBD at CB 1 receptors was negative allosteric
modulation at concentrations below 1 μM. The studies by Price et al. (2005) and Baillie et al. …

Discovery of a biased allosteric modulator for cannabinoid 1 receptor: preclinical anti-glaucoma efficacy

S Garai, LM Leo, AM Szczesniak… - Journal of Medicinal …, 2021 - ACS Publications
… of novel CB1R allosteric modulators as … 1), exhibiting enantiospecific allosteric CB1R
modulation. As an ago-PAM, the resolved R-(+)-enantiomer (GAT228, 7) is a partial allosteric

CB1 allosteric modulators and their therapeutic potential in CNS disorders

CA Mielnik, VM Lam, RA Ross - Progress in Neuro-Psychopharmacology …, 2021 - Elsevier
… vitro and in vivo pharmacology of CB 1 allosteric modulators. We will discuss the challenges
… It has been speculated that pregnenolone may show probe dependence (ie THC versus 2-…

Allosteric modulation: an alternate approach targeting the cannabinoid CB1 receptor

T Nguyen, JX Li, BF Thomas, JL Wiley… - Medicinal research …, 2017 - Wiley Online Library
… This review details the complex pharmacological profiles of these allosteric modulators, …
reported CB1 allosteric modulators. The ultimate development of CB1 receptor allosteric ligands …

Structure of an allosteric modulator bound to the CB1 cannabinoid receptor

Z Shao, W Yan, K Chapman, K Ramesh… - Nature chemical …, 2019 - nature.com
… To gain a better molecular understanding of the interaction and mechanism of these allosteric
modulators, we determined the crystal structure of CB1 with the agonists CP55940 and …

Allosteric modulators of cannabinoid receptor 1: developing compounds for improved specificity

R Dopart, D Lu, AH Lichtman… - Drug metabolism …, 2018 - Taylor & Francis
… In this review, we summarize the concept of allosteric modulation and focus … allosteric
modulators, ORG27569 and PSNCBAM-1 and their derivatives, and a few other recent modulators. …

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

L Khurana, K Mackie, D Piomelli, DA Kendall - Neuropharmacology, 2017 - Elsevier
… -generation of allosteric modulators of CB 1 receptor, their structure-… and the allosteric binding
site(s) on the CB 1 receptor. … on the allosteric modulation of the CB 1 receptor and gives a …