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

P Morales, P Goya, N Jagerovic… - Cannabis and …, 2016 - liebertpub.com
In 2005, the first evidence of an allosteric binding site at the CB1R was provided by the
identification of three indoles of the company Organon that were allosteric enhancers of …

Allosteric modulation: an alternate approach targeting the cannabinoid CB1 receptor

T Nguyen, JX Li, BF Thomas, JL Wiley… - Medicinal research …, 2017 - Wiley Online Library
The cannabinoid CB1 receptor is a G protein coupled receptor and plays an important role
in many biological processes and physiological functions. A variety of CB1 receptor agonists …

Negative allosteric modulation of CB1 cannabinoid receptor signaling suppresses opioid-mediated reward

V Iyer, C Rangel-Barajas, TJ Woodward… - Pharmacological …, 2022 - Elsevier
Blockade of cannabinoid type 1 (CB 1)-receptor signaling decreases the rewarding
properties of many drugs of abuse and has been proposed as an anti-addiction strategy …

Novel electrophilic and photoaffinity covalent probes for mapping the cannabinoid 1 receptor allosteric site (s)

PM Kulkarni, AR Kulkarni, A Korde… - Journal of medicinal …, 2016 - ACS Publications
Undesirable side effects associated with orthosteric agonists/antagonists of cannabinoid 1
receptor (CB1R), a tractable target for treating several pathologies affecting humans, have …

Novel analogs of PSNCBAM-1 as allosteric modulators of cannabinoid CB1 receptor

S Bertini, A Chicca, F Gado, C Arena, D Nieri… - Bioorganic & medicinal …, 2017 - Elsevier
In this work, we explored the molecular framework of the known CB1R allosteric modulator
PSNCBAM-1 with the aim to generate new bioactive analogs and to deepen the structure …

Negative allosteric modulation of cannabinoid CB1 receptor signaling suppresses opioid-mediated tolerance and withdrawal without blocking opioid antinociception

V Iyer, SA Saberi, R Pacheco, EF Sizemore… - bioRxiv, 2024 - biorxiv.org
The direct blockade of CB1 cannabinoid receptors produces therapeutic effects as well as
adverse side-effects that limit their clinical potential. CB1 negative allosteric modulators …

Negative allosteric modulation of CB1 cannabinoid receptor signalling decreases intravenous morphine self‐administration and relapse in mice

I Oliva, F Kazi, LN Cantwell, GA Thakur… - Addiction …, 2024 - Wiley Online Library
The endocannabinoid system interacts with the reward system to modulate responsiveness
to natural reinforcers, as well as drugs of abuse. Previous preclinical studies suggested that …

Exploring the benzimidazole ring as a substitution for indole in cannabinoid allosteric modulators

L Hernandez-Folgado, LA Stevenson… - Cannabis and …, 2016 - liebertpub.com
Abstract Introduction and Objectives: The traditional approach to target a particular receptor
is to design compounds that bind to the same site as the endogenous ligand, the so-called …