Allosteric modulatorCB(1) receptorHybridMolecular modellingStructure-activity relationshipAllosteric modulation offers an alternate approach to target the cannabinoid type-1 receptor (CB1) for therapeutic benefits. Examination of the two widely studied prototypic CB1 negative allosteric modulators (NAMs) Org...
Cannabidiol (CBD), which has a diverse range of pharmacological actions (Martin et al.2021), including CB1R negative allosteric modulation (Laprairie et al.2015), has been reported to alleviate opioid withdrawal symptoms, (Bhargava1976; Kudrich et al.2022; Scicluna et al.2022). We recently r...
In accordance with the operational model of allosteric modulation, this correlates to positive binding cooperativity (α) and negative functional cooperativity (β). Real-time analysis of ORG on agonist-mediated inhibition of cyclic adenosine monophosphate (cAMP) identified that ORG caused time-dependent...
Allosteric modulator ORG27569 induces a CB1 cannabinoid receptor high affinity agonist binding state, receptor internalization and Gi-independent ERK1/2 activation. J Biol Chem 287:12070-12082.Ahn, K. H.; Mahmoud, M. M.; Kendall, D. A. Allosteric modulator ORG27569 induces CB1 cannabi...
X. Behavioral Effects of the Cannabinoid CB1 Receptor Allosteric Modulator ORG27569 in Rats. Pharmacol. Res. Perspect. 2014, 2 (6), e00069.Ding Y, Qiu Y, Jing L, Thorn DA, Zhang Y, Li JX (2014). Behavioral effects of the cannabinoid CB1 receptor allosteric modulator ORG27569 in rats....
Parameterization of Org27569: an allosteric modulator of the cannabinoid CB1 G protein-coupled receptor. J. Comput. Chem. 32, 2119-2126.Iliff HA, Lynch DL, Kotsikorou E, Reggio PH. Parameterization of Org27569: An allosteric modulator of the cannabinoid CB(1) G protein-coupled receptor. J ...
This document is a correction notice for an article titled "Effects of CB1 receptor negative allosteric modulator Org27569 on oxycodone withdrawal symptoms in mice" published in the journal Psychopharmacology. The correction addresses an error in the original article regarding the incidence of diarrhea ...