Minireview on CB1 Receptor Allosteric Modulation
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Abstract
The endocannabinoid system (ECS) constitutes a multifaceted neuromodulatory network orchestrating a spectrum of physiological processes through the interplay of endogenous ligands, metabolic enzymes, and cannabinoid receptors (CB1R and CB2R). Among these, CB1R—an abundantly expressed G protein-coupled receptor (GPCR)—exerts pivotal influence on neurological, metabolic, and nociceptive functions. Therapeutic exploitation of CB1R, however, has historically been constrained by the neuropsychiatric liabilities associated with orthosteric ligands. In this context, allosteric modulation, targeting receptor sites topographically distinct from the orthosteric pocket, has emerged as a strategy capable of conferring both subtype selectivity and enhanced safety. Herein, we synthesize recent progress in the discovery, structural characterization, and pharmacological evaluation of CB1R allosteric modulators, emphasizing mechanistic heterogeneity, therapeutic implications, and the evolving paradigms for rational drug design.
Keywords:
CB1 receptor Allosteric modulation Endocannabinoid system Positive allosteric modulators Negative allosteric modulators GPCRFull Article
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Copyright © 2026 by the author(s). This is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY 4.0) license, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
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How to Cite
Ming Yee, B., Yi Ying, P., Chek Kouk, K. (2026). Minireview on CB1 Receptor Allosteric Modulation. BiomedicaSphere, 1(1), 19-28. https://doi.org/10.59324/bmsj.2026.1(1).03