Mu Opioid Receptor Positive Allosteric Modulator BMS-986122 Confers Agonist-Dependent G Protein Subtype Signaling Bias.

ABSTRACT: The mu opioid receptor (MOR) is a G protein-coupled receptor (GPCR) and is responsible for the effects of all medically used opioids. Most opioids activate all inhibitory Gαi/o/z proteins through MOR, initiating signaling events that culminate in a variety of physiological effects such as analgesia, euphoria, and respiratory depression. Gaining a better understanding of how the chemical structure of opioids influences the functional activation profiles of G protein subtypes by MOR is critical for disentangling the multitude of opioid effects and the development of safer analgesics. A recent development in opioid pharmacology has been the discovery of positive allosteric modulators (PAMs) for opioid receptors, such as BMS-986122, which act at the MOR to increase the potency of full agonists

SUBMITTER: Grieble GM 

PROVIDER: S-EPMC12138978 | biostudies-literature | 2025 Jun

REPOSITORIES: biostudies-literature