Author

John R. Traynor

2 papers indexed here

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Aug 2026

Structure-Function Analysis of the Benzyloxy Moiety of the Delta-Opioid Receptor Positive Modulator BMS-986187: Identification of a Derivative with High Selectivity for the Delta-Opioid Receptor over the Mu-Opioid Receptor In Vitro and In Vivo.

Positive allosteric modulators (PAMs) of the delta-opioid receptor (DOR) enhance endogenous opioid signaling while avoiding the convulsant liability of orthosteric agonists. However, the prototypical DOR-PAM, BMS-986187, also potentiates mu-opioid receptor (MOR) signaling, raising concerns regarding respiratory depress...

Meng-Chu Li, Sherrice Zhang, Alexander J. Powell et al. · Journal of Medicinal Chemist... · 0 citations

Open access Aug 2026

High potency μ-opioid receptor agonists engage sodium-bound receptor states.

The simple 2-state conformational selection model of G protein-coupled receptor activation suggests that, by binding to a high-affinity state, an agonist shifts receptor equilibrium in favor of active state (R∗) conformations that recruit heterotrimeric G proteins over inactive (R) conformations. Agonist binding affini...

Alexander J. Powell, Nicholas W. Griggs, J. Iñiguez-Lluhí et al. · Molecular Pharmacology · 0 citations