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The δ-opioid receptor positive allosteric modulator BMS 986187 is a G-protein-biased allosteric agonist.

M Alexander Stanczyk | Kathryn E Livingston | Louise Chang | Zara Y Weinberg | Manojkumar A Puthenveedu | John R Traynor
British journal of pharmacology | 2019

The δ-opioid receptor is an emerging target for the management of chronic pain and depression. Biased signalling, the preferential activation of one signalling pathway over another downstream of δ-receptors, may generate better therapeutic profiles. BMS 986187 is a positive allosteric modulator of δ-receptors. Here, we ask if BMS 986187 can directly activate the receptor from an allosteric site, without an orthosteric ligand, and if a signalling bias is generated.

Pubmed ID: 30710458

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