The δ-opioid receptor positive allosteric modulator BMS 986187 is a G-protein-biased allosteric agonist.
M Alexander StanczykKathryn E LivingstonLouise ChangZara Y WeinbergManojkumar A PuthenveeduJohn R TraynorPublished in: British journal of pharmacology (2019)
This is the first evidence of biased agonism mediated through direct binding to an allosteric site on an opioid receptor, without a ligand at the orthosteric site. Our data suggest that agonists targeting δ-receptors, or indeed any GPCR, through allosteric sites may be a novel way to promote signalling bias and thereby potentially produce a more specific pharmacology than can be observed by activation via the orthosteric site.