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

Background and Purpose 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 al...

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Veröffentlicht in:	British journal of pharmacology 2019-06, Vol.176 (11), p.1649-1663
Hauptverfasser:	Stanczyk, M. Alexander, Livingston, Kathryn E., Chang, Louise, Weinberg, Zara Y., Puthenveedu, Manojkumar A., Traynor, John R.
Format:	Artikel
Sprache:	eng
Schlagworte:	Activation Agonists Allosteric properties Allosteric Site Animals Arrestin Bias Cell lines CHO Cells Chronic pain Cricetulus Desensitization G protein-coupled receptors GTP-Binding Proteins - agonists GTP-Binding Proteins - metabolism Guanosine 5'-O-(3-Thiotriphosphate) - metabolism HEK293 Cells Humans Internalization Ligands Male Mice Narcotics Opioid receptors Pharmacology Phosphorylation Proteins Receptors, Opioid, delta - metabolism Research Paper Research Papers Signal transduction Xanthones - pharmacology
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