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Background and Purpose
G protein‐biased μ opioid receptor agonists have the potential to induce less receptor desensitisation and tolerance than balanced opioids. Here, we investigated if the cyclic endomorphin analogue Tyr‐c[D‐Lys‐Phe‐Tyr‐Gly] (Compound 1) is a G protein‐biased μ agonist and characterised its ability to induce rapid receptor desensitisation in mammalian neurones.
Experimental...
Phosphorylation is considered a key event in the signalling and regulation of the μ opioid receptor (MOPr). Here, we used mass spectroscopy to determine the phosphorylation status of the C‐terminal tail of the rat MOPr expressed in human embryonic kidney 293 (HEK‐293) cells. Under basal conditions, MOPr is phosphorylated on Ser363 and Thr370, while in the presence of morphine or [D‐Ala2, NMe‐Phe4,...
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