Fig. 8: Schematic diagram: MOR–CCKBR heteromerization antagonizes MOR activity and morphine analgesia. | Experimental & Molecular Medicine

Fig. 8: Schematic diagram: MOR–CCKBR heteromerization antagonizes MOR activity and morphine analgesia.

From: Heteromerization of μ-opioid receptor and cholecystokinin B receptor through the third transmembrane domain of the μ-opioid receptor contributes to the anti-opioid effects of cholecystokinin octapeptide

Fig. 8

a When MOR is not heteromerized with CCKBR, MOR has high binding affinity with its agonist DAMGO (shown here as an example) and highly activates signal transmissions, such as strong DAMGO-induced ERK1/2 phosphorylation and inhibition of cAMP accumulation. b When MOR directly forms heteromers with CCKBR, the ligand-binding affinity of MOR is decreased, and agonist-induced ERK1/2 phosphorylation and cAMP inhibition are diminished, exhibiting CCK-8 antagonism to morphine analgesia. c Disruption of the heteromerization of MOR–CCKBR with TM3MOR-TAT treatment enhances the activities of the MOR and thus improves the analgesic effects of μ-opioid agonists such as DAMGO or morphine

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