Bifunctional peptide-based opioid agonist–nociceptin antagonist ligands for dual treatment of acute and neuropathic pain

Bifunctional peptide-based opioid agonist–nociceptin antagonist ligands for dual treatment of acute and neuropathic pain

K Guillemyn, J Starnowska, C Lagard… - Journal of medicinal …, 2016 - ACS Publications

Herein, the opioid pharmacophore H-Dmt-d-Arg-Aba-β-Ala-NH2 (7) was linked to peptide 
ligands for the nociceptin receptor. Combination of 7 and NOP ligands (eg, H-Arg-Tyr-Tyr-
Arg-Ile-Lys-NH2) led to binding affinities in the low nanomolar domain. In vitro, the hybrids …

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