Pharmacological characterization of cebranopadol a novel analgesic acting as mixed nociceptin/orphanin FQ and opioid receptor agonist

A Rizzi, MC Cerlesi, C Ruzza… - Pharmacology …, 2016 - Wiley Online Library
The aim of the study was to investigate the in vitro and in vivo pharmacological profile of
cebranopadol, a novel agonist for opioid and nociceptin/orphanin FQ (N/OFQ) receptors …

Synthesis and evaluation of a novel bivalent selective antagonist for the mu-delta opioid receptor heterodimer that reduces morphine withdrawal in mice

KM Olson, A Keresztes, JK Tashiro… - Journal of medicinal …, 2018 - ACS Publications
A major limitation in the study of the mu-delta opioid receptor heterodimer (MDOR) is that
few selective pharmacological tools exist and no heteromer-selective antagonists. We thus …

[HTML][HTML] Atypical opioid receptors: unconventional biology and therapeutic opportunities

CB Palmer, M Meyrath, M Canals, E Kostenis… - Pharmacology & …, 2022 - Elsevier
Endogenous opioid peptides and prescription opioid drugs modulate pain, anxiety and
stress by activating four opioid receptors, namely μ (mu, MOP), δ (delta, DOP), κ (kappa …

Preclinical testing of nalfurafine as an opioid-sparing adjuvant that potentiates analgesia by the mu opioid receptor-targeting agonist morphine

SW Kaski, AN White, JD Gross, KR Trexler, K Wix… - … of Pharmacology and …, 2019 - ASPET
Mu opioid receptor (MOR)-targeting analgesics are efficacious pain treatments, but
notorious for their abuse potential. In preclinical animal models, coadministration of …

Peptide and nonpeptide ligands for the nociceptin/orphanin FQ receptor ORL1: research tools and potential therapeutic agents

N Zaveri - Life sciences, 2003 - Elsevier
The 17-amino acid neuropeptide nociceptin/Orphanin FQ (N/OFQ) was recently identified as
the endogenous ligand for the opioid receptor-like (ORL1) receptor, a fourth member of the …

Discovery of Spiro[cyclohexane-dihydropyrano[3,4-b]indole]-amines as Potent NOP and Opioid Receptor Agonists

S Schunk, K Linz, S Frormann, C Hinze… - ACS medicinal …, 2014 - ACS Publications
We report the discovery of spiro [cyclohexane-pyrano [3, 4-b] indole]-amines, as functional
nociceptin/orphanin FQ peptide (NOP) and opioid receptor agonists with strong efficacy in …

Opioid activity profiles indicate similarities between the nociceptin/orphanin FQ and opioid receptors

JE Hawkinson, M Acosta-Burruel, SA Espitia - European journal of …, 2000 - Elsevier
Nociceptin (orphanin FQ) is the recently discovered peptide agonist for the orphan receptor
opioid receptor-like 1 (ORL1). Despite the high sequence homology between ORL1 and the …

Distribution of functional opioid receptors in human dorsal root ganglion neurons

JK Moy, JE Hartung, MG Duque, R Friedman… - Pain, 2020 - journals.lww.com
Preclinical evidence has highlighted the importance of the m-opioid peptide (MOP) receptor
on primary afferents for both the analgesic actions of MOP receptor agonists, as well as the …

Characterization of opiates, neuroleptics, and synthetic analogs at ORL1 and opioid receptors

N Zaveri, WE Polgar, CM Olsen, AB Kelson… - European journal of …, 2001 - Elsevier
Nociceptin/orphanin FQ (N/OFQ) was recently identified as the endogenous ligand for the
opioid-receptor like (ORL1) receptor. Although the ORL1 receptor shows sequence …

[HTML][HTML] MOP and NOP receptor interaction: Studies with a dual expression system and bivalent peptide ligands

MF Bird, J McDonald, B Horley, JP O'Doherty, B Fraser… - Plos one, 2022 - journals.plos.org
Opioids targeting mu; μ (MOP) receptors produce analgesia in the peri-operative period and
palliative care. They also produce side effects including respiratory depression …