Non-peptidergic OP4 receptor agonist inhibits morphine antinociception but does not influence morphine dependence

J Kotlinska, J Wichmann, P Rafalski, S Talarek… - …, 2003 - journals.lww.com
The non-peptidergic opioid receptor-like 1 (ORL1, OP4) receptor ligand, Ro 64-6198 {(1S,
3aS)-8-(2, 3, 3a, 4, 5, 6-hexahydro-1H-phenalen-1-yl)-1-phenyl-1, 3, 8-triaza-spiro [4, 5] …

In vivo characterization of MMP-2200, a mixed δ/μ opioid agonist, in mice

JJ Lowery, TJ Raymond, D Giuvelis, JM Bidlack… - Journal of pharmacology …, 2011 - ASPET
We have previously reported the chemistry and antinociceptive properties of a series of
glycosylated enkephalin analogs (glycopeptides) exhibiting approximately equal affinity and …

Functional antagonism of μ-, δ-and κ-opioid antinociception by orphanin FQ

JS Mogil, JE Grisel, G Zhangs, JK Belknap… - Neuroscience …, 1996 - Elsevier
Orphanin FQ (OFQ) is the recently isolated endogenous ligand for the orphan opioid-like
receptor, LC132. Initial reports suggested that OFQ increased pain sensitivity when injected …

Comparison of the in vitro efficacy of μ, δ, κ and ORL1 receptor agonists and non-selective opioid agonists in dog brain membranes

PA Lester, JR Traynor - Brain research, 2006 - Elsevier
Morphine and related opioid agonists are frequently used in dogs for their analgesic
properties, their sedative effects and as adjuncts to anesthesia. Such compounds may be …

Buprenorphine and related orvinols

SM Husbands - Research and development of opioid-related …, 2013 - ACS Publications
The orvinols, including buprenorphine, emerged from research carried out by Reckitt and
Colman in the 1960s and 1970s. Regulatory approval of buprenorphine for the treatment of …

Bivalent Ligands That Target μ Opioid (MOP) and Cannabinoid1 (CB1) Receptors Are Potent Analgesics Devoid of Tolerance

M Le Naour, E Akgün, A Yekkirala… - Journal of medicinal …, 2013 - ACS Publications
Given that μ opioid (MOP) and canabinoid (CB1) receptors are colocalized in various
regions of the central nervous system and have been reported to associate as heteromer …

Abuse potential of biased mu opioid receptor agonists

SS Negus, KB Freeman - Trends in pharmacological sciences, 2018 - cell.com
G protein-biased mu opioid receptor (GPB-MOR) agonists constitute an emerging class of
opioid analgesics. The first-in-class GPB-MOR agonist TRV130 (oliceridine) produces …

[HTML][HTML] IUPHAR review: Recent progress in the development of Mu opioid receptor modulators to treat opioid use disorders

PP Pagare, R Flammia, Y Zhang - Pharmacological Research, 2024 - Elsevier
Abstract Opioid Use Disorder (OUD) can be described as intense preoccupation with using
or obtaining opioids despite the negative consequences associated with their use. As the …

[HTML][HTML] Alternatively spliced mu opioid receptor C termini impact the diverse actions of morphine

J Xu, Z Lu, A Narayan, VP Le Rouzic… - The Journal of …, 2017 - Am Soc Clin Investig
Extensive 3′ alternative splicing of the mu opioid receptor gene OPRM1 creates multiple C-
terminal splice variants. However, their behavioral relevance remains unknown. The present …

Biased agonism of the μ-opioid receptor by TRV130 increases analgesia and reduces on-target adverse effects versus morphine: a randomized, double-blind …

DG Soergel, RA Subach, N Burnham, MW Lark… - Pain, 2014 - journals.lww.com
An experimental medicine comparison of the novel biased ligand TRV130 to morphine
reveals that selective signaling at the mu opioid receptor may improve opioid therapeutic …