Results 21 to 30 of about 1,463,708 (228)

Functional bias of morphine and oliceridine under conditions of minor injury

Molecular Pain, 2021
Recent reports suggest pain from surgical injury may influence the risks associated with exposure to opioids. In mice, hind-paw incision attenuates morphine-primed reinstatement due to kappa opioid receptor activation by dynorphin.
Chinwe Nwaneshiudu, Xiao-Yu Shi, Peyman Sahbaie, J David Clark   +3 more
doaj   +1 more source

Itching-like behavior: A common effect of the kappa opioid receptor antagonist 5′-guanidinonaltrindole and the biased kappa opioid receptor agonist 6′-guanidinonaltrindole in mice

Medicine in Drug Discovery, 2021
Activation of the KOR produces antipruritic effects. In this study, we investigated three KOR ligands for their abilities to cause scratching behaviors in mice, an animal model of itch, and the involvement of the KOR in these behaviors.
Alan Cowan, Lee-Yuan Liu-Chen, Saadet Inan   +2 more
doaj   +1 more source

Controlling opioid receptor functional selectivity by targeting distinct subpockets of the orthosteric site

eLife, 2021
Controlling receptor functional selectivity profiles for opioid receptors is a promising approach for discovering safer analgesics; however, the structural determinants conferring functional selectivity are not well understood.
Rajendra Uprety, Tao Che, Saheem A Zaidi, Steven G Grinnell, Balázs R Varga, Abdelfattah Faouzi, Samuel T Slocum, Abdullah Allaoa, András Varadi, Melissa Nelson, Sarah M Bernhard, Elizaveta Kulko, Valerie Le Rouzic, Shainnel O Eans, Chloe A Simons, Amanda Hunkele, Joan Subrath, Ying Xian Pan, Jonathan A Javitch, Jay P McLaughlin, Bryan L Roth, Gavril W Pasternak, Vsevolod Katritch, Susruta Majumdar   +23 more
doaj   +1 more source

Opioid mediated activity and expression of mu and delta opioid receptors in isolated human term non-laboring myometrium [PDF]

, 2013
The existence of opioid receptors in mammalian myometrial tissue is now widely accepted. Previously enkephalin degrading enzymes have been shown to be elevated in pregnant rat uterus and a met-enkephalin analogue has been shown to alter spontaneous ...
McMorrow, Jason P., Carey, Michael F., Campion, Deirdre P., O\u27Connor, J. J., Fanning, Rebecca A., O'Connor, J. J.   +5 more
core   +1 more source

In vitro and in vivo Pharmacological Activities of 14-O-Phenylpropyloxymorphone, a Potent Mixed Mu/Delta/Kappa-Opioid Receptor Agonist With Reduced Constipation in Mice

Frontiers in Pharmacology, 2018
Pain, particularly chronic pain, is still an unsolved medical condition. Central goals in pain control are to provide analgesia of adequate efficacy and to reduce complications associated with the currently available drugs.
Roberta Lattanzi, Silvia Rief, Helmut Schmidhammer, Lucia Negri, Mariana Spetea   +4 more
doaj   +1 more source

Effects of dezocine on morphine tolerance and opioid receptor expression in a rat model of bone cancer pain

BMC Cancer, 2021
Background Clinically, the coadministration of opioids to enhance antinociception and decrease tolerance has attracted increasing research attention. We investigated the effects of dezocine, a mu- and kappa-opioid receptor agonist/antagonist, on morphine
Lin-xin Wu, Yan-peng Dong, Qian-mei Zhu, Bo Zhang, Bo-lun Ai, Tao Yan, Guo-hua Zhang, Li Sun   +7 more
doaj   +1 more source

Opioid Receptor-Mediated Regulation of Neurotransmission in the Brain

Frontiers in Molecular Neuroscience, 2022
Opioids mediate their effects via opioid receptors: mu, delta, and kappa. At the neuronal level, opioid receptors are generally inhibitory, presynaptically reducing neurotransmitter release and postsynaptically hyperpolarizing neurons.
Kaitlin C. Reeves, Kaitlin C. Reeves, Nikhil Shah, Nikhil Shah, Braulio Muñoz, Brady K. Atwood, Brady K. Atwood   +6 more
doaj   +1 more source

Pharmacological profiles of opioid ligands at Kappa opioid receptors [PDF]

BMC Pharmacology, 2006
Abstract Background The aim of the present study was to describe the activity of a set of opioid drugs, including partial agonists, in a human embryonic kidney cell system stably expressing only the mouse κ-opioid receptors.
Gharagozlou, Parham, Hashemi, Ezzat, DeLorey, Timothy M, Clark, J David, Lameh, Jelveh   +4 more
openaire   +2 more sources

Alterations in Cortical and Basal Ganglia Levels of Opioid Receptor Binding in a Rat Model of l-DOPA-Induced Dyskinesia

Neurobiology of Disease, 2001
Opioid receptor-binding autoradiography was used as a way to map sites of altered opioid transmission in a rat model of l-DOPA-induced dyskinesia. Rats with unilateral 6-hydroxydopamine lesions of the nigrostriatal pathways sustained a 3-week treatment ...
P.A. Johansson, M. Andersson, K.E. Andersson, M.A. Cenci   +3 more
doaj   +1 more source

Inhibition of activity of GABA transporter GAT1 by δ-opioid receptor [PDF]

, 2012
Analgesia is a well-documented effect of acupuncture. A critical role in pain sensation plays the nervous system, including the GABAergic system and opioid receptor (OR) activation.
Fucke, Thomas, Schwarz, Wolfgang, Xu, Nanjie, Pu, Lu, Pei, Gang, Gu, Quanbao, Xia, Peng, Ren, Shuanglai   +7 more
core   +1 more source