Results 31 to 40 of about 71,106 (270)

Dynorphin activation of kappa opioid receptor promotes microglial polarization toward M2 phenotype via TLR4/NF-κB pathway

Cell & Bioscience, 2020
Microglia-mediated neuroinflammation is associated with epilepsy. Switching microglial polarization from the pro-inflammatory M1 phenotype to the anti-inflammatory M2 phenotype represents a novel therapeutic strategy for mitigating epileptogenesis.
Lin Liu, Yingtong Xu, H. Dai, Shan Tan, Xiao Mao, Zhiheng Chen   +5 more
semanticscholar   +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

Mu Opioid Receptor Heterodimers Emerge as Novel Therapeutic Targets: Recent Progress and Future Perspective

Frontiers in Pharmacology, 2020
Opioids are the most effective analgesics used in the clinical management of cancer pain or non-cancer pain. However, chronic opioids therapy can cause many side effects including respiratory depression, nausea, sedation, itch, constipation, analgesic ...
Li Zhang, Jiang-Tao Zhang, Lihua Hang, Tong Liu, Tong Liu   +4 more
doaj   +1 more source

Potential for Kappa-Opioid Receptor Agonists to Engineer Nonaddictive Analgesics: A Narrative Review.

Anesthesia and Analgesia, 2020
A serious adverse effect of prescription opioid analgesics is addiction, both to these analgesics and to illicit drugs like heroin that also activate the µ-opioid receptor (MOR).
Shane W Kaski, Allison N. White, J. Gross, D. Siderovski   +3 more
semanticscholar   +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 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

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

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

Neurons derived from human-induced pluripotent stem cells express mu and kappa opioid receptors

Neural Regeneration Research, 2021
Neuroprotection studies have shown that induced pluripotent stem (iPS) cells have the possibility to transform neuroprotection research. In the present study, iPS cells were generated from human renal epithelial cells and were then differentiated into ...
Zhi-Hai Ju, Xuan Liang, Yao-Yao Ren, Luo-Wa Shu, Yan-Hong Yan, Xu Cui   +5 more
doaj   +1 more source

The Kappa Opioid Receptor: Candidate Pharmacotherapeutic Target for Multiple Sclerosis

Drugs and Drug Candidates, 2023
Multiple sclerosis (MS) afflicts millions of people worldwide. While multiple therapeutics have recently been developed and approved as treatment agents, they are not 100% effective.
Brian Reed, Surya Dutta
doaj   +1 more source