Results 21 to 30 of about 88,456 (270)

Discovery of Potent Kappa Opioid Receptor Agonists Derived from Akuammicine. [PDF]

J Med Chem
Hennessy MR, Creed SM, Gutridge AM, Rusali LE, Luo D, Sepehri B, Rhoda ES, Villegas JA, van Rijn RM, Riley AP.   +9 more
europepmc   +3 more sources

Opportunities and Challenges for In Silico Drug Discovery at Delta Opioid Receptors

Pharmaceuticals, 2022
The delta opioid receptor is a Gi-protein-coupled receptor (GPCR) with a broad expression pattern both in the central nervous system and the body. The receptor has been investigated as a potential target for a multitude of significant diseases including ...
Yazan J. Meqbil, Richard M. van Rijn
doaj   +1 more source

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

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

The unsolved case of “bone-impairing analgesics”. The endocrine effects of opioids on bone metabolism [PDF]

, 2015
The current literature describes the possible risks for bone fracture in chronic analgesics users. There are three main hypotheses that could explain the increased risk of fracture associated with central analgesics, such as opioids: 1) the increased ...
COLUZZI, FLAMINIA, MATTIA, Consalvo, Pergolizzi, Joseph, Raffa, Robert B   +3 more
core   +6 more sources

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

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

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