Results 1 to 10 of about 688,936 (303)

Molecular mechanism of allosteric modulation of opioid receptors

Signal Transduction and Targeted Therapy
Opioid analgesics provide potent pain relief but are limited by severe adverse effects, tolerance, and interindividual genetic variability in response. Poly-pharmacology and allosteric modulation of opioid receptors offer promising strategies to enhance ...
Heli Wang, Zhuang Miao, Chang Zhao, Hong Fu, Xiaowen Tian, Xinlei Liu, Lei Wang, Yuan Liu, Xingyu Liu, Xihao Yong, Lantian Su, Wei Yan, Lin Cheng, Renjie Chai, Zhenhua Shao, Bowen Ke   +15 more
doaj   +1 more source

Common Mechanisms Underlying Opioid Tolerance and Dependence and Neuropathic Pain: Role of Metabotropic Glutamate Receptors

Pain Research and Management, 2000
It has been suggested that opioid tolerance and dependence share common mechanisms with neuropathic pain. This short review deals with the role of glutamate and glutamate receptors in opioid tolerance and dependence, and neuropathic pain.
Marian E Fundytus
doaj   +1 more source

Amelioration of injury-induced tissue acidosis by a nonsteroidal analgesic attenuates antinociceptive effects of the pH-dependent opioid agonist NFEPP

Scientific Reports, 2022
Opioid agonists are powerful drugs for managing pain. However, their central side effects are limiting their use and drugs with similar potency, but a lower risk profile are needed. (±)-N-(3-fluoro-1-phenethylpiperidine-4-yl)-N-phenylpropionamide (NFEPP)
Melih Ö. Celik, Roger Negrete, Riccardo Di Rosso, Halina Machelska, Christoph Stein   +4 more
doaj   +1 more source

Opioid and GABAB receptors differentially couple to an adenylyl cyclase/protein kinase A downstream effector after chronic morphine treatment.

Frontiers in Pharmacology, 2014
Opioids are intensely addictive, and cessation of their chronic use is associated with a highly aversive withdrawal syndrome. A cellular hallmark of withdrawal is an opioid sensitive protein kinase A-dependent increase in GABA transporter-1 (GAT-1 ...
Elena Elizabeth Bagley
doaj   +1 more source

Analgesia linked to Nav1.7 loss of function requires µ- and δ-opioid receptors [version 1; referees: 2 approved]

Wellcome Open Research, 2018
Background: Functional deletion of the Scn9a (sodium voltage-gated channel alpha subunit 9) gene encoding sodium channel Nav1.7 makes humans and mice pain-free. Opioid signalling contributes to this analgesic state.
Vanessa Pereira, Queensta Millet, Jose Aramburu, Cristina Lopez-Rodriguez, Claire Gaveriaux-Ruff, John N. Wood   +5 more
doaj   +1 more source

The Hippocampus Is the Place to Be: Opioid Receptors and LTP

Cell Reports, 2019
Nam et al. (2019) genetically modulate the expression of astrocytic μ-opioid receptors to reveal they are necessary for drug-induced conditioned place preference.
Thomas M. Sanderson, John Georgiou, Patrick Tidball, Graham L. Collingridge   +3 more
doaj   +1 more source

Usefulness for the combination of G protein- and β-arrestin-biased ligands of μ-opioid receptors: Prevention of antinociceptive tolerance

Molecular Pain, 2017
Background µ-Opioid receptor internalization is considered to be critically linked to antinociceptive tolerance. Although µ-opioid receptor agonists have been administered simultaneously with other drugs to control pain, little information is available ...
Tomohisa Mori, Naoko Kuzumaki, Takamichi Arima, Michiko Narita, Ryunosuke Tateishi, Takashige Kondo, Yusuke Hamada, Hirotsugu Kuwata, Miho Kawata, Mitsuaki Yamazaki, Kazuyuki Sugita, Akinobu Matsuzawa, Kanae Baba, Takayasu Yamauchi, Kimio Higashiyama, Miki Nonaka, Kanako Miyano, Yasuhito Uezono, Minoru Narita   +18 more
doaj   +1 more source

Synthesis, Biological Evaluation, and SAR Studies of 14β-phenylacetyl Substituted 17-cyclopropylmethyl-7, 8-dihydronoroxymorphinones Derivatives: Ligands With Mixed NOP and Opioid Receptor Profile

Frontiers in Psychiatry, 2018
A series of 14β-acyl substituted 17-cyclopropylmethyl-7,8-dihydronoroxymorphinone compounds has been synthesized and evaluated for affinity and efficacy for mu (MOP), kappa (KOP), and delta (DOP) opioid receptors and nociceptin/orphanin FQ peptide (NOP ...
Vinod Kumar, Willma E. Polgar, Gerta Cami-Kobeci, Mark P. Thomas, Taline V. Khroyan, Lawrence Toll, Stephen M. Husbands   +6 more
doaj   +1 more source

Homeostatic scaling of dynorphin signaling by a non-canonical opioid receptor

Nature Communications
The endogenous opioid system provides powerful control over emotions, nociception, and motivation among many other fundamental nervous system functions.
Xiaona Li, Nathan D. Winters, Shubhi Pandey, Colten Lankford, Hannah M. Stoveken, Emery Smith, Chu-Ting Chang, Stefano Zucca, Louis Scampavia, Timothy Spicer, Kirill A. Martemyanov   +10 more
doaj   +1 more source

Indole Alkaloids as Biased Opioid Receptor Modulators

Pharmaceuticals
Background: Opioid receptors are a commonly used target for treatment of pain conditions. Most opioids used in therapy are linked to adverse effects such as tolerance, dependence, and respiratory depression.
Oliver Grundmann, Allison Henderson
doaj   +1 more source