Results 31 to 40 of about 1,574,238 (214)

Highly-selective µ-opioid receptor antagonism does not block L-DOPA-induced dyskinesia in a rodent model

BMC Research Notes, 2020
Objectives Dopamine-replacement utilizing L-DOPA is still the mainstay treatment for Parkinson’s disease (PD), but often leads to development of L-DOPA-induced dyskinesia (LID), which can be as debilitating as the motor deficits.
Mitchell J. Bartlett, Lisa Y. So, Lajos Szabò, David P. Skinner, Kate L. Parent, Michael L. Heien, Todd W. Vanderah, Robin Polt, Scott J. Sherman, Torsten Falk   +9 more
doaj   +1 more source

Opioid receptor agonist–antagonists in pain management: receptor specific mechanisms, dose response relationships, and clinical combination strategies

Frontiers in Pain Research
Opioid receptor agonist–antagonists occupy a distinctive position between high-efficacy agonists and pure antagonists and have been widely used in clinical pain management.
Sining Zhao, Sining Zhao, Zhiqiang Xue, Shu Wang   +3 more
doaj   +1 more source

The influence of μ-opioid and noradrenaline reuptake inhibition in the modulation of pain responsive neurones in the central amygdala by tapentadol in rats with neuropathy [PDF]

, 2015
Treatments for neuropathic pain are either not fully effective or have problematic side effects. Combinations of drugs are often used. Tapentadol is a newer molecule that produces analgesia in various pain models through two inhibitory mechanisms, namely
Gonçalves, L, Friend, LV, Dickenson, AH
core  

The Untranslated Region of μ-Opioid Receptor mRNA Contributes to Reduced Opioid Sensitivity in CXBK Mice

, 2001
It is well known that there are individual differences in a sensitivity to analgesics. Several lines of evidence have suggested that the level of opioid-induced analgesia is dependent on the level of expression of the μ-opioid receptor (μ-OR).
Toru Kobayashi, Kazutaka Ikeda, Toshiro Kumanishi, Hiroaki Niki, Ryoji Yano, Tomio Ichikawa   +5 more
core   +1 more source

Beta1 subunits enable fentanyl‐induced BK channel activation and opioid regulation of cerebral artery diameter

FEBS Open Bio, EarlyView.
During the current opioid crisis, the majority of overdose deaths are attributed to ultra‐potent synthetic opioids, such as fentanyl. While fentanyl exerts its action via opioid receptors, we propose that potassium channels in the brain blood vessels may also sense fentanyl.
Shiwani Thapa, Mohammed Nooh, Akhil Geddati, Alex Dopico, Anna N. Bukiya   +4 more
wiley   +1 more source

Ligand-Specific Regulation of the Endogenous Mu-Opioid Receptor by Chronic Treatment with Mu-Opioid Peptide Agonist [PDF]

, 2013
Since the discovery of the endomorphins (EM), the postulated endogenous peptide agonists of the mu-opioid receptors, several analogues have been synthesized to improve their binding and pharmacological profiles.
Murányi Marianna, Szűcs, Mária, Dochnal Roberta, Kicsi Emese, Kicsi, Emese Gabriella, Fábián Gabriella, Szabó Gyula, Szabó, Gyula, Zentai, András, Bozó, Beáta, Fábián, Gabriella, Birkás Erika, Cinar Resat, Bozó Bea, Birkás, Erika, Kékesi Orsolya Sára, Cinar, Resat, Tóth, Géza, Mácsai Mónika, Mácsai, Mónika, Kékesi, Orsolya, Dochnal, Roberta Beatrix, Tóth Géza, Szűcs Mária, Murányi, Marianna, Zentai András   +25 more
core   +2 more sources

Impact of chronic migraine attacks and their severity on the endogenous μ-opioid neurotransmission in the limbic system

NeuroImage: Clinical, 2019
Objective: To evaluate, in vivo, the impact of ongoing chronic migraine (CM) attacks on the endogenous μ-opioid neurotransmission. Background: CM is associated with cognitive-emotional dysfunction. CM is commonly associated with frequent acute medication
Hassan Jassar, Thiago D. Nascimento, Niko Kaciroti, Marcos F. DosSantos, Theodora Danciu, Robert A. Koeppe, Yolanda R. Smith, Marcelo E. Bigal, Frank Porreca, Kenneth L. Casey, Jon-Kar Zubieta, Alexandre F. DaSilva   +11 more
doaj   +1 more source

Harnessing the Anti-Nociceptive Potential of NK2 and NK3 Ligands in the Design of New Multifunctional μ/δ-Opioid Agonist–Neurokinin Antagonist Peptidomimetics

Molecules, 2021
Opioid agonists are well-established analgesics, widely prescribed for acute but also chronic pain. However, their efficiency comes with the price of drastically impacting side effects that are inherently linked to their prolonged use.
Charlène Gadais, Justyna Piekielna-Ciesielska, Jolien De Neve, Charlotte Martin, Anna Janecka, Steven Ballet   +5 more
doaj   +1 more source

Potent Dmt-Tic Pharmacophoric δ- and μ-Opioid Receptor Antagonists

, 2016
A series of dimeric Dmt-Tic (2‘,6‘-dimethyl-l-tyrosyl-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid) analogues (8−14, 18−22) were covalently linked through diaminoalkane and symmetric or asymmetric 3,6-diaminoalkyl-2(1H)-pyrazinone moieties.
Akihiro Ambo (2351002), Yuko Tsuda (2422411), Yoshio Fujita (140865), Yoshio Okada (2422420), Yusuke Sasaki (764045), Ewa Marczak (2488429), Lawrence H. Lazarus (2350999), Yunden Jinsmaa (1936186), Anna Miyazaki (2422414), Sharon D. Bryant (2488435), Severo Salvadori (402452), Kimitaka Shiotani (2488432), Tingyou Li (2488426)   +12 more
core   +1 more source

Innovative Approach Reveals How Receptors Control G Protein State Equilibria

Advanced Science, EarlyView.
Using conformational specific trFRET biosensors of the Gi protein (depicted at the bottom), the authors show that receptor activation can not only release GDP from the inactive G protein, but can also release GTP from the activated G protein, leading to the reformation of the RG ternary complex.
Alexandre Bouyssou, Mélanie Da Silva, Julien Soulé, Ludovic Fabre, Laurent Lamarque, Rémy Sounier, Thierry Durroux, Sébastien Granier, Thomas Roux, Elodie Dupuis, Eric Trinquet, Philippe Rondard, Jean‐Philippe Pin   +12 more
wiley   +1 more source