Results 31 to 40 of about 117,188 (306)

Evaluation of the analgesic effect of 4-anilidopiperidine scaffold containing ureas and carbamates [PDF]

, 2016
Fentanyl is a powerful opiate analgesic typically used for the treatment of severe and chronic pain, but its prescription is strongly limited by the well-documented side-effects.
Benyhe, Sa ́ndor, CARRADORI, Simone, Csaba To ̈mbo ̈ly, Erdei, Anna I., Ferenc O. ̈tvos, Ferenc Za ́dor, Fidanza, Lorenzo, Marzoli, Francesca, Mirzaie, Sako, MOLLICA, Adriano, MONTI, LUDOVICA, Moriello, Aniello Schiano, Novellino, Ettore, Petrocellis, Luciano De, PIERETTI, stefano, Samavati, Reza, STEFANUCCI, AZZURRA, Szabolcs Dvora ́csko, Szucs, Edina   +18 more
core   +1 more source

The opioid receptor: emergence through millennia of pharmaceutical sciences

Frontiers in Pain Research, 2023
Throughout history humanity has searched for an optimal approach to the use of opioids that maximizes analgesia while minimizing side effects. This review reflects upon the conceptualization of the opioid receptor and the critical role that the ...
Carolyn A. Fairbanks, Carolyn A. Fairbanks, Carolyn A. Fairbanks, Cristina D. Peterson, Cristina D. Peterson   +4 more
doaj   +1 more source

Phylogenomic analysis reveals extensive phylogenetic mosaicism in the Human GPCR Superfamily [PDF]

, 2007
A novel high throughput phylogenomic analysis (HTP) was applied to the rhodopsin G-protein coupled receptor (GPCR) family. Instances of phylogenetic mosaicism between receptors were found to be frequent, often as instances of correlated mosaicism and ...
Allaby, Robin G., Woodwark, Mathew
core   +1 more source

Peripheral sensitization increases opioid receptor expression and activation by crotalphine in rats.

PLoS ONE, 2014
Inflammation enhances the peripheral analgesic efficacy of opioid drugs, but the mechanisms involved in this phenomenon have not been fully elucidated. Crotalphine (CRP), a peptide that was first isolated from South American rattlesnake C.d.
Vanessa Olzon Zambelli, Ana Carolina de Oliveira Fernandes, Vanessa Pacciari Gutierrez, Julio Cesar Batista Ferreira, Carlos Amilcar Parada, Daria Mochly-Rosen, Yara Cury   +6 more
doaj   +1 more source

Molecular and cellular mechanisms of the age-dependency of opioid analgesia and tolerance

Molecular Pain, 2012
The age-dependency of opioid analgesia and tolerance has been noticed in both clinical observation and laboratory studies. Evidence shows that many molecular and cellular events that play essential roles in opioid analgesia and tolerance are actually age-
Zhao Jing, Xin Xin, Xie Guo-xi, Palmer Pamela, Huang Yu-guang   +4 more
doaj   +1 more source

The effects of pioglitazone, a PPARγ receptor agonist, on the abuse liability of oxycodone among nondependent opioid users [PDF]

, 2016
Aims: Activation of PPARγ by pioglitazone (PIO) has shown some efficacy in attenuating addictive-like responses in laboratory animals. The ability of PIO to alter the effects of opioids in humans has not been characterized in a controlled laboratory ...
Alonzo, Banks, Begelow, Beitner-Johnson, Berger, Bhargava, Bland, Bush, Bussiere, Carr, Chang, Cone, Cooper, de Guglielmo, de Guglielmo, Dhalla, Eisenstein, Eisenstein, Eisenstein, Eng, Ferguson, Fraser, Gagnon, Garrido, Gelinas, Gillies, Hopkins, Hutchinson, Hutchinson, Hutchinson, Jeanne M. Manubay, Jermaine D. Jones, Johnston, Katz, Kielian, Kreutzberg, Ledeboer, Levine, Maria A. Sullivan, Marie-Claire, Martin, Mellon, Moreno, Nakajima, Narita, Pacifici, Pelvig, Roberto Ciccocioppo, Sandra D. Comer, Sarruf, Shanthi Mogali, Song, SPSS, Stoll, Stopponi, Stopponi, Strain, Sweitzer, Tawfik, Tontonoz, Verena E. Metz, Verkhratsky, Walker, Walker, Walsh, Walsh, Watkins, Watkins, Wightman, Woods, Wybran, Zacny, Zacny, Zacny, Zhang   +74 more
core   +1 more source

Targeting peripheral opioid receptors to promote analgesic and anti-inflammatory actions

Frontiers in Pharmacology, 2013
Mechanisms of endogenous pain control are significant. Increasing studies have clearly produced evidence for the clinical usefulness of opioids in peripheral analgesia.
Katerina eIwaszkiewicz, Jennifer eSchneider, Susan eHua   +2 more
doaj   +1 more source

In Vitro Analyses of Spinach-Derived Opioid Peptides, Rubiscolins: Receptor Selectivity and Intracellular Activities through G Protein- and β-Arrestin-Mediated Pathways

Molecules, 2021
Activated opioid receptors transmit internal signals through two major pathways: the G-protein-mediated pathway, which exerts analgesia, and the β-arrestin-mediated pathway, which leads to unfavorable side effects. Hence, G-protein-biased opioid agonists
Yusuke Karasawa, Kanako Miyano, Hideaki Fujii, Takaaki Mizuguchi, Yui Kuroda, Miki Nonaka, Akane Komatsu, Kaori Ohshima, Masahiro Yamaguchi, Keisuke Yamaguchi, Masako Iseki, Yasuhito Uezono, Masakazu Hayashida   +12 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 [PDF]

, 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.
Lattanzi, Roberta, Negri, Lucia, Rief, Silvia, Schmidhammer, Helmut, Spetea, Mariana.   +4 more
core   +2 more sources

Delta-opioid receptor endocytosis in spinal cord after dermenkephalin activation

BMC Neuroscience, 2000
Background The delta(δ)-opioid receptors belong to the G protein-coupled receptors and in vitro studies have shown that δ-opioid receptors undergo an internalization process in response to agonist stimulation.
Gastard Myriam
doaj   +1 more source