Results 21 to 30 of about 779,673 (234)

Historical Review: Opiate Addiction and Opioid Receptors

Cell Transplantation, 2019
Substance use disorders (SUDs), defined as a collection of symptoms including tolerance and withdrawal, are chronic illnesses characterized by relapse and remission. In the United States, billions of dollars have been lost due to SUDs.
Shaocheng Wang
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

Antinociceptive potency of a fluorinated cyclopeptide Dmt-c[D-Lys-Phe-p-CF3-Phe-Asp]NH2

Journal of Enzyme Inhibition and Medicinal Chemistry, 2018
Opioid peptides and opiate drugs such as morphine, mediate their analgesic effects, but also undesired side effects, mostly through activation of the mu opioid receptor.
Justyna Piekielna-Ciesielska, Adriano Mollica, Stefano Pieretti, Jakub Fichna, Agata Szymaszkiewicz, Marta Zielińska, Radzisław Kordek, Anna Janecka   +7 more
doaj   +1 more source

Deuterated buprenorphine retains pharmacodynamic properties of buprenorphine and resists metabolism to the active metabolite norbuprenorphine in rats

Frontiers in Pharmacology, 2023
Introduction: An active metabolite of buprenorphine (BUP), called norbuprenorphine (NorBUP), is implicated in neonatal opioid withdrawal syndrome when BUP is taken during pregnancy.
Venumadhav Janganati, Paloma Salazar, Brian J. Parks, Gregory S. Gorman, Paul L. Prather, Eric C. Peterson, Alexander W. Alund, Jeffery H. Moran, Jeffery H. Moran, Peter A. Crooks, Lisa K. Brents   +10 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

The Role of the Endogenous Opioid System in the Vocal Behavior of Songbirds and Its Possible Role in Vocal Learning

Frontiers in Physiology, 2022
The opioid system in the brain is responsible for processing affective states such as pain, pleasure, and reward. It consists of three main receptors, mu- (μ-ORs), delta- (δ-ORs), and kappa- (κ-ORs), and their ligands – the endogenous opioid peptides ...
Utkarsha A. Singh, Soumya Iyengar
doaj   +1 more source

Interactions of the opioid and cannabinoid systems in reward: Insights from knockout studies

Frontiers in Pharmacology, 2015
The opioid system consists of three receptors, mu, delta, and kappa, which are activated by endogenous opioid peptides (enkephalins, endorphins and dynorphins). The endogenous cannabinoid system comprises lipid neuromodulators (endocannabinoids), enzymes
Katia eBefort
doaj   +1 more source

Nanobody-enabled monitoring of kappa opioid receptor states

Nature Communications, 2020
Recent studies revealed that G protein-coupled receptors rapidly interconvert between multiple states. Here, authors use the kappa opioid receptor (KOR) and show how two state-dependent nanobodies provide real-time reporting of ligand stabilized states ...
Tao Che, Justin English, Brian E. Krumm, Kuglae Kim, Els Pardon, Reid H. J. Olsen, Sheng Wang, Shicheng Zhang, Jeffrey F. Diberto, Noah Sciaky, F. Ivy Carroll, Jan Steyaert, Daniel Wacker, Bryan L. Roth   +13 more
doaj   +1 more source

Semisynthetic neoclerodanes as kappa opioid receptor probes [PDF]

Bioorganic & Medicinal Chemistry, 2012
Modification of the furan ring of salvinorin A (1), the main active component of Salvia divinorum, has resulted in novel neoclerodane diterpenes with opioid receptor affinity and activity. Conversion of the furan ring to an aldehyde at the C-12 position (5) has allowed for the synthesis of analogues with new carbon-carbon bonds at that position ...
Lovell, Kimberly M., Vasiljevik, Tamara, Araya, Juan Jose, Lozama, Anthony, Prevatt-Smith, Katherine M., Day, Victor W., Dersch, Christina M., Rothman, Richard B., Butelman, Eduardo R., Kreek, Mary Jeanne, Prisinzano, Thomas E.   +10 more
openaire   +3 more sources

Therapeutic Prospects of Ketamine for Cataplexy in Narcolepsy Type 1: Evidence from a Human Case and a Murine Model

Annals of Neurology, EarlyView.
Narcolepsy type 1 is characterized by cataplexy, for which current treatments targeting monoaminergic, histaminergic, and GABAergic pathways may be ineffective or poorly tolerated. We report the case of a 34‐year‐old man with narcolepsy type 1, intolerant to standard therapies, who experienced marked and sustained cataplexy reduction with morning ...
Francois Ricordeau, Sebastien Arthaud, Leila Langbour, Silvia Melzi, Aurelie Richard‐Mornas, Hannah Doudoux, Benjamin Rolland, Laure Peter‐Derex, Christelle Peyron   +8 more
wiley   +1 more source