Results 21 to 30 of about 2,577,172 (407)

Structure of the μ Opioid Receptor-Gi Protein Complex

Nature, 2018
The μ-opioid receptor (μOR) is a G-protein-coupled receptor (GPCR) and the target of most clinically and recreationally used opioids. The induced positive effects of analgesia and euphoria are mediated by μOR signalling through the adenylyl cyclase ...
A. Koehl, Hongli Hu, S. Maeda, Yan Zhang, Q. Qu, Joseph M. Paggi, Naomi R. Latorraca, D. Hilger, R. Dawson, H. Matile, G. Schertler, S. Granier, W. Weis, R. Dror, A. Manglik, G. Skiniotis, B. Kobilka   +16 more
semanticscholar   +1 more source

7‑hydroxymitragynine is an active metabolite of mitragynine and a key mediator of its analgesic effects [PDF]

, 2019
Mitragynina speciosa, more commonly known as kratom, is a plant native to Southeast Asia, the leaves of which have been used traditionally as a stimulant, analgesic, and treatment for opioid addiction.
Ansonoff, Michael, Gassaway, Madalee M., Grinnell, Steven G., Javitch, Jonathan A., Kruegel, Andrew C., Langreck, Cory, Le Rouzic, Valerie, Majumdar, Susruta, Pasternak, Gavril W., Pekarskaya, Elizabeth A., Pintar, John E., Sames, Dalibor, Uprety, Rajendra   +12 more
core   +3 more sources

Functional modulation of human delta opioid receptor by neuropeptide FF

BMC Neuroscience, 2005
Background Neuropeptide FF (NPFF) plays a role in physiological pain sensation and opioid analgesia. For example, NPFF potentiates opiate-induced analgesia and the delta opioid receptor antagonist naltrindole inhibits NPFF-induced antinociception.
Panula Pertti, Änkö Minna-Liisa
doaj   +1 more source

Scalable Production of Highly-Sensitive Nanosensors Based on Graphene Functionalized with a Designed G Protein-Coupled Receptor [PDF]

, 2014
We have developed a novel, all-electronic biosensor for opioids that consists of an engineered mu opioid receptor protein, with high binding affinity for opioids, chemically bonded to a graphene field-effect transistor to read out ligand binding.
Crook, Alexander, Han, Gang Hee, Hong, Sung Ju, Johnson, A. T. Charlie, Lerner, Mitchell B., Liu, Renyu, Matsunaga, Felipe, Park, Yung Woo, Perez-Aguilar, Jose Manuel, Saven, Jeffery G., Xi, Jin   +10 more
core   +4 more sources

The atypical chemokine receptor ACKR3/CXCR7 is a broad-spectrum scavenger for opioid peptides

Nature Communications, 2020
Endogenous opioid peptides and prescription opioid drugs modulate pain, anxiety and stress by activating opioid receptors, currently classified into four subtypes. Here we demonstrate that ACKR3/CXCR7, hitherto known as an atypical scavenger receptor for
M. Meyrath, M. Szpakowska, J. Zeiner, L. Massotte, Myriam P Merz, Tobias Benkel, Katharina Simon, Jochen Ohnmacht, J. D. Turner, R. Krüger, V. Seutin, M. Ollert, E. Kostenis, A. Chevigné   +13 more
semanticscholar   +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 [PDF]

, 2018
© 2018 Kumar, Polgar, Cami-Kobeci, Thomas, Khroyan, Toll and Husbands.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 ...
Cami-Kobeci, Champion, Cheng, Christoph, Ding, Dooley, Greedy, Greiner, Gumusel, Günther, Hu, Huang, Jenck, Khroyan, Khroyan, Kiguchi, Ko, Lewis, Lewis, Lia, Manabe, Meunier, Meunier, Mogil, Mollereau, Moynihan, Pomonis, Raffa, Reinsceid, Rizzi, Rossi, Saccone, Sandin, Schmidhammer, Schmidhammer, Schmidhammer, Spagnolo, Sukhtankar, Thompson, Toll, Toll, Traynor, Ueda, Vanderah, Váradi, Woodcock, Yu, Zeilhofer   +47 more
core   +3 more sources

APOLLO‐2: A Randomized, Placebo and Active‐Controlled Phase III Study Investigating Oliceridine (TRV130), a G Protein–Biased Ligand at the μ‐Opioid Receptor, for Management of Moderate to Severe Acute Pain Following Abdominoplasty

Pain Practice, 2019
The clinical utility of conventional IV opioids is limited by the occurrence of opioid‐related adverse events. Oliceridine is a novel G protein–biased μ‐opioid receptor agonist designed to provide analgesia with an improved safety and tolerability ...
N. Singla, F. Skobieranda, D. Soergel, Monica Y Salamea, D. Burt, M. Demitrack, E. Viscusi   +6 more
semanticscholar   +1 more source

Lack of μ-Opioid Receptor-Mediated G-Protein Activation in the Spinal Cord of Mice Lacking Exon 1 or Exons 2 and 3 of the MOR-1 Gene

Journal of Pharmacological Sciences, 2003
: The G-protein activation induced by μ-opioid receptor agonists was determined in spinal cord membranes from two types of μ-opioid receptor knockout mice: mice with a disruption of exon 1 (MOR (Exon 1)-KO) or exons 2 and 3 (MOR (Exons 2 and 3)-KO) of ...
Hirokazu Mizoguchi, Hsiang-En Wu, Minoru Narita, Ichiro Sora, F. Scott Hall, George R. Uhl, Horace H. Loh, Hiroshi Nagase, Leon F. Tseng   +8 more
doaj   +1 more source

Modeling buprenorphine reduction of fentanyl-induced respiratory depression

JCI Insight, 2022
BACKGROUND Potent synthetic opioids, such as fentanyl, are increasingly abused, resulting in unprecedented numbers of fatalities from respiratory depression.
Erik Olofsen, Marijke Hyke Algera, Laurence Moss, Robert L. Dobbins, Geert J. Groeneveld, Monique van Velzen, Marieke Niesters, Albert Dahan, Celine M. Laffont   +8 more
doaj   +1 more source

Modulation of Neurally Mediated Vasodepression and Bradycardia by Electroacupuncture through Opioids in Nucleus Tractus Solitarius. [PDF]

, 2018
Stimulation of vagal afferent endings with intravenous phenylbiguanide (PBG) causes both bradycardia and vasodepression, simulating neurally mediated syncope.
Fu, Liang-Wu, Guo, Zhi-Ling, Longhurst, John C, Tjen-A-Looi, Stephanie C   +3 more
core   +3 more sources