Results 41 to 50 of about 1,142,563 (307)

Signal Transduction and Pathogenic Modifications at the Melanocortin-4 Receptor: A Structural Perspective [PDF]

, 2019
The melanocortin-4 receptor (MC4R) can be endogenously activated by binding of melanocyte-stimulating hormones (MSH), which mediates anorexigenic effects. In contrast, the agouti-related peptide (AgRP) acts as an endogenous inverse agonist and suppresses
Biebermann, Heike, Cerdá-Reverter, José Miguel, Heyder, Nicolas, Kleinau, Gunnar, Krude, Heiko, Kwiatkowski, Dennis, Kühnen, Peter, Scheerer, Patrick, Soletto, Lucia, Speck, David, Szczepek, Michal   +10 more
core   +1 more source

Morphine activates neuroinflammation in a manner parallel to endotoxin [PDF]

, 2012
Opioids create a neuroinflammatory response within the CNS, compromising opioid-induced analgesia and contributing to various unwanted actions. How this occurs is unknown but has been assumed to be via classic opioid receptors.
A. A. Somogyi, A. J. de Jesus, A. Reddy, Barochia, Bevan, Bokhari, Dziarski, H. Yin, Hargreaves, Hoshino, Hutchinson, Hutchinson, Hutchinson, Hutchinson, Hutchinson, Hutchinson, J. Thomas, Jacquet, Joce, K. Cheng, K. Ramos, Kirikae, L. C. Loram, L. R. Watkins, Lewis, Li, Liu, Liu, M. R. Hutchinson, Manavalan, Milligan, Nagyoszi, Narita, Ohto, Park, Resman, Rice, Slivka, Takeuchi, Viriyakosol, Watkins, X. Wang, Youn   +42 more
core   +2 more sources

Alum adjuvant is more effective than MF59 at prompting early germinal center formation in response to peptide-protein conjugates and enhancing efficacy of a vaccine against opioid use disorders

Human Vaccines & Immunotherapeutics, 2019
Opioid use disorders (OUD) and fatal overdoses are a national emergency in the United States. Therapeutic vaccines offer a promising strategy to treat OUD and reduce the incidence of overdose.
Christine Robinson, Carly Baehr, Shirdi E. Schmiel, Claudia Accetturo, Daniel L. Mueller, Marco Pravetoni   +5 more
doaj   +1 more source

Nociceptin attenuates the escalation of oxycodone self-administration by normalizing CeA-GABA transmission in highly addicted rats. [PDF]

, 2020
Approximately 25% of patients who are prescribed opioids for chronic pain misuse them, and 5 to 10% develop an opioid use disorder. Although the neurobiological target of opioids is well known, the molecular mechanisms that are responsible for the ...
Carrette, Lieselot LG, de Guglielmo, Giordano, George, Olivier, Kallupi, Marsida, Kononoff, Jenni, Palmer, Abraham A, Schweitzer, Paul, Solberg Woods, Leah C   +7 more
core  

A Bicyclic Analog of the Linear Peptide Arodyn Is a Potent and Selective Kappa Opioid Receptor Antagonist

Molecules
Kappa opioid receptor (KOR) antagonists have potential therapeutic applications in the treatment of stress-induced relapse to substance abuse and mood disorders.
Solomon A. Gisemba, Michael J. Ferracane, Thomas F. Murray, Jane V. Aldrich   +3 more
doaj   +1 more source

Opioid Receptors in Immune and Glial Cells-Implications for Pain Control [PDF]

, 2020
Opioid receptors comprise μ (MOP), δ (DOP), κ (KOP), and nociceptin/orphanin FQ (NOP) receptors. Opioids are agonists of MOP, DOP, and KOP receptors, whereas nociceptin/orphanin FQ (N/OFQ) is an agonist of NOP receptors.
Celik, Melih Ö., Machelska, Halina
core   +1 more source

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

Neuroprotective Potential of Biphalin, Multireceptor Opioid Peptide, Against Excitotoxic Injury in Hippocampal Organotypic Culture

Neurochemical Research, 2011
Biphalin is a dimeric opioid peptide that exhibits affinity for three types of opioid receptors (MOP, DOP and KOP). Biphalin is undergoing intensive preclinical study. It was recognized that activation of δ-opioid receptor elicits neuroprotection against
M. Kawalec, J. Kowalczyk, M. Beręsewicz, A. Lipkowski, B. Zabłocka   +4 more
semanticscholar   +1 more source

Design and structural validation of peptide–drug conjugate ligands of the kappa-opioid receptor

Nature Communications, 2023
Despite the increasing number of GPCR structures and recent advances in peptide design, the development of efficient technologies allowing rational design of high-affinity peptide ligands for single GPCRs remains an unmet challenge.
Edin Muratspahić, Kristine Deibler, Jianming Han, Nataša Tomašević, Kirtikumar B. Jadhav, Aina-Leonor Olivé-Marti, Nadine Hochrainer, Roland Hellinger, Johannes Koehbach, Jonathan F. Fay, Mohammad Homaidur Rahman, Lamees Hegazy, Timothy W. Craven, Balazs R. Varga, Gaurav Bhardwaj, Kevin Appourchaux, Susruta Majumdar, Markus Muttenthaler, Parisa Hosseinzadeh, David J. Craik, Mariana Spetea, Tao Che, David Baker, Christian W. Gruber   +23 more
doaj   +1 more source

A Bioresorbable Neural Interface for On‐Demand Thermal Pain Block

Advanced Functional Materials, EarlyView.
Bioresorbable, implantable neural electronics provide dynamic, on‐demand thermal modulation of peripheral nerves for safe, drug‐free pain relief. A microscale thin‐film heater and temperature sensor embedded within biodegradable encapsulants enable precise temperature control via real‐time feedback.
Jeonghwan Park, Hak‐Young Ahn, Minho Seong, Taehoon Kim, Yulin Zhou, Yameng Xu, Jaehee Lee, Ritika Raj Menghani, Yujin Choi, Minsu Park, Nadir Muzaffar, Youngeun Lee, Seung Gi Seo, Jong Uk Kim, Sang Min Won, Jahyun Koo, Elena Aprea, Taeyeon Kim, Ying Yan, Matthew R. MacEwan, Wilson Z. Ray, Raudel Avila, Geumbee Lee, John A. Rogers   +23 more
wiley   +1 more source