Results 1 to 10 of about 2,581,877 (313)

Ligand and G-protein selectivity in the κ-opioid receptor [PDF]

Nature, 2023
The κ-opioid receptor (KOR) represents a highly desirable therapeutic target for treating not only pain but also addiction and affective disorders^ 1 .
Jianming Han, Jingying Zhang, Antonina L. Nazarova, Sarah M. Bernhard, B. Krumm, Lei Zhao, Jordy Homing Lam, Vipin A. Rangari, Susruta Majumdar, David E. Nichols, Vsevolod Katritch, Peng Yuan, Jonathan F. Fay, Tao Che   +13 more
openalex   +2 more sources

Opioid Receptor-Mediated Regulation of Neurotransmission in the Brain

Frontiers in Molecular Neuroscience, 2022
Opioids mediate their effects via opioid receptors: mu, delta, and kappa. At the neuronal level, opioid receptors are generally inhibitory, presynaptically reducing neurotransmitter release and postsynaptically hyperpolarizing neurons.
Kaitlin C. Reeves, Nikhil P. Shah, B. Muñoz, Brady K. Atwood   +3 more
semanticscholar   +1 more source

Toll-Like Receptor 4 (TLR4)/Opioid Receptor Pathway Crosstalk and Impact on Opioid Analgesia, Immune Function, and Gastrointestinal Motility

Frontiers in Immunology, 2020
Toll-like receptor 4 (TLR4) recognizes exogenous pathogen-associated molecular patterns (PAMPs) and endogenous danger-associated molecular patterns (DAMPs) and initiates the innate immune response.
Peng Zhang, Meirong Yang, Chunhua Chen, Liu Liu, Xinchuan Wei, Si Zeng   +5 more
semanticscholar   +1 more source

Nanobody-enabled monitoring of kappa opioid receptor states

Nature Communications, 2020
Recent studies show that GPCRs rapidly interconvert between multiple states although our ability to interrogate, monitor and visualize them is limited by a relative lack of suitable tools.
T. Che, J. G. English, B. Krumm, Kuglae Kim, E. Pardon, Reid H. J. Olsen, Sheng Wang, Sheng Wang, Shicheng Zhang, J. Diberto, N. Sciaky, F. Carroll, J. Steyaert, Daniel Wacker, Daniel Wacker, B. Roth   +15 more
semanticscholar   +1 more source

Mu Opioid Receptor Heterodimers Emerge as Novel Therapeutic Targets: Recent Progress and Future Perspective

Frontiers in Pharmacology, 2020
Opioids are the most effective analgesics used in the clinical management of cancer pain or non-cancer pain. However, chronic opioids therapy can cause many side effects including respiratory depression, nausea, sedation, itch, constipation, analgesic ...
Li Zhang, Jiang-Tao Zhang, Li-hua Hang, Tong Liu   +3 more
semanticscholar   +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

On the G-protein-coupled receptor heteromers and their allosteric receptor-receptor interactions in the central nervous system: focus on their role in pain modulation [PDF]

, 2013
The modulatory role of allosteric receptor-receptor interactions in the pain pathways of the Central Nervous System and the peripheral nociceptors has become of increasing interest.
Agnati, Luigi F, Borroto-Escuela, Dasiel O, Fuxe, Kjell, Rivera, Alicia, Romero-Fernandez, Wilber, Tarakanov, Alexander O, Van Craenenbroeck, Kathleen   +6 more
core   +3 more sources

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

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

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