Results 1 to 10 of about 25,455 (216)

Nanobody-enabled monitoring of kappa opioid receptor states [PDF]

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   +4 more sources

Novel dual kappa/mu opioid ligands based on a tetrahydroisoquinoline-valine hybrid nucleus [PDF]

Scientific Reports
Opioid addiction constitutes a significant global health challenge. Kappa opioid receptor (KOP) modulators have demonstrated efficacy in treating resistant drug abuse cases.
Ahmad Abdelwaly, Hesham Safwan, Shamba Chatterjee, Mohamed Elsayed, Khaled M. Darwish, Amar Chittiboyina, Mohamed A. Helal   +6 more
doaj   +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, Kaitlin C. Reeves, Nikhil Shah, Nikhil Shah, Braulio Muñoz, Brady K. Atwood, Brady K. Atwood   +6 more
doaj   +1 more source

Expression and Localization of Opioid Receptors in Male Germ Cells and the Implication for Mouse Spermatogenesis. [PDF]

PLoS ONE, 2016
The presence of endogenous opioid peptides in different testicular cell types has been extensively characterized and provides evidence for the participation of the opioid system in the regulation of testicular function.
Haizea Estomba, Iraia Muñoa-Hoyos, Marta Gianzo, Itziar Urizar-Arenaza, Luis Casis, Jon Irazusta, Nerea Subirán   +6 more
doaj   +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

Pharmacology of Kappa Opioid Receptors: Novel Assays and Ligands

Frontiers in Pharmacology, 2022
The present study investigated the in vitro pharmacology of the human kappa opioid receptor using multiple assays, including calcium mobilization in cells expressing chimeric G proteins, the dynamic mass redistribution (DMR) label-free assay, and a ...
Chiara Sturaro, Davide Malfacini, Michela Argentieri, Francine M. Djeujo, Erika Marzola, Valentina Albanese, Chiara Ruzza, Chiara Ruzza, Remo Guerrini, Remo Guerrini, Girolamo Calo’, Paola Molinari   +11 more
doaj   +1 more source

Design and development of novel, short, stable dynorphin-based opioid agonists for safer analgesic therapy

Frontiers in Pharmacology, 2023
Kappa opioid receptors have exceptional potential as an analgesic target, seemingly devoid of many problematic Mu receptor side-effects. Kappa-selective, small molecule pharmaceutical agents have been developed, but centrally mediated side-effects limit ...
Rink-Jan Lohman, Karnaker Reddy Tupally, Ajit Kandale, Peter J. Cabot, Harendra S. Parekh   +4 more
doaj   +1 more source

Controlling opioid receptor functional selectivity by targeting distinct subpockets of the orthosteric site

eLife, 2021
Controlling receptor functional selectivity profiles for opioid receptors is a promising approach for discovering safer analgesics; however, the structural determinants conferring functional selectivity are not well understood.
Rajendra Uprety, Tao Che, Saheem A Zaidi, Steven G Grinnell, Balázs R Varga, Abdelfattah Faouzi, Samuel T Slocum, Abdullah Allaoa, András Varadi, Melissa Nelson, Sarah M Bernhard, Elizaveta Kulko, Valerie Le Rouzic, Shainnel O Eans, Chloe A Simons, Amanda Hunkele, Joan Subrath, Ying Xian Pan, Jonathan A Javitch, Jay P McLaughlin, Bryan L Roth, Gavril W Pasternak, Vsevolod Katritch, Susruta Majumdar   +23 more
doaj   +1 more source

Models of neuroinflammation for the assessment of kappa-opioid receptor ligands

Фармация и фармакология (Пятигорск), 2023
The development of new drugs to combat neuroinflammation is highly relevant as it opens up possibilities for the treatment of a wide range of diseases, including Alzheimer’s disease, Parkinson’s disease, epilepsy, schizophrenia, depression, and others ...
K. Yu. Kalitin, A. A. Spasov, O. Yu. Mukha   +2 more
doaj   +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, Lihua Hang, Tong Liu, Tong Liu   +4 more
doaj   +1 more source