Results 11 to 20 of about 83,214 (263)

Possible Involvement of Hallucinogenic Effects in the Aversive Effects Induced by Kappa-Opioid and 5-HT_2A _/2C Receptor Agonists in Mice. [PDF]

Neuropsychopharmacol Rep
This study developed a simple way to test new psychoactive substances (NPS) in mice. Two drugs, U50,488H and DOI caused aversive and abnormal behaviors in mice, likely linked to their hallucinogenic properties. These results suggest such behavioral tests could help quickly identify and regulate harmful psychoactive drugs. ABSTRACT Aim The regulation of
Kato H, Ichimaru Y, Kurihara M, Sogawa K, Funada M, Suzuki T.   +5 more
europepmc   +2 more sources

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

Ascent of the kappa-opioid receptor in psychopharmacology [PDF]

Psychopharmacology, 2010
Often overshadowed by other members of the endogenous opioid receptor family, kappa-opioid receptors (KORs) are rapidly emerging as an important target for the study and treatment of a variety of central nervous system disorders. This Special Issue is dedicated to 18 papers that describe some of the newest and most important developments.
William A, Carlezon, Klaus A, Miczek
openaire   +2 more sources

Pharmacological profiles of opioid ligands at Kappa opioid receptors [PDF]

BMC Pharmacology, 2006
Abstract Background The aim of the present study was to describe the activity of a set of opioid drugs, including partial agonists, in a human embryonic kidney cell system stably expressing only the mouse κ-opioid receptors.
Gharagozlou, Parham, Hashemi, Ezzat, DeLorey, Timothy M, Clark, J David, Lameh, Jelveh   +4 more
openaire   +2 more sources

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

Opioids and opioid receptors; understanding pharmacological mechanisms as a key to therapeutic advances and mitigation of the misuse crisis

BJA Open, 2023
Opioids are a mainstay in acute pain management and produce their effects and side effects (e.g., tolerance, opioid-use disorder and immune suppression) by interaction with opioid receptors.
David G. Lambert
doaj   +1 more source