Results 41 to 50 of about 416,668 (254)

In Silico to In Cerebro—Development of the Orexin Receptor Antagonist “Photorexant” for Photomodulation In Vitro and in Mouse Brains

Angewandte Chemie International Edition, EarlyView.
Following a structure‐based design approach, photoswitchable derivatives of the FDA‐approved drug suvorexant were designed, docked, synthesized, and characterized pharmacologically at the orexin 1 and 2 receptors (OX1R and OX2R). Optimized “photorexant” showed up to an 11‐fold difference in IC50 between photoisomers, enabled dynamic and reversible ...
Marcus Angermann, Marie H. Deventer, Vicente Ledesma‐Martin, Nuno Martinho, Alix Flake, Silvia Mori, Angel Nuñez, Jaime Pignatelli, Rita C. Guedes, Christophe P. Stove, Michael Decker   +10 more
wiley   +1 more source

Antinociceptive potency of a fluorinated cyclopeptide Dmt-c[D-Lys-Phe-p-CF3-Phe-Asp]NH2

Journal of Enzyme Inhibition and Medicinal Chemistry, 2018
Opioid peptides and opiate drugs such as morphine, mediate their analgesic effects, but also undesired side effects, mostly through activation of the mu opioid receptor.
Justyna Piekielna-Ciesielska, Adriano Mollica, Stefano Pieretti, Jakub Fichna, Agata Szymaszkiewicz, Marta Zielińska, Radzisław Kordek, Anna Janecka   +7 more
doaj   +1 more source

Proto‐Panic Modulation by Caffeine‐Proteinoid Complexes

Journal of Applied Polymer Science, EarlyView.
Caffeine–proteinoid microspheres synthesized by thermal polymerization exhibit compartmentalized drug loading with encapsulation efficiencies of 61%–82% and triphasic release kinetics. Electrochemical monitoring reveals multi‐scale oscillatory dynamics consistent with chaotic and damped harmonic behavior, while Boolean logic operations demonstrate ...
Panagiotis Mougkogiannis, Andrew Adamatzky   +1 more
wiley   +1 more source

Opioid peptide-derived analgesics [PDF]

The AAPS Journal, 2005
Two recent developments of opioid peptide-based analgesics are reviewed. The first part of the review discusses the dermorphin-derived, cationic-aromatic tetrapeptide H-Dmt-D-Arg-Phe-Lys-NH(2) ([Dmt(1)]DALDA, where Dmt indicates 2',6'-dimethyltyrosine), which showed subnanomolar mu receptor binding affinity, extraordinary mu receptor selectivity, and ...
openaire   +2 more sources

Gabapentinoids‐duloxetine combination therapy for chronic pain: A mechanism oriented rational to bridge theoretical knowledge and real life setting

British Journal of Clinical Pharmacology, EarlyView.
Chronic pain represents a complex debilitating condition that extends beyond the protective function of physiological pain, often persisting as an independent disease entity. Chronic primary and secondary pain syndromes reflect a multifaceted continuum involving nociceptive, neuropathic and nociplastic mechanisms.
Stefania Nobili, Maurizio Evangelista, Elena Lucarini, Elena G. Giugliano, Carla Ghelardini, Laura Micheli, Lorenzo Di Cesare Mannelli   +6 more
wiley   +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

Effects of chronic treatment with atypical neuroleptics on the biosynthesis and release of opioid peptides in guinea-pig ileum

, 1985
The guinea-pig ileum myenteric plexus is known to contain opioid peptides, which can be released by electric stimulation at high frequency. Haloperidol, a classic neuroleptic drug, increases the biosynthesis and release of endogenous opioid peptides from
Martínez, J. A., Brugger, A. J., Milanés, M. V., Vargas, M. L., Pérez, D.   +4 more
core   +1 more source

Safety of opioid patch initiation in Australian residential aged care [PDF]

, 2015
Explores opioid use by aged care facility residents before and after initiation of transdermal opioid patches. Abstract Objective: To explore opioid use by aged care facility residents before and after initiation of transdermal opioid patches. Design:
Lisa Pont, Svetla Gadzhanova, Elizabeth Roughead, Roughead, E.E., Pont, L.G., Gadzhanova, S.   +5 more
core   +1 more source

Histamine and the mechanisms of nausea and vomiting: Translating the uncertain pharmacology of cyclizine

British Journal of Clinical Pharmacology, EarlyView.
Abstract Cyclizine is a long‐established, short‐acting drug, registered for preventing motion sickness, post‐operative nausea and vomiting (PONV) and ‘vomiting of known cause’. The latter is not defined but may include pregnancy and patients receiving palliative care, historically accepted without large, controlled trials.
Gareth J. Sanger, Paul L. R. Andrews
wiley   +1 more source

Concomitant duplications of opioid peptide and receptor genes before the origin of jawed vertebrates. [PDF]

PLoS ONE, 2010
BACKGROUND: The opioid system is involved in reward and pain mechanisms and consists in mammals of four receptors and several peptides. The peptides are derived from four prepropeptide genes, PENK, PDYN, PNOC and POMC, encoding enkephalins, dynorphins ...
Görel Sundström, Susanne Dreborg, Dan Larhammar   +2 more
doaj   +1 more source