Results 51 to 60 of about 549,398 (188)

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

Merkel cells, a new localization of prepro‐orexin and orexin receptors [PDF]

Journal of Anatomy, 2004
AbstractOrexins (OXA and OXB) are peptides derived from a common precursor called prepro‐orexin. They act through G‐protein receptors named orexin 1 receptor (OX1R) and orexin 2 receptor (OX2R). Orexins were first demonstrated in neurons of the lateral hypothalamus and found to be related to the control of food intake.
Andrés, Beiras-Fernández, Rosalía, Gallego, Montserrat, Blanco, Tomás, García-Caballero, Carlos, Diéguez, Andrés, Beiras   +5 more
openaire   +2 more sources

Characterization of a putative orexin receptor in Ciona intestinalis sheds light on the evolution of the orexin/hypocretin system in chordates

Scientific Reports
Tunicates are evolutionary model organisms bridging the gap between vertebrates and invertebrates. A genomic sequence in Ciona intestinalis (CiOX) shows high similarity to vertebrate orexin receptors and protostome allatotropin receptors (ATR).
Maiju K. Rinne, Lauri Urvas, Ilona Mandrika, Dāvids Fridmanis, Darren M. Riddy, Christopher J. Langmead, Jyrki P. Kukkonen, Henri Xhaard   +7 more
doaj   +1 more source

Plasma and breast milk pharmacokinetics of suvorexant in healthy lactating women

British Journal of Clinical Pharmacology, EarlyView.
Aim This paper aims to evaluate the plasma and breast milk pharmacokinetics of suvorexant, an orexin receptor antagonist used to treat insomnia at a maximum dose of 20 mg, in healthy lactating women. Methods The paper reports on an open‐label Phase 1 study in 12 healthy lactating women.
Jacqueline McCrea, Andrew Litovsky, Prachi Wickremasingha, Nairita Ghosal, Brad Roadcap, Robert Valesky, Robin Lee, Leea D. Reed, Ming Wang, Wei Fang, Rebecca Wrishko   +10 more
wiley   +1 more source

Interactions between Lateral Hypothalamic Orexin and Dorsal Raphe Circuitry in Energy Balance

Brain Sciences
Orexin/hypocretin terminals innervate the dorsal raphe nucleus (DRN), which projects to motor control areas important for spontaneous physical activity (SPA) and energy expenditure (EE).
Vijayakumar Mavanji, Brianna L. Pomonis, Laurie Shekels, Catherine M. Kotz   +3 more
doaj   +1 more source

Orexin-A and endocannabinoids are involved in obesity-associated alteration of hippocampal neurogenesis, plasticity, and episodic memory in mice

Nature Communications, 2021
The authors show that adult hippocampal neurogenesis is altered in the dentate gyrus of obese mice with subsequent inhibition of long-term potentiation and impairment of pattern separation. Inhibition of orexin-A action at orexin-1 receptors rescued both
Nicola Forte, Serena Boccella, Lea Tunisi, Alba Clara Fernández-Rilo, Roberta Imperatore, Fabio Arturo Iannotti, Maria De Risi, Monica Iannotta, Fabiana Piscitelli, Raffaele Capasso, Paolo De Girolamo, Elvira De Leonibus, Sabatino Maione, Vincenzo Di Marzo, Luigia Cristino   +14 more
doaj   +1 more source

Bidirectional Pathological Axis Between Alzheimer's Disease and Circadian Rhythm Disturbance: Mechanisms and Therapeutic Strategies

iNew Medicine, EarlyView.
This graphical abstract illustrates a bidirectional vicious cycle between Alzheimer’s disease (AD) and circadian rhythm disturbance (CRD). On the one hand, AD pathology, including amyloid‐β (Aβ) plaque deposition and tau hyperphosphorylation, may damage the suprachiasmatic nucleus (SCN) and disrupt melatonin signaling, leading to sleep fragmentation ...
Jiajia Qin, Xianfeng Yu, Yayu Wang, Xiaohan Song, Yuehua Wang, Zhixin Wang, Wei Miao, Xudong Yang, Jiajia Zhu, Xiaoqun Zhu, Maria‐Trinidad Herrero   +10 more
wiley   +1 more source

Neurobiology of the Orexin System and Its Potential Role in the Regulation of Hedonic Tone

Brain Sciences, 2022
Orexin peptides comprise two neuropeptides, orexin A and orexin B, that bind two G-protein coupled receptors (GPCRs), orexin receptor 1 (OXR1) and orexin receptor 2 (OXR2).
Martin A. Katzman, Matthew P. Katzman
doaj   +1 more source

Advancing pharmacometrics in Africa—Transition from capacity development toward job creation

CPT: Pharmacometrics &Systems Pharmacology, Volume 14, Issue 3, Page 407-419, March 2025.
Abstract Trained pharmacometricians remain scarce in Africa due to limited training opportunities, lack of a pharmaceutical product development ecosystem, and emigration to high‐income countries. The Applied Pharmacometrics Training (APT) fellowship program was established to address these gaps and specifically foster job creation for talent retention.
Goonaseelan (Colin) Pillai, Samer Mouksassi, Innocent G. Asiimwe, Craig R. Rayner, Steven Kern, Phumla Sinxadi, Paolo Denti, Eric Decloedt, Catriona Waitt, Bernhards R. Ogutu, Rik de Greef   +10 more
wiley   +1 more source

Role of orexin receptors in histamine- and chloroquine-induced pruriceptive processing

Neuroscience Research
It is known that orexin peptides are involved in nociceptive processing, while little is known about the roles of these peptides in itch processing. To reveal the functions of orexin peptides in pruriceptive processing, orexin A (OX-A) and orexin B (OX-B)
Anna Kanemaru-Kawazoe, Hideki Funahashi, Yoichiro Kogoh, Ayaka Haruta-Tsukamoto, Yu Miyahara, Toshikazu Nishimori, Yasushi Ishida, Yoji Hirano   +7 more
doaj   +1 more source