Defining the organizational structure of dopamine and muscarninic acetylcholine receptors [PDF]
, 2015 No abstract ...
Alvarez-Curto, Elisa +4 more
core +1 more source
Kinetic properties of “dual” orexin receptor antagonists at OX1R and OX2R orexin receptors [PDF]
Frontiers in Neuroscience, 2013 Orexin receptor antagonists represent attractive targets for the development of drugs for the treatment of insomnia. Both efficacy and safety are crucial in clinical settings and thorough investigations of pharmacokinetics and pharmacodynamics can predict contributing factors such as duration of action and undesirable effects.
Callander, GE +15 more
openaire +3 more sources
Pancreatic exocrine insufficiency after bariatric surgery [PDF]
, 2017 Morbid obesity is a lifelong disease, and all patients require complementary follow-up including nutritional surveillance by a multidisciplinary team after bariatric procedures.
Arnelo, Urban +7 more
core +1 more source
Multiple signaling pathways of orexin receptors. [PDF]
Springerplus, 2015 Orexin/hypocretin peptides are central for the regulation of the sleep/arousal states, and have, in addition, a role in the regulation of e.g. metabolism, addiction, stress response and pain gating. Orexin responses are mediated by G-protein-coupled OX1 and OX2 orexin receptors. Orexin signaling (in different cell types) is very versatile, ranging from
Kukkonen J.
europepmc +3 more sources
The hypocretin/orexin antagonist almorexant promotes sleep without impairment of performance in rats. [PDF]
, 2014 The hypocretin receptor (HcrtR) antagonist almorexant (ALM) has potent hypnotic actions but little is known about neurocognitive performance in the presence of ALM.
Kilduff, Thomas S +4 more
core +2 more sources
A selective role for neuronal activity regulated pentraxin in the processing of sensory-specific incentive value [PDF]
, 2007 Neuronal activity regulated pentraxin (Narp) is a secreted neuronal product which clusters AMPA receptors and regulates excitatory synaptogenesis. Although Narp is selectively enriched in brain, its role in behavior is not known.
Baraban, Jay M +6 more
core +1 more source
The Dual Orexin Receptor Antagonist Almorexant Induces Sleep and Decreases Orexin-Induced Locomotion by Blocking Orexin 2 Receptors [PDF]
Sleep, 2012 Orexin peptides activate orexin 1 and orexin 2 receptors (OX(1)R and OX(2)R), regulate locomotion and sleep-wake. The dual OX(1)R/OX(2)R antagonist almorexant reduces activity and promotes sleep in multiple species, including man. The relative contributions of the two receptors in locomotion and sleep/wake regulation were investigated in mice.Mice ...
Géraldine M, Mang +8 more
openaire +2 more sources
Three classes of ligands each bind to distinct sites on the orphan G protein-coupled receptor GPR84 [PDF]
, 2017 Medium chain fatty acids can activate the pro-inflammatory receptor GPR84 but so also can molecules related to 3,3′-diindolylmethane. 3,3′-Diindolylmethane and decanoic acid acted as strong positive allosteric modulators of the function of each other and
De Vos, Steve +8 more
core +3 more sources
British Journal of Clinical Pharmacology, EarlyView.Aims Fazamorexant is a dual orexin receptor antagonist being developed for the treatment of insomnia. This study aims to determine the dose‐exposure‐response relationship of single‐dose fazamorexant vs. zolpidem in young adult and elderly healthy Chinese volunteers. Methods This single‐centre, randomized, double‐blind, double‐dummy, placebo‐ and active‐
Chen Xia +3 more
wiley +1 more source
Selective loss of GABAB receptors in orexin/hypocretin-producing neurons results in disrupted sleep/wakefulness architecture [PDF]
, 2007 We generated mice with a selective loss of GABAB receptors in orexin neurons. Orexin neurons in these GABAB1<sup>-/-(orexin)</sup> mice showed reduced responsiveness to GABA<sub>A</sub> receptor agonists due to a ...
Bernard Bettler +10 more
core +1 more source