Results 11 to 20 of about 16,588 (201)

Orexin receptor agonist Yan 7874 is a weak agonist of orexin/hypocretin receptors and shows orexin receptor-independent cytotoxicity [PDF]

PLOS ONE, 2017
Two promising lead structures of small molecular orexin receptor agonist have been reported, but without detailed analyses of the pharmacological properties. One of them, 1-(3,4-dichlorophenyl)-2-[2-imino-3-(4-methylbenzyl)-2,3-dihydro-1H-benzo[d]imidazol-1-yl]ethan-1-ol (Yan 7874), is commercially available, and we set out to analyze its properties ...
Turku, Ainoleena, Rinne, Maiju K., af Gennas, Gustav Boije, Xhaard, Henri, Lindholm, Dan, Kukkonen, Jyrki P.   +5 more
openaire   +7 more sources

Functional cardiac orexin receptors: role of orexin-B/orexin 2 receptor in myocardial protection. [PDF]

Clin Sci (Lond), 2018
Orexins/hypocretins exert cardiovascular effects which are centrally mediated. In the present study, we tested whether orexins and their receptors may also act in an autocrine/paracrine manner in the heart exerting direct effects. Quantitative reverse transcription-PCR (RT-PCR), immunohistochemical and Western blot analyses revealed that the rat heart ...
Patel VH, Karteris E, Chen J, Kyrou I, Mattu HS, Dimitriadis GK, Rodrigo G, Antoniades C, Antonopoulos A, Tan BK, Hillhouse EW, Ng A, Randeva HS.   +12 more
europepmc   +9 more sources

Orexin Directly Excites Orexin Neurons through Orexin 2 Receptor [PDF]

The Journal of Neuroscience, 2010
Orexin neurons (hypocretin neurons) have a critical role in the regulation of sleep/wakefulness, especially in the maintenance of arousal. Here, we revealed that orexin neurons are directly and indirectly activated by orexin via the orexin 2 receptor (OX2R).
Akihiro, Yamanaka, Sawako, Tabuchi, Tomomi, Tsunematsu, Yugo, Fukazawa, Makoto, Tominaga   +4 more
openaire   +2 more sources

Orexin Receptor Antagonists [PDF]

Current Sleep Medicine Reports, 2017
This paper focuses on the role of orexin receptors in sleep as evidenced in recent preclinical and clinical work. Orexin A and B and their two receptors (OX1R and OX2R) play essential roles in arousal and sleep/wake regulation, addiction, and stress. The absence of orexin producing cells in the lateral hypothalamus or of orexins in the CSF results in ...
B.T. Shireman, M.A. Letavic
openaire   +3 more sources

Orexinergic Input to Dopaminergic Neurons of the Human Ventral Tegmental Area [PDF]

, 2013
The mesolimbic reward pathway arising from dopaminergic (DA) neurons of the ventral tegmental area (VTA) has been strongly implicated in reward processing and drug abuse.
A Bisetti, AJ Lawrence, Alice Y. W. Chang, AR Di Sebastiano, B Boutrel, B Boutrel, B Wang, BA Baldo, Beáta Á. Borsay, C Baimel, C Peyron, CM Kotz, CS Molnar, Csilla S. Molnár, CV Dayas, D Georgescu, D Sulzer, E Hirsch, E Hrabovszky, E Hrabovszky, Erik Hrabovszky, G Aston-Jones, G Martin, GC Harris, GC Harris, J Fadel, J Xia, JA Hollander, JJ Balcita-Pedicino, K Mukai, L de Lecea, László Herczeg, M Barrot, M Narita, NM Vittoz, NM Vittoz, Péter Gergely, R Fronczek, R Sharf, R Sharf, RM Chemelli, S Deurveilher, S Srinivasan, SL Borgland, SV Mahler, T Bullmann, T Nakamura, T Sakurai, TM Korotkova, TM Korotkova, XY Lu, Y Date, Z Liposits, Zsolt Liposits   +53 more
core   +10 more sources

Orexin-1 receptor-cannabinoid CB1 receptor heterodimerization results in both ligand-dependent and -independent coordinated alterations of receptor localization and function [PDF]

, 2006
Following inducible expression in HEK293 cells, the human orexin-1 receptor was targeted to the cell surface but became internalized following exposure to the peptide agonist orexin A.
Canals Buj, M., Ellis, J., Milasta, S., Milligan, G., Pediani, J.D.   +4 more
core   +1 more source

In Vitro Signaling Properties of Cannabinoid and Orexin Receptors: How Orexin Receptors Influence Cannabinoid Receptor-Mediated Signaling. [PDF]

Pharmacol Res Perspect
ABSTRACTThe co‐expression of different types of G protein‐coupled receptors (GPCRs) in the same cells can have implications for receptor signaling and receptor cross‐talk, potentially altering the apparent potency or efficacy of ligands targeting each receptor.
Mohamed KA, Laprairie RB.
europepmc   +4 more sources

Orexin-Corticotropin-Releasing Factor Receptor Heteromers in the Ventral Tegmental Area as Targets for Cocaine [PDF]

, 2015
Release of the neuropeptides corticotropin-releasing factor (CRF) and orexin-A in the ventral tegmental area (VTA) play an important role in stress-induced cocaine-seeking behavior.
Aguinaga, David, Cai, Ning-Sheng, Canela, Enric I, Casadó, Vicent, Cortés, Antonio, Ferré, Sergi, Hausch, Felix, Howell, Lesley A., Lluís, Carme, Mallol, Josefa, McCormick, Peter J., McDowell, Kimberly, Moreno, Estefanía, Moreno-Delgado, David, Navarro, Gemma, Quiroz, César, Rea, William, Sierakowiak, Adam   +17 more
core   +1 more source

Orexin/hypocretin receptor signalling cascades [PDF]

British Journal of Pharmacology, 2013
Orexin (hypocretin) peptides and their two known G‐protein‐coupled receptors play essential roles in sleep–wake control and powerfully influence other systems regulating appetite/metabolism, stress and reward. Consequently, drugs that influence signalling by these receptors may provide novel therapeutic opportunities for treating sleep disorders ...
J P, Kukkonen, C S, Leonard
openaire   +2 more sources

Hypocretin-1 receptors regulate the reinforcing and reward-enhancing effects of cocaine: pharmacological and behavioral genetics evidence. [PDF]

, 2012
Considerable evidence suggests that transmission at hypocretin-1 (orexin-1) receptors (Hcrt-R1) plays an important role in the reinstatement of extinguished cocaine-seeking behaviors in rodents.
Fowler, Christie D, Hollander, Jonathan A, Kenny, Paul J, Pham, Don   +3 more
core   +3 more sources