Functional cardiac orexin receptors: role of orexin-B/orexin 2 receptor in myocardial protection
نویسندگان
چکیده
منابع مشابه
Orexin and Orexin Receptors
“Reverse pharmacology”, i.e., ligand identification using cell lines expressing orphan receptors, combined with genetic engineering techniques, has increased our understanding of novel signaling systems in the body. Orexin is the first and most successful example of the factors to which such an approach was applied. Our group initially identified orexin A and orexin B as endogenous peptide liga...
متن کاملOrexin directly excites orexin neurons through orexin 2 receptor.
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). Orexin B (1 μM) induced depolarization in orexin neurons, which was still observed in the presence of TTX (1 μM), AP-5 (50 μM), and CNQX (...
متن کاملBlockade of orexin-1 receptors attenuates orexin-2 receptor antagonism-induced sleep promotion in the rat.
Orexins are peptides produced by lateral hypothalamic neurons that exert a prominent role in the maintenance of wakefulness by activating orexin-1 (OX1R) and orexin-2 (OX2R) receptor located in wake-active structures. Pharmacological blockade of both receptors by the dual OX1/2R antagonist (2R)-2-[(1S)-6,7-dimethoxy-1-{2-[4-(trifluoromethyl)phenyl]ethyl}-3,4-dihydroisoquinolin-2(1H)-yl]-N-methy...
متن کاملThe dual orexin receptor antagonist almorexant induces sleep and decreases orexin-induced locomotion by blocking orexin 2 receptors.
STUDY OBJECTIVES 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. DESIGN Mice lacking orexin recep...
متن کاملOrexin receptor agonist Yan 7874 is a weak agonist of orexin/hypocretin receptors and shows orexin receptor-independent cytotoxicity
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. As test system we utilized human OX1 and OX2...
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ژورنال
عنوان ژورنال: Clinical Science
سال: 2018
ISSN: 0143-5221,1470-8736
DOI: 10.1042/cs20180150