Disubstituted piperidines as potent orexin (hypocretin) receptor antagonists
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چکیده
منابع مشابه
OX1 and OX2 orexin/hypocretin receptor pharmacogenetics
Orexin/hypocretin peptide mutations are rare in humans. Even though human narcolepsy is associated with orexin deficiency, this is only extremely rarely due to mutations in the gene coding prepro-orexin, the precursor for both orexin peptides. In contrast, coding and non-coding variants of the OX1 and OX2 orexin receptors have been identified in many human populations; sometimes, these have bee...
متن کاملOrexin receptor antagonists as therapeutic agents for insomnia
Insomnia is a common clinical condition characterized by difficulty initiating or maintaining sleep, or non-restorative sleep with impairment of daytime functioning. Currently, treatment for insomnia involves a combination of cognitive behavioral therapy (CBTi) and pharmacological therapy. Among pharmacological interventions, the most evidence exists for benzodiazepine (BZD) receptor agonist dr...
متن کاملOrexin, orexin receptor antagonists and central cardiovascular control
Orexin makes an important contribution to the regulation of cardiovascular function. When injected centrally under anesthesia, orexin increases blood pressure, heart rate and sympathetic nerve activity. This is consistent with the location of orexin neurons in the hypothalamus and the distribution of orexin terminals in the central autonomic network. Thus, the two orexin receptors, Ox1R and Ox2...
متن کاملRunning title: Orexin (Hypocretin) Receptor Agonists and Antagonists for Treatment of Sleep Disorders Orexin (Hypocretin) Receptor Agonists and Antagonists for Treatment of Sleep Disorders Rationale for Development and Current Status
*KURAに登録されているコンテンツの利用については,著作権法に規定されている私的使用や引用などの範囲内で行ってください。 *著作権法に規定されている私的使用や引用などの範囲を超える利用を行う場合には,著作権者の許諾を得てください。ただし,著作権者 から著作権等管理事業者(学術著作権協会,日本著作出版権管理システムなど)に権利委託されているコンテンツの利用手続については ,各著作権等管理事業者に確認してください。 Title Orexin (Hypocretin) receptor agonists and antagonists for treatment of sleep disorders: Rationale for development and current status Author(s) Mieda, Michihiro; Sakurai, Takeshi Cita...
متن کاملCholecystokinin activates orexin/hypocretin neurons through the cholecystokinin A receptor.
Orexin A and B are neuropeptides implicated in the regulation of sleep/wakefulness and energy homeostasis. The regulatory mechanism of the activity of orexin neurons is not precisely understood. Using transgenic mice in which orexin neurons specifically express yellow cameleon 2.1, we screened for factors that affect the activity of orexin neurons (a total of 21 peptides and six other factors w...
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ژورنال
عنوان ژورنال: Bioorganic & Medicinal Chemistry Letters
سال: 2012
ISSN: 0960-894X
DOI: 10.1016/j.bmcl.2012.04.122