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Orexin receptors: Targets and applications

Fundamental & Clinical Pharmacology, 2021
AbstractOver the years, elucidating targets from the neural circuits that can be used to treat disorders pertaining to the nervous system and extending their scope to other systems have always proved interesting to researchers. The role of various peptides and neurotransmitters has been elucidated and is being developed as therapeutic targets.
Subhiksha Subramanian   +1 more
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Selective orexin receptor antagonists

Bioorganic & Medicinal Chemistry Letters, 2013
The orexin, or hypocretin, neuropeptides (orexin-A and orexin-B) are produced on neurons in the hypothalamus which project to key areas of the brain that control sleep-wake states, modulation of food intake, panic, anxiety, emotion, reward and addictive behaviors.
Terry P, Lebold   +2 more
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A molecular network map of orexin-orexin receptor signaling system

Journal of Cell Communication and Signaling, 2022
Orexins are excitatory neuropeptides, which are predominantly associated with feeding behavior, sleep-wake cycle and energy homeostasis. The orexinergic system comprises of HCRTR1 and HCRTR2, G-protein-coupled receptors of rhodopsin family and the endogenous ligands processed from HCRT pro-hormone, Orexin A and Orexin B.
Oishi Chatterjee   +9 more
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Orexin Receptor Antagonists

Pharmaceutical Patent Analyst, 2012
The orexin neuropeptides bind to two G protein-coupled receptors, orexin-1 and -2. Small-molecule antagonism of the receptors has potential therapeutic utility in a number of areas, most notably insomnia, for which the most advanced dual orexin receptor antagonist has now completed clinical trials.
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Structure−Activity Studies of Orexin A and Orexin B at the Human Orexin 1 and Orexin 2 Receptors Led to Orexin 2 Receptor Selective and Orexin 1 Receptor Preferring Ligands

Journal of Medicinal Chemistry, 2004
The neuropeptides orexin A and B (also known as hypocretins) play an important role in many physiological and behavioral activities. Orexins are ligands of two closely related G-protein-coupled receptors, that are the named orexin 1 and orexin 2 receptors. To clearly identify the minimal ligand sequences required for receptor activation, we synthesized
Manja, Lang   +4 more
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Orexins Activate Histaminergic Neurons via the Orexin 2 Receptor

Biochemical and Biophysical Research Communications, 2002
Orexins (orexin A and B) are recently identified neuropeptides implicated in the regulation of vigilance states and energy homeostasis. We have shown here the physiological significance of histaminergic neurons in the orexin-induced arousal responses. Immunohistochemical and electron microscopic techniques revealed direct synaptic interaction between ...
Akihiro, Yamanaka   +9 more
openaire   +2 more sources

Chimeric, mutant orexin receptors show key interactions between orexin receptors, peptides and antagonists

European Journal of Pharmacology, 2011
Orexin receptor antagonists are being investigated as therapeutic agents for insomnia and addictive disorders. In this study the interactions between the orexin receptors (orexin 1 receptor and orexin 2 receptor), orexin peptides, and small molecule orexin antagonists were explored.
Da-Thao, Tran   +8 more
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Orexins and orexin receptors: implication in feeding behavior

Regulatory Peptides, 1999
Orexin-A and -B are initially identified as endogenous ligands for an orphan G protein coupled receptor. Since the discovery of orexins, investigations of their functions have been guided by their distribution in the lateral hypothalamic area, which has been implicated in feeding behavior.
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Orexins/hypocretins and orexin receptors in apoptosis: a mini‐review

Acta Physiologica, 2010
AbstractAn unexpected and fascinating aspect of the neuropeptides orexins has recently emerged when it was shown that orexins acting at orexin receptors OX1R or OX2R induce dramatic apoptosis resulting in massive reduction in cell growth in various cancer cell lines.
M, Laburthe, T, Voisin, A, El Firar
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Sleep, feeding, and neuropeptides: roles of orexins and orexin receptors

Current Opinion in Neurobiology, 2002
Recent studies using molecular genetics in mice and dogs, as well as histopathological analyses of human disease, have come to the same conclusion: the human sleep disorder narcolepsy is caused by failure of signaling mediated by orexin (hypocretin) neuropeptides. These and other findings strongly suggest that the orexin system plays a critical role in
Michihiro, Mieda, Masashi, Yanagisawa
openaire   +2 more sources

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