Lemborexant, a dual
orexin receptor antagonist, is Eisai's in-house discovered and developed small molecule compound that inhibits
orexin neurotransmission by binding competitively to the two subtypes of
orexin receptors (
orexin receptor 1 and 2).
Lemborexant, a dual
orexin receptor antagonist, is an in-house discovered novel small molecule which inhibits
orexin by binding competitively to two subtypes of
orexin receptors (
orexin receptor 1 and 2).
The cause of this overactivity is not clear but may be driven by certain adipokines, signaling cytokines produced by adipose tissue (including
orexin, leptin, free fatty acids, tumor necrosis factor, interleukin-6, C-reactive protein, angiotensinogen, and adiponectin).
2011), we named the three candidates Air-CCAPR1-Like (similar to cardioacceleratory peptide receptor), Air-AAR1-Like (similar to allatostatin-A receptor), and Air-OX2R1-Like (similar to
orexin receptor type 2).
Orexin A is 33 amino acid long and has two intrachain disulfide bonds while
Orexin B is a linear 28 amino acid residue peptide.
The nonbenzodiazepine hypnotics eszopiclone and Zolpidem as well as the
orexin receptor antagonist suvorexant improved short-term sleep quality, though the effect was small and there was significant evidence of harm as described above.
Table 1 11 Pharmacological domains Acetylcholine Dopamine GABA Glutamate Histamine Ion channel Melatonin Norepinephrine Opioid
Orexin Serotonin Table 2 9 Modes of action Enzyme inhibitor Enzyme modulator Ion channel blocker Neurotransmitters releaser Positive allosteric modulator Receptor agonist Receptor antagonist Receptor partial agonist Reuptake inhibitor
US Food and Drug Administration (FDA)-approved hypnotic medications fall into 5 families (TABLE 2(40)): benzodiazepines (BDZs), benzodiazepine agonists (BDZAs, sometimes called "Z drugs"), melatonin agonists (eg, ramelteon), tricyclic antidepressants (eg, low-dose doxepin), and
orexin antagonists (eg, suvorexant).
Impaired
orexin receptor expression in the Kolliker-Fuse nucleus in sudden infant death syndrome: possible involvement of this nucleus in arousal pathophysiology.
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Orexins--also known as hypocretins, are neuropeptides synthesized in the posterolateral hypothalamus, and are represented by
Orexin A and
Orexin B.
The hypothalamic neuropeptide
orexin is released into the accumbens and SB334867, an
orexin-1 receptor antagonist, inhibits relapse in rodents.
