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An orexin receptor antagonist, or orexin antagonist, is a drug that inhibits the effect of orexin by acting as a receptor antagonist of one (selective orexin receptor antagonist or SORA) or both (dual orexin receptor antagonis or DORA) of the orexin receptors, OX 1 and OX 2. [1] Medical applications include treatment of sleep disorders such as ...
Orexin (/ ɒ ˈ r ɛ k s ɪ n /), also known as hypocretin, is a neuropeptide that regulates arousal, wakefulness, and appetite. [5] It exists in the forms of orexin-A and orexin-B.The most common form of narcolepsy, type 1, in which the individual experiences brief losses of muscle tone ("drop attacks" or cataplexy), is caused by a lack of orexin in the brain due to destruction of the cells ...
An orexigenic, or appetite stimulant, is a drug, hormone, or compound that increases appetite and may induce hyperphagia.This can be a medication or a naturally occurring neuropeptide hormone, such as ghrelin, orexin or neuropeptide Y, [1] [2] which increases hunger and therefore enhances food consumption.
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Preclinical research has suggested that orexin antagonists may reduce appetite, but daridorexant and other orexin antagonists have not been associated with weight loss in clinical trials. [16] Daridorexant may have a small risk of suicidal ideation. [26] Orexin receptor antagonists can affect the reward system and produce drug-liking responses ...
Side effects of lemborexant include somnolence, fatigue, headache, and abnormal dreams. [3] [8] The medication is a dual orexin receptor antagonist (DORA). [3] [8] It acts as a selective dual antagonist of the orexin receptors OX 1 and OX 2. [3] [8] Lemborexant has a long elimination half-life of 17 to 55 hours and a time to peak of about 1 to ...
However, orexin-B shows a 5- to 10-fold selectivity for orexin receptor type 2, whilst orexin-A is equipotent at both receptors. [2] [3] Several orexin receptor antagonists are in development for potential use in sleep disorders. [4] The first of these, suvorexant, has been on the market in the United States since 2015. [5]
Orexins strongly excite various brain nuclei to affect an organism's wakefulness by affecting their dopamine, norepinephrine, histamine and acetylcholine systems. [3] These systems work together to stabilize the organism's sleep cycles. Once made, the orexin peptides can bind to the orexin receptor; which is a G protein-coupled receptor. This ...