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Orexin Receptor Antagonist
An orexin receptor antagonist, or orexin antagonist, is a drug that inhibits the effect of orexin by acting as a receptor antagonist of one or both of the orexin receptors, OX1 and OX2. Medical applications include treatment of sleep disorders such as insomnia. Examples Marketed * Daridorexant (nemorexant; Quviviq) – dual OX1 and OX2 antagonist – approved for insomnia in January 2022, formerly under development for sleep apnea – half-life 8 hours * Lemborexant (Dayvigo) – dual OX1 and OX2 antagonist – approved for insomnia in December 2019 and released June 1 2020, under development for circadian rhythm sleep disorders, chronic obstructive pulmonary disease, and sleep apnea – half-life 17–55 hours * Suvorexant (Belsomra) – dual OX1 and OX2 antagonist – approved for insomnia in August 2014, under development for delirium – half-life 12 hours Under development * Seltorexant (MIN-202, JNJ-42847922, JNJ-922) – selective OX2 antagonist – under development ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Orexin
Orexin (), also known as hypocretin, is a neuropeptide that regulates arousal, wakefulness, and appetite. 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 that produce it.Stanford Center for NarcolepsFAQ(retrieved 27-Mar-2012) It exists in the forms of Orexin-A and Orexin-B. There are 50,000–80,000 orexin-producing neurons in the human brain, located predominantly in the perifornical area and lateral hypothalamus. They project widely throughout the central nervous system, regulating wakefulness, feeding, and other behaviours. There are two types of orexin peptide and two types of orexin receptor. Orexin was discovered in 1998 almost simultaneously by two independent groups of researchers working on the rat brain. One group named it orexin, from ''orexis,'' meaning "appetite" in Greek; the other group named it ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
JNJ-10397049
JNJ-10397049 is a potent and highly selective OX2 receptor antagonist. In animals, JNJ-10397049 was found to have sleep-promoting effects and to attenuate the reinforcing effects of ethanol Ethanol (abbr. EtOH; also called ethyl alcohol, grain alcohol, drinking alcohol, or simply alcohol) is an organic compound. It is an alcohol with the chemical formula . Its formula can be also written as or (an ethyl group linked to a .... References Bromoarenes Dioxanes Orexin antagonists Ureas {{Sedative-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Network Meta-analysis
A meta-analysis is a statistical analysis that combines the results of multiple scientific studies. Meta-analyses can be performed when there are multiple scientific studies addressing the same question, with each individual study reporting measurements that are expected to have some degree of error. The aim then is to use approaches from statistics to derive a pooled estimate closest to the unknown common truth based on how this error is perceived. Meta-analytic results are considered the most trustworthy source of evidence by the evidence-based medicine literature.Herrera Ortiz AF., Cadavid Camacho E, Cubillos Rojas J, Cadavid Camacho T, Zoe Guevara S, Tatiana Rincón Cuenca N, Vásquez Perdomo A, Del Castillo Herazo V, & Giraldo Malo R. A Practical Guide to Perform a Systematic Literature Review and Meta-analysis. Principles and Practice of Clinical Research. 2022;7(4):47–57. https://doi.org/10.21801/ppcrj.2021.74.6 Not only can meta-analyses provide an estimate of the unk ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Sleep Quality
Sleep is a sedentary state of mind and body. It is characterized by altered consciousness, relatively inhibited Perception, sensory activity, reduced muscle activity and reduced interactions with surroundings. It is distinguished from wakefulness by a decreased ability to react to stimulus (physiology), stimuli, but more reactive than a coma or disorders of consciousness, with sleep displaying different, active brain patterns. Sleep occurs in sleep cycle, repeating periods, in which the body alternates between two distinct modes: REM sleep and non-rapid eye movement sleep, non-REM sleep. Although REM stands for "rapid eye movement", this mode of sleep has many other aspects, including virtual paralysis of the body. dream, Dreams are a succession of images, ideas, emotions, and sensations that usually occur involuntarily in the mind during certain stages of sleep. During sleep, most of the human body, body's systems are in an anabolic state, helping to restore the Immunity (medi ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Total Sleep Time
Sleep is a sedentary state of mind and body. It is characterized by altered consciousness, relatively inhibited sensory activity, reduced muscle activity and reduced interactions with surroundings. It is distinguished from wakefulness by a decreased ability to react to stimuli, but more reactive than a coma or disorders of consciousness, with sleep displaying different, active brain patterns. Sleep occurs in repeating periods, in which the body alternates between two distinct modes: REM sleep and non-REM sleep. Although REM stands for "rapid eye movement", this mode of sleep has many other aspects, including virtual paralysis of the body. Dreams are a succession of images, ideas, emotions, and sensations that usually occur involuntarily in the mind during certain stages of sleep. During sleep, most of the body's systems are in an anabolic state, helping to restore the immune, nervous, skeletal, and muscular systems; these are vital processes that maintain mood, memory, an ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Sleep Efficiency
Sleep efficiency (SE) is the ratio between the time a person spends asleep, and the total time dedicated to sleep (i.e. both sleeping and attempting to fall asleep or fall back asleep). It is given as a percentage. SE of 80% or more is considered normal/healthy with most young healthy adults displaying SE above 90%. SE can be determined with a polysomnograph and is an important parameter of a sleep study. Sleep efficiency is often described as the ratio between time spent asleep ("total sleep time (TST)"), and time spent "in bed" ("time in bed (TIB)"), however, TIB does not encompass "non-sleep-related activities" performed in bed (e.g. reading, watching television, etc.) as the phrase may seem to suggest. Clinical significance Apparently long sleep duration may in fact be a sign of low sleep efficiency. SE is significantly reduced in insomnia; SE is therefore an important clinical parameter in clinical investigations of insomnia. SE declines with age and low SE is common in the ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Wake After Sleep Onset
Middle-of-the-night insomnia (MOTN) is characterized by having difficulty returning to sleep after waking up during the night or very early in the morning. This kind of insomnia (sleeplessness) is different from initial or sleep-onset insomnia, which consists of having difficulty falling asleep at the beginning of sleep. The disrupted sleep patterns caused by middle-of-the-night insomnia make many sufferers of the condition complain of fatigue the following day. Excessive daytime sleepiness is reported nearly two times higher by individuals with nocturnal awakenings than by people who sleep through the night. Sleep research conducted in the 1990s showed that such waking up during the night may be a natural sleep pattern, rather than a form of insomnia. If interrupted sleep (called "biphasic sleeping" or " bimodal sleep") is perceived as normal and not referred to as "insomnia", less distress is caused and a return to sleep usually occurs after about one hour. Causes * Pain * Pr ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Latency To Persistent Sleep
In sleep science, sleep onset latency (SOL) is the length of time that it takes to accomplish the transition from full wakefulness to sleep, normally to the lightest of the non-REM sleep stages. Sleep latency studies Pioneering Stanford University sleep researcher William C. Dement reports early development of the concept, and of the first test for it, the Multiple Sleep Latency Test (MSLT), in his book ''The Promise of Sleep''. Dement and colleagues including Mary Carskadon had been seeking an objective measure of daytime sleepiness to help assess the effects of sleep disorders. In the course of evaluating experimental results, they realized that the amount of time it took to fall asleep in bed was closely linked to the subjects' own self-evaluated level of sleepiness. "This may not seem like an earthshaking epiphany, but conceiving and developing an objective measure of sleepiness was perhaps one of the most important advances in sleep science," Dement and coauthor Christopher ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Dose Dependence
Dose or Dosage may refer to: Music * ''Dose'' (Gov't Mule album), 1998 * ''Dose'' (Latin Playboys album) * ''Dosage'' (album), by the band Collective Soul * "Dose" (song), a 2018 song by Ciara * "Dose", song by Filter from the album '' Short Bus'' Science * Dose (biochemistry), a measured quantity of a medicine, nutrient, or pathogen which is delivered as a unit. * Dosage form, a mixture of active and inactive components used to administer a medication * Dosing, feeding chemicals or medicines when used in small quantities * Effective dose (pharmacology), a dose or concentration of a drug that produces a biological response * Absorbed dose, a measure of energy deposited in matter from ionizing radiation *Equivalent dose, a measure of cancer/heritable health risk in tissue from ionizing radiation *Effective dose (radiation) Effective dose is a dose quantity in the International Commission on Radiological Protection (ICRP) system of radiological protection.ICRP publication, 1 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
TCS-OX2-29
TCS-OX2-29 is an orexin antagonist. It was the first non-peptide antagonist developed that is selective for the orexin receptor subtype OX2, with an IC50 of 40nM and selectivity of around 250x for OX2 over OX1 receptors. Orexin antagonists are expected to be useful for the treatment of insomnia, with subtype-selective antagonists such as TCS-OX2-29 potentially offering more specificity of action compared to non-selective orexin antagonists like almorexant Almorexant, also known by its development code ACT-078573, is an orexin antagonist, acting as a competitive antagonist of the OX1 and OX2 orexin receptors, which was being developed by the pharmaceutical companies Actelion and GSK for the treat .... References Carboxamides Orexin antagonists Norsalsolinol ethers 4-Pyridyl compounds Sedatives Tert-butyl compounds {{sedative-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
SB-408124
SB-408124 is a drug which is a non-peptide antagonist selective for the orexin receptor subtype OX1, with around 70x selectivity for OX1 over OX2 receptors, and improved oral bioavailability compared to the older OX1 antagonist SB-334867. It is used in scientific research into the function of orexinergic neurons in the body. References Orexin antagonists Fluoroarenes Quinolines Sedatives Ureas {{sedative-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Anorectic
An anorectic or anorexic is a drug which reduces appetite, resulting in lower food consumption, leading to weight loss. By contrast, an appetite stimulant is referred to as orexigenic. The term is (from the Greek ''ἀν-'' (an-) = "without" and ''ὄρεξις'' (órexis) = "appetite"), and such drugs are also known as anorexigenic, anorexiant, or appetite suppressant. History Used on a short-term basis clinically to treat obesity, some appetite suppressants are also available over-the-counter. Most common natural appetite suppressants are based on '' Hoodia'', a genus of 13 species in the flowering plant family Apocynaceae, under the subfamily Asclepiadoideae. Several appetite suppressants are based on a mix of natural ingredients, mostly using green tea as its basis, in combination with other plant extracts such as fucoxanthin, found naturally in seaweed. Drugs of this class are frequently stimulants of the phenethylamine family, related to amphetamine. The German and ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
