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| Formula | C22H25F3N2O4S |
| Molar mass | 470.51 g·mol−1 |
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Firazorexton (INN) is an experimental orexin 2 (OX2) receptor agonist first described in a 2019 patent filed by Takeda Pharmaceutical Company. [1] [2]
Azapirones are a class of drugs used as anxiolytics, antidepressants, and antipsychotics. They are commonly used as add-ons to other antidepressants, such as selective serotonin reuptake inhibitors (SSRIs).
Etoperidone, associated with several brand names, is an atypical antidepressant which was developed in the 1970s and either is no longer marketed or was never marketed. It is a phenylpiperazine related to trazodone and nefazodone in chemical structure and is a serotonin antagonist and reuptake inhibitor (SARI) similarly to them.
The orexin receptor (also referred to as the hypocretin receptor) is a G-protein-coupled receptor that binds the neuropeptide orexin. There are two variants, OX1 and OX2, each encoded by a different gene (HCRTR1, HCRTR2).
Orexin receptor type 2 (Ox2R or OX2), also known as hypocretin receptor type 2 (HcrtR2), is a protein that in humans is encoded by the HCRTR2 gene.
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, which increases hunger and therefore enhances food consumption. Usually appetite enhancement is considered an undesirable side effect of certain drugs as it leads to unwanted weight gain, but sometimes it can be beneficial and a drug may be prescribed solely for this purpose, especially when the patient is suffering from severe appetite loss or muscle wasting due to cystic fibrosis, anorexia, old age, cancer or AIDS. There are several widely used drugs which can cause a boost in appetite, including tricyclic antidepressants (TCAs), tetracyclic antidepressants, natural or synthetic cannabinoids, first-generation antihistamines, most antipsychotics and many steroid hormones. In the United States, no hormone or drug has currently been approved by the FDA specifically as an orexigenic, with the exception of Dronabinol, which received approval for HIV/AIDS-induced anorexia only.
Eugeroics, also known as wakefulness-promoting agents and wakefulness-promoting drugs, are a class of drugs that promote wakefulness and alertness. They are medically indicated for the treatment of certain sleep disorders including excessive daytime sleepiness (EDS) in narcolepsy or obstructive sleep apnea (OSA). Eugeroics are also often prescribed off-label for the treatment of EDS in idiopathic hypersomnia, a rare and often debilitating sleep disorder which currently has no official treatments approved by the Food and Drug Administration (FDA). In contrast to classical psychostimulants, such as methylphenidate and amphetamine, which are also used in the treatment of these disorders, eugeroics typically do not produce euphoria, and, consequently, have a lower addictive potential.
Osemozotan (MKC-242) is a selective 5-HT1A receptor agonist with some functional selectivity, acting as a full agonist at presynaptic and a partial agonist at postsynaptic 5-HT1A receptors. 5-HT1A receptor stimulation influences the release of various neurotransmitters including serotonin, dopamine, norepinephrine, and acetylcholine. 5-HT1A receptors are inhibitory G protein-coupled receptor. Osemozotan has antidepressant, anxiolytic, antiobsessional, serenic, and analgesic effects in animal studies, and is used to investigate the role of 5-HT1A receptors in modulating the release of dopamine and serotonin in the brain, and their involvement in addiction to abused stimulants such as cocaine and methamphetamine.
Melatonin receptor agonists are analogues of melatonin that bind to and activate the melatonin receptor. Agonists of the melatonin receptor have a number of therapeutic applications including treatment of sleep disorders and depression. The discovery and development of melatonin receptor agonists was motivated by the need for more potent analogues than melatonin, with better pharmacokinetics and longer half-life. Melatonin receptor agonists were developed with the melatonin structure as a model.
Motesanib is an experimental drug candidate originally developed by Amgen but later investigated by the Takeda Pharmaceutical Company. It is an orally administered small molecule belonging to angiokinase inhibitor class which acts as an antagonist of VEGF receptors, platelet-derived growth factor receptors, and stem cell factor receptors. It is used as the phosphate salt motesanib diphosphate. After clinical trials in thyroid cancer, non-small cell lung cancer, gastrointestinal stromal cancer, colorectal cancer, and breast cancer, the drug was not found to show sufficient efficacy for further development, and development was abandoned by Takeda.
Brigatinib, sold under the brand name Alunbrig among others, is a small-molecule targeted cancer therapy being developed by ARIAD Pharmaceuticals, Inc. Brigatinib acts as both an anaplastic lymphoma kinase (ALK) and epidermal growth factor receptor (EGFR) inhibitor.
Suvorexant, sold under the trade name Belsomra, is an orexin antagonist medication for the treatment of insomnia. It is effective for insomnia, at least for four weeks and as compared to a placebo.
Filorexant (INN, USAN) (code name MK-6096) is an orexin antagonist which is or was under development by Merck for the treatment of insomnia. It is a dual antagonist of the OX1 and OX2 receptors. As of March 2014, filorexant has completed phase II clinical trials. It was also investigated as a migraine prophylaxis, but was not found effective, and in major depressive disorder and painful diabetic neuropathy. As of May 2015, filorexant is no longer listed on Merck's online development pipeline.
Naltalimide (INN) (code name TRK-130, formerly TAK 363) is a novel, centrally-acting opioid drug which is under development by Takeda and Toray for the treatment of overactive bladder/urinary incontinence. It acts as a potent and selective partial agonist of the μ-opioid receptor (Ki = 0.268 nM, EC50 = 2.39 nM, Emax = 66.1%) over the δ-opioid (Ki = 121 nM, EC50 = 26.1 nM, Emax = 71.0%) and κ-opioid receptors (Ki = 8.97 nM, EC50 = 9.51 nM, Emax = 62.6%). Notably, naltalimide somehow appears to lack certain undesirable side effects such as constipation seen with other μ-opioid receptor agonists such as morphine. It enhances bladder storage via suppression of the afferent limb of the micturition reflex pathway.
Lemborexant, sold under the brand name Dayvigo, is a medication for the treatment of insomnia characterized by difficulties with sleep onset and/or sleep maintenance in adults. Lemborexant was approved in the United States for use by adults with insomnia in December 2019.
Daridorexant, sold under the brand name Quviviq, is an orexin antagonist medication that is used for the treatment of insomnia. It is taken by mouth.
Vibegron, sold under the brand name Gemtesa, is a medication for the treatment of overactive bladder.
Danavorexton is a selective orexin 2 receptor agonist. As of March 2021, danavorexton is under investigation for the treatment of narcolepsy, idiopathic hypersomnia, and sleep apnea.
TAK-994 is an orexin receptor agonist which is under development by Takeda for the treatment of narcolepsy. It is a small-molecule and orally active compound and acts as a highly selective agonist of the orexin receptor 2 (OX2) (>700-fold selectivity over the orexin receptor 1 (OX1)). It reached phase 2 clinical trials for narcolepsy but clinical trials were paused in October 2021 for safety reasons. The chemical structure of TAK-994 has yet to be disclosed.
Suntinorexton (INN) is an experimental orexin receptor agonist.. It acts as a selective agonist of the orexin OX2 receptor and was described in 2019 in a patent by Takeda Pharmaceutical Company.
Omidenepag isopropyl is a pharmaceutical drug used for the treatment of glaucoma and ocular hypertension.
Proposed INN: List 123
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