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Aripiprazole, sold under the brand names Abilify and Aristada, among others, is an atypical antipsychotic. It is primarily used in the treatment of schizophrenia, obsessive compulsive disorder (OCD), and bipolar disorder; other uses include as an add-on treatment in major depressive disorder, tic disorders, and irritability associated with autism. Aripiprazole is taken by mouth or via injection into a muscle. A Cochrane review found low-quality evidence of effectiveness in treating schizophrenia.
Muscarinic acetylcholine receptors, or mAChRs, are acetylcholine receptors that form G protein-coupled receptor complexes in the cell membranes of certain neurons and other cells. They play several roles, including acting as the main end-receptor stimulated by acetylcholine released from postganglionic fibers in the parasympathetic nervous system.
Aceclidine is a parasympathomimetic miotic agent used in the treatment of narrow angle glaucoma.
Amisulpride is an antiemetic and antipsychotic medication used at lower doses intravenously to prevent and treat postoperative nausea and vomiting; and at higher doses by mouth to treat schizophrenia and acute psychotic episodes. It is sold under the brand names Barhemsys and Solian, Socian, Deniban and others. At very low doses it is also used to treat dysthymia.
A muscarinic agonist is an agent that activates the activity of the muscarinic acetylcholine receptor. The muscarinic receptor has different subtypes, labelled M1-M5, allowing for further differentiation.
Propiomazine, sold under the brand name Propavan among others, is an antihistamine which is used to treat insomnia and to produce sedation and relieve anxiety before or during surgery or other procedures and in combination with analgesics as well as during labor. Propiomazine is a phenothiazine, but is not used therapeutically as a neuroleptic because it does not block dopamine receptors well.
A muscarinic receptor antagonist (MRA) is a type of anticholinergic agent that blocks the activity of the muscarinic acetylcholine receptor. The muscarinic receptor is a protein involved in the transmission of signals through certain parts of the nervous system, and muscarinic receptor antagonists work to prevent this transmission from occurring. Notably, muscarinic antagonists reduce the activation of the parasympathetic nervous system. The normal function of the parasympathetic system is often summarised as "rest-and-digest", and includes slowing of the heart, an increased rate of digestion, narrowing of the airways, promotion of urination, and sexual arousal. Muscarinic antagonists counter this parasympathetic "rest-and-digest" response, and also work elsewhere in both the central and peripheral nervous systems.
The muscarinic acetylcholine receptor M4, also known as the cholinergic receptor, muscarinic 4 (CHRM4), is a protein that, in humans, is encoded by the CHRM4 gene.
Xanomeline is a small molecule muscarinic acetylcholine receptor agonist that was first synthesized in a collaboration between Eli Lilly and Novo Nordisk as an investigational therapeutic being studied for the treatment of central nervous system disorders.
Vedaclidine (INN, codenamed LY-297,802, NNC 11-1053) is an experimental analgesic drug which acts as a mixed agonist–antagonist at muscarinic acetylcholine receptors, being a potent and selective agonist for the M1 and M4 subtypes, yet an antagonist at the M2, M3 and M5 subtypes. It is orally active and an effective analgesic over 3× the potency of morphine, with side effects such as salivation and tremor only occurring at many times the effective analgesic dose. Human trials showed little potential for development of dependence or abuse, and research is continuing into possible clinical application in the treatment of neuropathic pain and cancer pain relief.
Pimavanserin, sold under the brand name Nuplazid, is an atypical antipsychotic which is approved for the treatment of Parkinson's disease psychosis and is also being studied for the treatment of Alzheimer's disease psychosis, schizophrenia, agitation, and major depressive disorder. Unlike other antipsychotics, pimavanserin is not a dopamine receptor antagonist.
Aripiprazole/sertraline is a combination formulation of aripiprazole (Abilify), an atypical antipsychotic, and sertraline (Zoloft), a selective serotonin reuptake inhibitor (SSRI), which was under development by Otsuka Pharmaceutical for the treatment of major depressive disorder (MDD). It combines serotonin reuptake inhibition from sertraline and modulation of dopamine and serotonin receptors from aripiprazole. In July 2017, it was in preregistration in Japan for the treatment of MDD. However, in September 2018, the regulatory submission in Japan for MDD was withdrawn.
Hypidone (developmental code name YL-0919) is an investigational serotonergic antidepressant which is under development for the treatment of major depressive disorder. It acts as a serotonin reuptake inhibitor, 5-HT1A receptor partial agonist, and 5-HT6 receptor full agonist. It is used as the hydrochloride salt. As of January 2021, hypidone is in phase 2 clinical trials for major depressive disorder.
KarXT is an investigational oral dual-drug fixed-dose combination of xanomeline and trospium. It is undergoing a phase 3 clinical trial for the treatment of schizophrenia. Xanomeline is a functionally preferring muscarinic M4 and M1 receptor agonist that readily passes into the central nervous system (CNS) to stimulate these receptors in key areas of the brain. Trospium is a non-selective muscarinic antagonist that does not cross into the CNS and reduces peripheral cholinergic side effects associated with xanomeline.
References
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- ↑ "Pomaglumetad methionil - Denovo Biopharma/Eli Lilly and Company - AdisInsight". adisinsight.springer.com. Springer. Retrieved 14 February 2020.
- ↑ "Emraclidine - Cerevel Therapeutics - AdisInsight". adisinsight.springer.com. Retrieved 2023-02-15.
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- ↑ "Cannabidiol - GW Pharmaceuticals - AdisInsight". adisinsight.springer.com. Springer. Retrieved 14 February 2020.
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- ↑ "Deudextromethorphan - Avanir Pharmaceuticals - AdisInsight". adisinsight.springer.com. Springer. Retrieved 14 February 2020.
- ↑ Nguyen, Linda; Thomas, Kelan L.; Lucke-Wold, Brandon P.; Cavendish, John Z.; Crowe, Molly S.; Matsumoto, Rae R. (March 2016). "Dextromethorphan: An update on its utility for neurological and neuropsychiatric disorders". Pharmacology & Therapeutics. 159: 1–22. doi:10.1016/j.pharmthera.2016.01.016. ISSN 1879-016X. PMID 26826604.
- ↑ "Roluperidone - Minerva Neurosciences - AdisInsight". adisinsight.springer.com. Springer. Retrieved 14 February 2020.
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- ↑ "Evenamide - Newron Pharmaceuticals - AdisInsight". adisinsight.springer.com. Springer. Retrieved 14 February 2020.
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- ↑ Vijeepallam, K.; Pandy, V.; Kunasegaran, T.; Murugan, D. D.; Naidu, M. (2016). "Mitragyna speciosa Leaf Extract Exhibits Antipsychotic-Like Effect with the Potential to Alleviate Positive and Negative Symptoms of Psychosis in Mice". Frontiers in Pharmacology. 7: 464. doi: 10.3389/fphar.2016.00464 . PMC 5138496 . PMID 27999544.
- ↑ Johnson, L. E.; Balyan, L.; Magdalany, A.; Saeed, F.; Salinas, R.; Wallace, S.; Veltri, C. A.; Swogger, M. T.; Walsh, Z.; Grundmann, O. (2020). "The Potential for Kratom as an Antidepressant and Antipsychotic". The Yale Journal of Biology and Medicine. 93 (2): 283–289. PMC 7309668 . PMID 32607089.