Chemistry:Itameline
Itameline (INN; developmental code name RU-47213) is a non-selective muscarinic acetylcholine receptor agonist which was under development for the treatment of Alzheimer's disease and memory disorders but was never marketed.[1][2][3] It has been referred to as a "nootropic" (cognitive enhancer).[4][5]
Itameline is a prodrug of RU-35963, an arecoline derivative.[6][7][2] It is an agonist of the muscarinic acetylcholine M1 receptor as well as of other muscarinic acetylcholine receptors.[8][6][9][7][2] Itameline is described as being superior to arecoline in terms of potency, central selectivity, and duration of action.[6][7] The drug shows antiamnesic effects in animals, for instance reversing scopolamine-induced memory deficits.[10][6][2][3] Structurally, it is a tetrahydropyridine similarly to xanomeline and milameline.[11]
Itameline was first described in the scientific literature by 1992.[3] It was under development by Hoechst Marion Roussel and reached phase 2 clinical trials by 1998 prior to the discontinuation of its development.[12][7][4]
References
- ↑ "Delving into the Latest Updates on Itameline with Synapse". 28 September 2024. https://synapse.patsnap.com/drug/e7be391dec4d43a0bfe0b96f9710de80.
- ↑ 2.0 2.1 2.2 2.3 "Ameliorating effects of RU 47213, a novel oral and long-lasting cholinomimetic agent, on working memory impairments in rats". Pharmacology, Biochemistry, and Behavior 56 (4): 663–668. April 1997. doi:10.1016/s0091-3057(96)00423-6. PMID 9130292.
- ↑ 3.0 3.1 3.2 "1-substituted-1,2,5,6-tetrahydropyridine-3-carboxaldehyde-O-alkyloximes as novel orally active and long-lasting muscarinic cholinergic agonists". European Journal of Medicinal Chemistry (Elsevier BV) 27 (5): 519–526. 1992. doi:10.1016/0223-5234(92)90186-5. ISSN 0223-5234.
- ↑ 4.0 4.1 "Cognitive enhancers (nootropics). Part 1: drugs interacting with receptors". Journal of Alzheimer's Disease 32 (4): 793–887. 2012. doi:10.3233/JAD-2012-121186. PMID 22886028.
- ↑ "List of drugs in development for neurodegenerative diseases". Neuro-Degenerative Diseases 1 (1): 50–70. 2004. doi:10.1159/000077879. PMID 16908974.
- ↑ 6.0 6.1 6.2 6.3 "Cholinergic drugs in pharmacotherapy of Alzheimer's disease". Mini Reviews in Medicinal Chemistry 2 (1): 11–25. February 2002. doi:10.2174/1389557023406638. PMID 12369954.
- ↑ 7.0 7.1 7.2 7.3 "Plant-derived compounds in clinical trials". Drug Discovery Today 13 (3–4): 161–171. February 2008. doi:10.1016/j.drudis.2007.10.010. PMID 18275914.
- ↑ "Muscarinic control of cardiovascular function in humans: a review of current clinical evidence". Clinical Autonomic Research 34 (1): 31–44. February 2024. doi:10.1007/s10286-024-01016-5. PMID 38305989.
- ↑ "Muscarinic M(1) agonists in the treatment of Alzheimer's disease". Expert Opinion on Investigational Drugs 9 (10): 2259–2267. October 2000. doi:10.1517/13543784.9.10.2259. PMID 11060805.
- ↑ "The cholinergic system and spatial learning". Behavioural Brain Research 221 (2): 389–411. August 2011. doi:10.1016/j.bbr.2010.11.036. PMID 21108971.
- ↑ "Xanomeline and the antipsychotic potential of muscarinic receptor subtype selective agonists". CNS Drug Reviews 9 (2): 159–186. 2003. doi:10.1111/j.1527-3458.2003.tb00247.x. PMID 12847557.
- ↑ "Selective modulation of muscarinic receptor subtypes: therapeutic potential". Emerging Drugs (Informa Healthcare) 3 (1): 67–80. 1998. doi:10.1517/14728214.3.1.67. ISSN 1361-9195.
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