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Itameline
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| Clinical data | |
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| Other names | RU-47213; RU47213 |
| Drug class | Non-selective muscarinic acetylcholine receptor agonist |
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| Chemical and physical data | |
| Formula | C14H15ClN2O3 |
| Molar mass | 294.74 g·mol−1 |
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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
[edit]- ^ "Delving into the Latest Updates on Itameline with Synapse". Synapse. 28 September 2024. Retrieved 26 October 2024.
- ^ a b c d M'Harzi M, Willig F, Gieules C, Palou AM, Oberlander C, Barzaghi F (April 1997). "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. doi:10.1016/s0091-3057(96)00423-6. PMID 9130292.
- ^ a b c Toja E, Bonetti C, Butti A, Hunt P, Fortin M, Barzaghi F, et al. (1992). "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. 27 (5). Elsevier BV: 519–526. doi:10.1016/0223-5234(92)90186-5. ISSN 0223-5234.
- ^ a b Froestl W, Muhs A, Pfeifer A (2012). "Cognitive enhancers (nootropics). Part 1: drugs interacting with receptors". Journal of Alzheimer's Disease. 32 (4): 793–887. doi:10.3233/JAD-2012-121186. PMID 22886028.
- ^ Fischer F, Matthisson M, Herrling P (2004). "List of drugs in development for neurodegenerative diseases". Neuro-Degenerative Diseases. 1 (1): 50–70. doi:10.1159/000077879. PMID 16908974.
- ^ a b c d Camps P, Muñoz-Torrero D (February 2002). "Cholinergic drugs in pharmacotherapy of Alzheimer's disease". Mini Reviews in Medicinal Chemistry. 2 (1): 11–25. doi:10.2174/1389557023406638. PMID 12369954.
- ^ a b c d Saklani A, Kutty SK (February 2008). "Plant-derived compounds in clinical trials". Drug Discovery Today. 13 (3–4): 161–171. doi:10.1016/j.drudis.2007.10.010. PMID 18275914.
- ^ Palma JA (February 2024). "Muscarinic control of cardiovascular function in humans: a review of current clinical evidence". Clinical Autonomic Research. 34 (1): 31–44. doi:10.1007/s10286-024-01016-5. PMC 10994193. PMID 38305989.
- ^ Korczyn AD (October 2000). "Muscarinic M(1) agonists in the treatment of Alzheimer's disease". Expert Opinion on Investigational Drugs. 9 (10): 2259–2267. doi:10.1517/13543784.9.10.2259. PMID 11060805.
- ^ Deiana S, Platt B, Riedel G (August 2011). "The cholinergic system and spatial learning". Behavioural Brain Research. 221 (2): 389–411. doi:10.1016/j.bbr.2010.11.036. PMID 21108971.
- ^ Mirza NR, Peters D, Sparks RG (2003). "Xanomeline and the antipsychotic potential of muscarinic receptor subtype selective agonists". CNS Drug Reviews. 9 (2): 159–186. doi:10.1111/j.1527-3458.2003.tb00247.x. PMC 6741650. PMID 12847557.
- ^ Eglen RM, Hegde SS (1998). "Selective modulation of muscarinic receptor subtypes: therapeutic potential". Emerging Drugs. 3 (1). Informa Healthcare: 67–80. doi:10.1517/14728214.3.1.67. ISSN 1361-9195.