Synonyms: AF710B
Compound class:
Synthetic organic
Comment: ANAVEX 3-71 is an oral, small molecule dual agonist of the σ1 (SIGMAR1) and M1 muscarinic acetylcholine receptors. Based on structure we matched ANAVEX 3-71 to AF710B, which appears to be the active S enantiomer of racemic AF710, in US20110281903A1 [3]. AF710B is described as both a M1 partial agonist and positive allosteric modulator in this patent and in peer reviewed articles [2,4]. AF710B was originally investigated for disease-modifying potential in Alzhermer's disease [1-2,4-6].
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References |
1. Fadiran EO, Hammond E, Tran J, Missling CU, Ette E. (2024)
Population-Based Characterization of the Pharmacokinetics and Food Effect of ANAVEX3-71, a Novel Sigma-1 Receptor and Allosteric M1 Muscarinic Receptor Agonist in Development for Treatment of Frontotemporal Dementia, Schizophrenia, and Alzheimer Disease. Clin Pharmacol Drug Dev, 13 (1): 21-31. [PMID:38073274] |
2. Fadiran EO, Hammond E, Tran J, Xue H, Chen J, Kaufmann WE, Missling CU, Darpo B. (2023)
Concentration-QTc Relationship from a Single Ascending Dose Study of ANAVEX3-71, a Novel Sigma-1 Receptor and Allosteric M1 Muscarinic Receptor Agonist in Development for the Treatment of Frontotemporal Dementia, Schizophrenia, and Alzheimer's Disease. Clin Pharmacol Drug Dev, 12 (9): 888-901. [PMID:37515316] |
3. Fisher A, Bar-Ner N, Nachum V. (2011)
Bicyclic heterocyclic spiro compounds. Patent number: US20110281903A1. Assignee: Israel Institute for Biological Research. Priority date: 26/01/2010. Publication date: 17/11/2011. |
4. Fisher A, Bezprozvanny I, Wu L, Ryskamp DA, Bar-Ner N, Natan N, Brandeis R, Elkon H, Nahum V, Gershonov E et al.. (2016)
AF710B, a Novel M1/σ1 Agonist with Therapeutic Efficacy in Animal Models of Alzheimer’s Disease. Neurodegener Dis, 16 (1-2): 95-110. [PMID:26606130] |
5. Hall H, Iulita MF, Gubert P, Flores Aguilar L, Ducatenzeiler A, Fisher A, Cuello AC. (2018)
AF710B, an M1/sigma-1 receptor agonist with long-lasting disease-modifying properties in a transgenic rat model of Alzheimer's disease. Alzheimers Dement, 14 (6): 811-823. [PMID:29291374] |
6. Orciani C, Do Carmo S, Foret MK, Hall H, Bonomo Q, Lavagna A, Huang C, Cuello AC. (2023)
Early treatment with an M1 and sigma-1 receptor agonist prevents cognitive decline in a transgenic rat model displaying Alzheimer-like amyloid pathology. Neurobiol Aging, 132: 220-232. [PMID:37864952] |