Chemistry:A-971432
From HandWiki
Short description: Chemical compound
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 Ball and stick structure of A-971432 | |
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| Formula | C18H17Cl2NO3 |
| Molar mass | 366.24 g·mol−1 |
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A-971432 is an orally bioavailable selective agonist of sphingosine-1-phosphate receptor 5 (S1PR5) discovered at AbbVie.[1] It was discovered using high-throughput chemistry.[2] S1P5 agonists have been proposed as an innovative mechanism for the treatment of neurodegenerative disorders such as Alzheimer's disease and lysosomal storage disorders such as Niemann–Pick disease.[3] Stimulation of S1PR5 with A-971432 has been shown to preserve blood-brain barrier integrity and exert a therapeutic effect in an animal model of Huntington’s disease.[4]
References
- ↑ "Preparation of 1-benzylazetidine-3-carboxylic acid derivatives as agonists and antagonists of the S1P5 receptor" WO patent application 2010093704, published 2010-08-19
- ↑ "Discovery of A-971432, An Orally Bioavailable Selective Sphingosine-1-Phosphate Receptor 5 (S1P5) Agonist for the Potential Treatment of Neurodegenerative Disorders". Journal of Medicinal Chemistry 58 (23): 9154–70. Nov 2015. doi:10.1021/acs.jmedchem.5b00928. PMID 26509640.
- ↑ "The use of selective sphingosine-1-phosphate receptor 5 agonists for the treatment of neurodegenerative disorders such as alzheimer's disease and lysosomal storage diseases such as niemann-pick c disease". Alzheimer's & Dementia 10 (4): P281. Jun 2014. doi:10.1016/j.jalz.2014.07.153.
- ↑ "Stimulation of S1PR5 with A-971432, a selective agonist, preserves blood-brain barrier integrity and exerts therapeutic effect in an animal model of Huntington's disease". Human Molecular Genetics 27 (14): 2490–2501. Apr 2018. doi:10.1093/hmg/ddy153. PMID 29688337.
Further reading
- "Sphingosine 1-phosphate receptor agonists: a patent review (2010-2012)". Expert Opin Ther Pat 23 (7): 817–41. Jul 2013. doi:10.1517/13543776.2013.783022. PMID 23541049.
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