A-971432
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A-971432 is an orally bioavailable selective
agonist An agonist is a chemical that activates a receptor to produce a biological response. Receptors are cellular proteins whose activation causes the cell to modify what it is currently doing. In contrast, an antagonist blocks the action of the ago ...
of sphingosine-1-phosphate receptor 5 (S1PR5) discovered at AbbVie. It was discovered using high-throughput chemistry. S1P5 agonists have been proposed as an innovative mechanism for the treatment of neurodegenerative disorders such as
Alzheimer's disease Alzheimer's disease (AD) is a neurodegeneration, neurodegenerative disease that usually starts slowly and progressively worsens. It is the cause of 60–70% of cases of dementia. The most common early symptom is difficulty in short-term me ...
and lysosomal storage disorders such as
Niemann–Pick disease Niemann–Pick disease is a group of severe inherited metabolic disorders, in which sphingomyelin accumulates in lysosomes in cells (the lysosomes normally degrade material that comes from out of cells). These disorders involve the dysfunctional ...
. 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.


References


Further reading

* {{cite journal , vauthors= Roberts E, Guerrero M, Urbano M, Rosen H , title = Sphingosine 1-phosphate receptor agonists: a patent review (2010-2012) , journal = Expert Opin Ther Pat , date = Jul 2013 , pmid = 23541049 , doi=10.1517/13543776.2013.783022 , volume=23 , issue = 7 , pages=817–41, s2cid = 24421259 Azetidines Carboxylic acids Phenol ethers Chloroarenes