FTBMT is an orally available, selective and potent agonist of GPR52. It exhibits antipsychotic and procognitive properties without causing catalepsy in rodents. FTBMT improves recognition memory in a novel object recognition test and mitigates MK-801-induced working memory deficits in a radial arm maze test in rats.
orally available, selective and potent agonist of GPR52
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G protein-coupled receptor 52 (GPR52) agonists are expected to improve the symptoms of psychiatric disorders. During exploration for a novel class of GPR52 agonists with good pharmacokinetic profiles, we synthesized 4-(3-(3-fluoro-5-(trifluoromethyl)benzyl)-5-methyl-1H-1,2,4-triazol-1-yl)-2-methylbenzamide (4u; half maximal effective concentration (EC50)=75nM, maximal response (Emax)=122%)
The Journal of pharmacology and experimental therapeutics, 363(2), 253-264 (2017-08-31)
GPR52 is a Gs-coupled G protein-coupled receptor that is predominantly expressed in the striatum and nucleus accumbens (NAc) and was recently proposed as a potential therapeutic target for schizophrenia. In the current study, we investigated the in vitro and in
Numer pozycji handlu globalnego
SKU
NUMER GTIN
SML2242-5MG
04061835249602
SML2242-25MG
04061835249596
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