Buta, Andriy published the artcileNovel Potent Orthosteric Antagonist of ASIC1a Prevents NMDAR-Dependent LTP Induction, Name: 3-(Methylamino)phenol, the publication is Journal of Medicinal Chemistry (2015), 58(11), 4449-4461, database is CAplus and MEDLINE.
Acid sensing ion channels 1a (ASIC1a) are of crucial importance in numerous physiol. and pathol. processes in the brain. Here we demonstrate that novel 2-oxo-2H-chromene-3-carboxamidine derivative 5b, designed with mol. modeling approach, inhibits ASIC1a currents with an apparent IC50 of 27 nM when measured at pH 6.7. Acidification to 5.0 decreases the inhibition efficacy by up to 3 orders of magnitude. The 5b mol. not only shifts pH dependence of ASIC1a activation but also inhibits its maximal evoked response. These findings suggest that compound 5b binds to pH sensor of ASIC1a acting as orthosteric noncompetitive antagonist. At 100 nM, compound 5b completely inhibits induction of long-term potentiation (LTP) in CA3-CA1 but not in MF-CA3 synapses. These findings support the knockout data indicating the crucial modulatory role of ASIC1a channels in the NMDAR-dependent LTP and introduce a novel type of ASIC1a antagonists.
Journal of Medicinal Chemistry published new progress about 14703-69-6. 14703-69-6 belongs to alcohols-buliding-blocks, auxiliary class Amine,Benzene,Phenol, name is 3-(Methylamino)phenol, and the molecular formula is C7H9NO, Name: 3-(Methylamino)phenol.
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