866927-10-8

中文名称:

866927-10-8

中文同义词:

英文名称:

IC87201

英文同义词:

IC87201;2-[(1H-Benzotriazol-6-ylamino)methyl]-4,6-dichlorophenol;IC-87201 (IC87201;Phenol, 2-[(1H-benzotriazol-6-ylamino)methyl]-4,6-dichloro-;IC87201 >=98% (HPLC)

CAS号:

866927-10-8

分子式:

C13H10Cl2N4O

分子量:

309.15

EINECS号:

相关类别:

API

Mol文件:

866927-10-8.mol

生物活性

IC87201 是 PSD95-nNOS 相互作用的抑制剂，可抑制 nMDAR 诱导的一氧化氮和 cGMP 的形成。

体外研究

IC87201 (500-1800 μM) does not inhibit any of the probe-PDZ interactions involving PDZ1, PDZ2, PDZ3 of PSD-95 or nNOS-PDZ, or bind the canonical PDZ ligand binding sites. IC87201 binds to the β-finger of nNOS-PDZ and allosterically inhibits the nNOS-PDZ/PSD-95-PDZ interactions. IC87201 shows high degree of fluorescence-based artefactual signal when using TAMRA-nNOS as probe. IC87201 (20 μM) suppresses NMDA-stimulated cGMP formation relative to vehicle, in cultured hippocampal neurons. IC87201 (10 and 100 nM) attenuats NMDA/glycine-induced decreases in neurite outgrowth. IC87201 dose-dependently reduces NMDA-induced cGMP production in primary hippocampal neurons (DIV 14-21) with an IC 50 of 2.7 μM. IC87201 increases the number of branches at 10-30 μM when compared to control-treated neurons.

体内研究

IC87201 (1, 4 and 10 mg/kg, i.p.) does not produce impairment in either spatial working memory or source memory. IC87201 (1 mg/kg) is effective in treating NMDA-induced thermal hyperalgesia in mice, with a corresponding peak plasma level of 55 ng/mL (or 0.2 μM).