204718-47-8

中文名称 204718-47-8

英文名称 NRA-0160

CAS 204718-47-8

分子式 C24H23F2N3OS

分子量 439.52

MOL 文件 204718-47-8.mol

204718-47-8 结构式

基本信息物理化学性质常见问题列表

基本信息

中文别名

化合物 T12252

英文别名

NRA-0160
2-Thiazolecarboxamide, 4-(4-fluorophenyl)-5-[2-[4-[(3-fluorophenyl)methylene]-1-piperidinyl]ethyl]-

物理化学性质

沸点625.3±65.0 °C(Predicted)

密度1.297±0.06 g/cm3(Predicted)

储存条件-20°C储存

溶解度溶于二甲基亚砜

酸度系数(pKa)14.89±0.50(Predicted)

常见问题列表

生物活性

NRA-0160 是一种选择性的 dopamine D4 receptor 拮抗剂，Ki 值为 0.48 nM；同时对 dopamine D2 receptor，D3 receptor，大鼠 5-HT2A receptor 和 α1 adrenoceptor 分别具有不同程度的亲和度，Ki 值分别为 >10000 nM，39 nM，180 nM 和 237 nM。

靶点

D ₄ Receptor

0.48 nM (Ki)

D ₃ Receptor

39 nM (Ki)

5-HT _2A Receptor

180 nM (Ki, in rat)

Rat α1 adrenoceptor

237 nM (Ki)

体内研究

NRA0160 (0.1, 1, or 3 mg/kg, i.p.) has no effect on PCP-induced hyperlocomotion, stereotypy or ataxia in SD rats. NRA0160, at any dose, does not reduce cumulated counts of locomotion and cumulated scores of stereotypy emerging, and has no effect on extracellular glutamate levels and locomotor activity emerged after saline injection. NRA0160 dose-dependently and significantly reverses the effects of MAP on both A9 and Al0 dopamine neurons. NRA0160 is slightly more potent in reversiig the effects of MAP on A10 (ED ₅₀ = 1.0 mg/kg) than on A9 dopamine neurons (ED ₅₀ = 1.3 mg/kg). NRA0160 reverses the effect of AP0 on both A9 and A10 dopamine neurons. ED ₅₀ values for the effects of NRA0160 on APO-induced inhibition of A9 and A10 dopamine neurons are 1.3 mg/kg and 0.5 mg/kg, respectively.