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204718-47-8

中文名稱 204718-47-8
英文名稱 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 結(jié)構(gòu)式 204718-47-8 結(jié)構(gòu)式

基本信息

中文別名
化合物 T12252
英文別名
NRA-0160
2-Thiazolecarboxamide, 4-(4-fluorophenyl)-5-[2-[4-[(3-fluorophenyl)methylene]-1-piperidinyl]ethyl]-

物理化學性質(zhì)

沸點625.3±65.0 °C(Predicted)
密度1.297±0.06 g/cm3(Predicted)
儲存條件-20°C儲存
溶解度溶于二甲基亞砜
酸度系數(shù)(pKa)14.89±0.50(Predicted)

常見問題列表

生物活性
NRA-0160 是一種選擇性的 dopamine D4 receptor 拮抗劑,Ki 值為 0.48 nM;同時對 dopamine D2 receptor,D3 receptor,大鼠 5-HT2A receptor 和 α1 adrenoceptor 分別具有不同程度的親和度,Ki 值分別為 >10000 nM,39 nM,180 nM 和 237 nM。
靶點

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)

體內(nèi)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.

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