204718-47-8
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- CAS号:
- 204718-47-8
- 英文名:
- NRA-0160
- 英文别名:
- NRA-0160;NRA0160,NRA 0160;2-Thiazolecarboxamide, 4-(4-fluorophenyl)-5-[2-[4-[(3-fluorophenyl)methylene]-1-piperidinyl]ethyl]-
- 中文名:
- 204718-47-8
- 中文别名:
- 化合物 T12252
- CBNumber:
- CB73175564
- 分子式:
- C24H23F2N3OS
- 分子量:
- 439.52
- MOL File:
- 204718-47-8.mol
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204718-47-8化学性质
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沸点:
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625.3±65.0 °C(Predicted)
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密度:
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1.297±0.06 g/cm3(Predicted)
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储存条件:
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Store at -20°C
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溶解度:
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Soluble in DMSO
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酸度系数(pKa):
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14.89±0.50(Predicted)
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204718-47-8性质、用途与生产工艺
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。
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D
4
Receptor
0.48 nM (Ki)
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D
3
Receptor
39 nM (Ki)
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5-HT
2A
Receptor
180 nM (Ki, in rat)
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Rat α1 adrenoceptor
237 nM (Ki)
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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.
204718-47-8
上下游产品信息
上游原料
下游产品
204718-47-8, 204718-47-8 相关搜索:
- 化合物 T12252
- 204718-47-8
- NRA0160,NRA 0160
- 2-Thiazolecarboxamide, 4-(4-fluorophenyl)-5-[2-[4-[(3-fluorophenyl)methylene]-1-piperidinyl]ethyl]-
- NRA-0160