SB 243213 dihydrochloride
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- CAS号:
- 1780372-25-9
- 英文名:
- SB 243213 dihydrochloride
- 英文别名:
- 中文名:
- SB 243213 dihydrochloride
- 中文别名:
- 化合物 T12859L
- CBNumber:
- CB28054537
- 分子式:
- C22H20ClF3N4O2
- 分子量:
- 464.87
- MOL File:
- 1780372-25-9.mol
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SB 243213 dihydrochloride化学性质
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溶解度:
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DMSO: 50mM; Ethanol: 100mM
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形态:
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A solid
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SB 243213 dihydrochloride性质、用途与生产工艺
SB 243213 dihydrochloride 是一种口服有效的，选择性的，高亲和力的 5-HT2C 受体拮抗剂，对人 5-HT2C 受体的 pKi 为 9.37，pKb 为 9.8。SB 243213 dihydrochloride 对多种神经递质受体、酶和离子通道具有超过 100 倍的选择性。SB 243213 dihydrochloride 具有改善的抗焦虑特性，有用于精神分裂症和运动障碍的潜力。
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Human 5-HT
2C
Receptor
9.37 (pKi)
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human 5-HT
1A
Receptor
<5.3 (pKi)
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human 5-HT
1B
Receptor
5.5 (pKi)
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human 5-HT
1D
Receptor
6.32 (pKi)
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human 5-HT
1E
Receptor
<5.4 (pKi)
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human 5-HT
1F
Receptor
5.35 (pKi)
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Human 5-HT
2A
Receptor
7.01 (pKi)
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human 5-HT
2B
Receptor
7.2 (pKi)
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Human 5-HT
6
Receptor
6.5 (pKi)
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Human 5-HT
7
Receptor
5.64 (pKi)
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SB 243213 dihydrochloride shows little affinity (pK
i
<6) for cloned human 5-HT
1A
, 5-HT
1B
, 5-HT
1E
, 5- HT
1F
and 5-HT
7
receptors. It shows weak affinity (pK
i
<6.5) for the cloned human 5-HT
1D
and D3 receptors and moderate affinity (pK
i
=6.7) for the cloned human D2 receptor.
SB 243213 dihydrochloride shows 100-fold selectivity over a wide range of neurotransmitter receptors, enzymes and ion channels.
SB 243213 dihydrochloride (0.1-10 mg/kg; p.o.; 1 h pre-test) dose-dependently and significantly increases the amount of time rats spent in social interaction over 15 min under brightly lit conditions and in an unfamiliar test box.
SB 243213 dihydrochloride (0.3 mg/kg; p.o.; 1 h pre-test) significantly increases time spent in social interaction.
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Animal Model:
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Male Sprague-Dawley experimentally naive rats (220-300 g)
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Dosage:
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0.1, 0.3, 1, 3, 10 mg/kg
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Administration:
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p.o.; 1 hour pre-test
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Result:
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Dose-dependently and significantly increased the amount of time rats spent in social interaction over 15 min under brightly lit conditions and in an unfamiliar test box.
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SB 243213 dihydrochloride
上下游产品信息
上游原料
下游产品
SB 243213 dihydrochloride
生产厂家
1780372-25-9, SB 243213 dihydrochloride 相关搜索:
- 制剂-激动剂
- 化合物 T12859L
- 1780372-25-9