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1780372-25-9

中文名稱 SB 243213 dihydrochloride
英文名稱 SB 243213 dihydrochloride
CAS 1780372-25-9
分子式 C22H20ClF3N4O2
分子量 464.87
MOL 文件 1780372-25-9.mol
1780372-25-9 結構式 1780372-25-9 結構式

基本信息

中文別名
化合物 T12859L

物理化學性質(zhì)

溶解度DMSO: 50mM; Ethanol: 100mM
形態(tài)A solid
顏色Light yellow to yellow

常見問題列表

生物活性
SB 243213 dihydrochloride 是一種口服有效的,選擇性的,高親和力的 5-HT2C 受體拮抗劑,對人 5-HT2C 受體的 pKi 為 9.37,pKb 為 9.8。SB 243213 dihydrochloride 對多種神經(jīng)遞質(zhì)受體、酶和離子通道具有超過 100 倍的選擇性。SB 243213 dihydrochloride 具有改善的抗焦慮特性,有用于精神分裂癥和運動障礙的潛力。
靶點

Human 5-HT 2C Receptor

9.37 (pKi)

human 5-HT 1A Receptor

<5.3 (pKi)

human 5-HT 1B Receptor

5.5 (pKi)

human 5-HT 1D Receptor

6.32 (pKi)

human 5-HT 1E Receptor

<5.4 (pKi)

human 5-HT 1F Receptor

5.35 (pKi)

Human 5-HT 2A Receptor

7.01 (pKi)

human 5-HT 2B Receptor

7.2 (pKi)

Human 5-HT 6 Receptor

6.5 (pKi)

Human 5-HT 7 Receptor

5.64 (pKi)

體外研究

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.

體內(nèi)研究

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.

Animal Model: Male Sprague-Dawley experimentally naive rats (220-300 g)
Dosage: 0.1, 0.3, 1, 3, 10 mg/kg
Administration: p.o.; 1 hour pre-test
Result: 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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