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200940-23-4

中文名稱 SB 243213 HYDROCHLORIDE
英文名稱 SB 243213 dihydrochloride
CAS 200940-23-4
分子式 C22H19F3N4O2.2HCl
分子量 464.87
MOL 文件 200940-23-4.mol
200940-23-4 結(jié)構(gòu)式 200940-23-4 結(jié)構(gòu)式

基本信息

中文別名
化合物 T12859
英文別名
SB 243213 hydrochloride
SB 243213 dihydrochloride
2,3-Dihydro-5-methyl-N-[6-[(2-methyl-3-pyridinyl)oxy]-3-pyridinyl]-6-(trifluoromethyl)-1H-Indole-1-carboxamide dihydrochloride

物理化學(xué)性質(zhì)

儲(chǔ)存條件-20°C儲(chǔ)存
溶解度在DMSO中溶解至50mM
形態(tài)粉末
SB 243213 HYDROCHLORIDE價(jià)格(試劑級(jí))
報(bào)價(jià)日期產(chǎn)品編號(hào)產(chǎn)品名稱CAS號(hào)包裝價(jià)格
2023/03/20HY-103112SB 243213 HYDROCHLORIDE
SB 243213 hydrochloride
200940-23-45mg900元
2023/03/20HY-103112SB 243213 HYDROCHLORIDE
SB 243213 hydrochloride
200940-23-410mg1500元
2023/03/20HY-103112SB 243213 HYDROCHLORIDE
SB 243213 hydrochloride
200940-23-425mg3500元

常見(jiàn)問(wèn)題列表

生物活性
SB 243213 hydrochloride 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(duì)人 5-HT2C 受體的 pKi 為 9.37,pKb 為 9.8。SB 243213 hydrochloride 對(duì)多種神經(jīng)遞質(zhì)受體、酶和離子通道具有超過(guò) 100 倍的選擇性。SB 243213 hydrochloride 具有改善的抗焦慮特性,有用于精神分裂癥和運(yùn)動(dòng)障礙的潛力。
靶點(diǎn)

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 hydrochloride 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 hydrochloride shows 100-fold selectivity over a wide range of neurotransmitter receptors, enzymes and ion channels.

體內(nèi)研究

SB 243213 hydrochloride (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 hydrochloride (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: PO; 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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