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151227-08-6

中文名稱 151227-08-6
英文名稱 AP521
CAS 151227-08-6
分子式 C20H19ClN2O3S
分子量 402.89
MOL 文件 151227-08-6.mol
151227-08-6 結構式 151227-08-6 結構式

基本信息

中文別名
化合物 T10344
英文別名
AP521

物理化學性質

儲存條件-20°C儲存
溶解度溶于二甲基亞砜
形態(tài)Solid
顏色White to off-white
化合物 AP521價格(試劑級)
報價日期產品編號產品名稱CAS號包裝價格
2025/05/22HY-100166151227-08-6
AP521
151227-08-65 mg1700元
2025/05/22HY-100166化合物 AP521
AP521
151227-08-610 mM * 1 mLin DMSO1870元
2025/05/22HY-100166化合物 AP521
AP521
151227-08-610 mg3000元

常見問題列表

生物活性
AP521 是一個人 5-HT1A 受體激動劑,其 IC50 值為 94 nM。
靶點

5-HT 1A Receptor

94 nM (IC 50 , in human)

5-HT 1A Receptor

135 nM (IC 50 , in rat)

5-HT 1B Receptor

254 nM (IC 50 , in rat)

5-HT 1B Receptor

5530 nM (IC 50 , in human)

5-HT 1D Receptor

418 nM (IC 50 , in human)

5-HT 5A Receptor

422 nM (IC 50 , in human)

5-HT 7 Receptor

198 nM (IC 50 , in rat)

體外研究

AP521 is an agonist of human 5-HT 1A receptor with IC 50 s of 135, 94, 254, 5530, 418, 422 and 198 nM for 5-HT 1A (rat), 5-HT 1A (human), 5-HT 1B (rat), 5-HT 1B (human), 5-HT 1D (human), 5-HT 5a (human) and 5-HT 7 (rat), respectively. AP521 also decreases the forskolin-induced cAMP accumulation from 10 nM to 10 μM.

體內研究

AP521 significantly increases the number of shock acceptances [F(5,105)=4.46, P<0.01] at doses between 0.5 to 10 mg/kg. Oral administration of AP521 at 3 and 10 mg/kg significantly decreases freezing time [F(3,60)=2.89, P<0.05]. AP521 significantly increases the time spent on the open arms by approximately 2-fold as compare to the vehicle treated group [F(3, 36)=4.21, P<0.05 for AP521]. The anxiolytic-like effect of AP521 appears to be dose-related. AP521 significantly increases the extracellular 5-HT level of the medial prefrontal cortex (mPFC) at 10 mg/kg from 0.5 to 1 h after administration. AP521 at 3 mg/kg tends to increase the extracellular 5-HT level, however, this increase is not significant.

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