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ChemicalBook CAS数据库列表 (2S)-(+)-5-(1,3,5-TRIMETHYLPYRAZOL-4-YL)-2-(DIMETHYLAMINO)TETRALIN

(2S)-(+)-5-(1,3,5-TRIMETHYLPYRAZOL-4-YL)-2-(DIMETHYLAMINO)TETRALIN

生物活性靶点体外研究体内研究 (2S)-(+)-5-(1,3,5-TRIMETHYLPYRAZOL-4-YL)-2-(DIMETHYLAMINO)TETRALIN 试剂级价格

CAS号:1000578-26-6
英文名:(2S)-(+)-5-(1,3,5-TRIMETHYLPYRAZOL-4-YL)-2-(DIMETHYLAMINO)TETRALIN
中文名:(2S)-(+)-5-(1,3,5-TRIMETHYLPYRAZOL-4-YL)-2-(DIMETHYLAMINO)TETRALIN
CBNumber:CB5846829
分子式:C18H25N3
分子量:283.41
MOL File:Mol file

(2S)-(+)-5-(1,3,5-TRIMETHYLPYRAZOL-4-YL)-2-(DIMETHYLAMINO)TETRALIN化学性质

沸点 :413.3±45.0 °C(Predicted)
密度 :1.09±0.1 g/cm3(Predicted)
储存条件 :Desiccate at -20°C
溶解度 :<28.34mg/ml in ethanol; <28.34mg/ml in DMSO
形态 :oil
酸度系数(pKa) :9.20±0.20(Predicted)
颜色 :Yellow

(2S)-(+)-5-(1,3,5-TRIMETHYLPYRAZOL-4-YL)-2-(DIMETHYLAMINO)TETRALIN性质、用途与生产工艺

生物活性 AS19 是一种有效的选择性 5-HT7 受体激动剂，IC50 值为 0.83 nM，Ki 为 0.6 nM。AS19 对 5-HT7 的选择性高于 5-HT1A，5-HT1B，5-HT1D 和 5-HT5A 受体 (Kis 分别为 89.7 nM，490 nM，6.6 nM 和 98.5 nM)。AS19 可增强记忆力，并逆转由 Scopolamine 或 Dizocilpine 引起的健忘症。

靶点

Human 5-HT ₇ Receptor

0.83 nM (IC ₅₀ )

Human 5-HT ₇ Receptor

0.6 nM (Ki)

5-HT _1A Receptor

89.7 nM (Ki)

5-HT _1B Receptor

490 nM (Ki)

5-HT _1D Receptor

6.6 nM (Ki)

5-HT ₅ Receptor

98.5 nM (Ki)

体外研究

The proliferation of T-cell from parachlorophenylalanine-treated mice is significantly reduced, addition of AS19 (1 μM) completely restores T-cell proliferation after 48 hours.

体内研究

AS19 (0.5-10 mg/kg; subcutaneous injection; for 24 hours; male Wistar rats) treatment improves memory consolidation in an autoshaping Pavlovian/instrumental learning task.

Animal Model:	Male Wistar rats (12-week-old) with autoshaping Pavlovian/instrumental learning task
Dosage:	0.5 mg/kg, 1 mg/kg, 5 mg/kg, 10 mg/kg
Administration:	Subcutaneous injection; for 24 hours
Result:	Enhanced memory formation in an autoshaping Pavlovian/instrumental learning task.