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1000578-26-6

中文名称 (2S)-(+)-5-(1,3,5-TRIMETHYLPYRAZOL-4-YL)-2-(DIMETHYLAMINO)TETRALIN
英文名称 (2S)-(+)-5-(1,3,5-TRIMETHYLPYRAZOL-4-YL)-2-(DIMETHYLAMINO)TETRALIN
CAS 1000578-26-6
分子式 C18H25N3
分子量 283.41
MOL 文件 1000578-26-6.mol
更新日期 2023/03/20 15:41:21
1000578-26-6 结构式 1000578-26-6 结构式

基本信息

中文别名
化合物 T10380
英文别名
AS 19
(2S)-(+)-5-(1,3,5-TRIMETHYLPYRAZOL-4-YL)-2-(DIMETHYLAMINO)TETRALIN
2-Naphthalenamine, 1,2,3,4-tetrahydro-N,N-dimethyl-5-(1,3,5-trimethyl-1H-pyrazol-4-yl)-, (2S)-

物理化学性质

储存条件Desiccate at -20°C
溶解度<28.34mg/ml in ethanol; <28.34mg/ml in DMSO
形态oil
颜色深黄色

常见问题列表

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.
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