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5-HT1A modulator 1 对 5-HT1A、α1-肾上腺素能受体和 D2 受体具有非常高的亲和力(IC50s = 2 nM、10 nM 和 40 nM)。
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5-HT1A modulator 1 对 5-HT1A、α1-肾上腺素能受体和 D2 受体具有非常高的亲和力(IC50s = 2 nM、10 nM 和 40 nM)。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 2,650 | 现货 | |
5 mg | ¥ 5,800 | 现货 | |
10 mg | ¥ 7,680 | 现货 | |
25 mg | ¥ 11,500 | 现货 | |
50 mg | ¥ 15,500 | 现货 |
产品描述 | 5-HT1A modulator 1 displays very high affinities for the 5-HT1A, α1-adrenergic receptor, and D2 receptor (IC50s = 2 nM, 10 nM, and 40 nM). |
靶点活性 | SPLA2:2 nM, α1-adrenoceptor:10 nM, 5-HT2A receptor:500 nM, 5-HT1B receptor:300 nM, 5-HT2C receptor:4000 nM, D2 receptor:40 nM |
体外活性 | 5-HT1A modulator 1 对5-HT1B、5-HT2A和5-HT2C具有亲和力(IC50分别为300nM,500nM和4000nM)[1]。 |
体内活性 | 5-HT1A modulator 1 (1 mg/kg; i.p)在小鼠中表现出对5-HT2A亚型94%的拮抗作用。5-HT1A modulator 1 (1 mg/kg;腹腔内)完全阻断定型行为和攀爬行为。在大鼠中,5-HT1A modulator 1 (口服,2 mg/kg和4mg/kg)分别显示63%和58%的拮抗作用,而在每千克8mg和16mg剂量时,拮抗作用完全(分别为103%和108%)。5-HT1A modulator 1 显著减少50%[1]的过动行为。 |
激酶实验 | Binding was determined using membranes prepared from bovine hippocampus. Receptors were labeled with 0.5 nM [3H]-8-OH-DPAT by incubating with 11 concentrations of test compounds (1-10^5 nM) for 30 min at 25°C. Nonspecific binding was determined using 10 μM buspirone. Competition experiments were analyzed using the iterative nonlinear least squares curve fitting program Inplot 4, GraphPad. IC50 values were calculated using the Cheng-Prusoff equation. |
动物实验 | Inject Swiss mice with test compounds (e.g. 5-HT1A modulators 1, 0.25 and 1 mg/kg i.p) prior to injection of 5-HTP (400 mg/kg i.p). Count the number of head twitches that occurred during the 10 minutes starting 10 minutes after the injection of 5HTP. Cyproheptadine was used as reference compound. Wistar rats (n=6) were used. 5-HT1A Modulator 1 was tested at pharmacological doses (1 and 2 mg/kg i.p) and high doses (32 and 64 mg/kg i.p). The intensity of forepaw pedaling was expressed as a percentage of the maximum possible score. The 5-HT1A agonist 8-OH-DPAT induced forepaw trampling and was used as a reference compound. |
别名 | 5-HT1Amodulator1 |
分子量 | 383.51 |
分子式 | C21H25N3O2S |
CAS No. | 142477-34-7 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||
溶解度信息 | DMSO: 5 mg/mL (13.04 mM) | ||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||
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