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5-HT1A modulator 1
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
5-HT1A modulator 1图片
CAS NO:142477-34-7
包装与价格:
包装价格(元)
1 mg电议
2 mg电议
5 mg电议

产品名称
5-HT1Amodulator1
产品介绍
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)。

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).

体外活性

5-HT1A modulator 1 displays affinities for the 5-HT1B, 5-HT2A, and 5-HT2C (IC50s = 300 nM, 500 nM, and 4000 nM)[1].

体内活性

5-HT1A modulator 1 (1 mg/kg; i.p) shows 94% antagonist action at 5-HT2A subtype in mice. 5-HT1A modulator 1 (1 mg/kg; i.p) completely blocks the stereotypes and the climbing. In rats, 5-HT1A modulator 1 (2 and 4 mg/kg; p.o) shows a respective 63% and 58% of antagonism and the antagonism is complete (103% and 108%) at doses of 8 and 16 mg/kg. 5-HT1A modulator 1 significantly reduces hyperactivity by 50%[1].

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.

Cas No.

142477-34-7

分子式

C21H25N3O2S

分子量

383.51

别名

5-HT1Amodulator1

储存和溶解度

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years