1. GPCR/G Protein Neuronal Signaling
  2. 5-HT Receptor
  3. 5-HT1A modulator 1

5-HT1A modulator 1 

目录号: HY-100290 纯度: 97.12%
COA 产品使用指南

5-HT1A modulator 1 对 5HT1A,肾上腺素能 α1 和多巴胺 D2 受体具有非常高的亲和力,IC50 分别为 2±0.3 nM,10±3 nM 和 40±9 nM。

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5-HT1A modulator 1 Chemical Structure

5-HT1A modulator 1 Chemical Structure

CAS No. : 142477-34-7

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Top Publications Citing Use of Products
  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

5-HT1A modulator 1 displays very high affinities for the 5HT1A, adrenergic α1 and dopamine D2 receptor with IC50s of 2 ±0.3 nM, 10 ± 3 nM and 40 ±9 nM, respectively.

IC50 & Target

sPLA2

2 nM (IC50)

5-HT2A Receptor

500 nM (IC50)

5-HT2C Receptor

4000 nM (IC50)

α1 receptor

10 nM (IC50)

D2 receptor

40 nM (IC50)

体外研究
(In Vitro)

5-HT1A modulator 1 (Compound 24) also displays affinities for the 5HT1B, 5-HT2A and 5-HT2C receptor with IC50s of 300±55 nM, 500±75 nM, and 4000±440 nM, respectively[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

5-HT1A modulator 1 (Compound 24) shows clear antagonist action at 5HT2A receptor subtype in mice. The antagonism is nearly complete at the dose of 1 mg/kg ip for 5-HT1A modulator 1 (94% of antagonism, p<0.01). 5-HT1A modulator 1 completely blocks the stereotypies and the climbing at the dose of 1 mg/kg ip (100% of antagonism). 5-HT1A modulator 1 is also tested in rats, using the same paradigm. After oral administration, 5-HT1A modulator 1 significantly (p<0.05) reduces the hyperactivity by 50% at the doses of 2 and 4 mg/kg po, respectively 63% and 58% of antagonism for 5-HT1A modulator 1; the antagonism is complete (103% and 108%) at the respective doses of 8 and 16 mg/kg po for 5-HT1A modulator 1 (p<0.01)[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

383.51

Formula

C21H25N3O2S

CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
纯度 & 产品资料
参考文献
Kinase Assay
[1]

Binding is determined using membranes prepared from bovine hippocampus. The receptor is labeled with 0.5 nM [3H]-8-hydroxydipropylaminotetralin (8-OH-DPAT) by incubation at 25°C for 30 min with 11 concentrations of the test compounds (1-105 nM). Nonspecific binding is determined using 10-5 Mbuspirone. Competition experiments are analyzed using the iterative nonlinear least-squares curve-fitting program Inplot 4, graphpad; IC50 values are calculated using the Cheng-Prusoff equation[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Rats[1]
Wistar rats (n=6) are used. 5-HT1A modulator 1 is tested at pharmacological doses (1 and 2 mg/kg ip, respectively) and at high doses (32 and 64 mg/kg ip) in rats. The intensity of forepaw treading is expressed as percentage of the maximal possible score. The 5HT1A agonist 8-OH-DPAT induces forepaw treading and is used as a reference compound.
Mice[1]
Swiss mice are injected with the test compound (e.g., 5-HT1A modulator 1, 0.25 and 1 mg/kg ip) before an injection of 5HTP (400 mg/kg ip). The number of head twiches occurring in a 10 min period starting 10 min after the injection of 5HTP is counted. Cyproheptadine is used as reference compound.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献

5-HT1A modulator 1 相关分类

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
5-HT1A modulator 1
目录号:
HY-100290
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