2. GPCR/G Protein Neuronal Signaling
  3. Adrenergic Receptor
  4. Amibegron

Amibegron  (Synonyms: SR-58611)

目录号: HY-111479
产品使用指南

摩尔计算器

Amibegron 是一种选择性的 β3-adrenoceptor 激动剂，对大鼠结肠 β-adrenoceptor 的 EC50 值为 3.5 nM；Amibegron 具有抗焦虑和抗抑郁的活性。

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Amibegron Chemical Structure

Amibegron Chemical Structure

CAS No. : 121524-08-1

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Amibegron 的其他形式现货产品:

Other Forms of Amibegron:

Amibegron 相关抗体

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α adrenergic receptor β adrenergic receptor

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Amibegron is a selective β3-adrenoceptor agonist, with an EC50 of 3.5 nM for β-adrenoceptor in rat colon; Amibegron has anxiolytic and antidepressant activity.

IC50 & Target

EC50: 3.5 nM (β-adrenoceptor, from rat colon), 499 nM (β-adrenoceptor, from rat uterus)[1], 1.2 μM (β2-adrenoceptor, from cerebellum), 4.6 μM (β1-adrenoceptor1, from cortex)[2]
体外研究
(In Vitro)

Amibegron is a selective β-adrenoceptor agonist, with an EC50 of 3.5 nM for β-adrenoceptor in rat colon, and 499 nM in rat uterus[1]. Amibegron hydrochloride (SR 58611A) shows little effect on β1- and β2-adrenoceptors, 5-HT uptake, noradrenaline (NA) uptake, and dopamine (DA) uptake from rat brain tissue, with IC50s of 4.6 and 1.2, 0.58, 2.5 and 3.2 μM, respectively; exhibits no effect on 5-HT1A, 5-HT2, MAO-A and MAO-B (IC50 > 10 μM)[2].

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

Amibegron 相关抗体:
体内研究
(In Vivo)

Amibegron hydrochloride (SR 58611A, 0.1 to 0.3 mg/kg, i.p.) potentiates the toxicity produced by yohimbine in mice. Amibegron hydrochloride (0.6 and 2 mg/kg, i.p.) is also active in the learned helplessness model of antidepressant-like activity in rats. However, Amibegron hydrochloride exhibits no effect on the spontaneous locomotor activity of mice at up to 10 mg/kg and of rats at up tp 30 mg/kg[2]. Amibegron hydrochloride (3 and 10 mg/kg, p.o.) increases the synthesis of 5-HT and tryptophan (Trp) levels in several rodent brain areas such as cortex, hippocampus, hypothalamus, striatum. In addition, Amibegron hydrochloride (10 mg/kg, p.o.) promotes the release of 5-HT in rat prefrontal cortex. Systemic (3 mg/kg, i.v.) or chronic administration of SR58611A (10 mg/kg, p.o.) does not affect the activity of serotonergic neurons in the rat dorsal raphe nucleus[3].

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

403.90

Formula

C22H26ClNO4
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献
Animal Administration
[2]

Mice[2]
This test is performed on groups of 10-20 mice. Amibegron hydrochloride (0.1 to 0.3 mg/kg) or vehicle are administered i.p. 30 min before the administration of yohimbine. Yohimbine hydrochloride is administered s.c. at a dose of 30 mg/kg always at the same time of day, between 1.30 and 3.30 p.m. Lethality is recorded the next morning at 9 a.m[2].
Rats[2]
The rats (n = 10 per group) are treated randomly according to one of the following protocols: the control sample, which receives no shock, is given vehicle; experimental animals with inescapable shock are treated daily with vehicle or Amibegron hydrochloride (up to 30 mg/kg). Animals are treated orally over 5 consecutive days, i.e. 6 h after shock pretreatment on day 1, and then twice per day, a half dose in the morning (30 min before shuttle-box session) and a half dose in the afternoon (except on the 5th day). Statistical analysis is performed on themean number of escape failures using a two-way analysis of variance followed by Dunnett's test[2].

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

Amibegron 相关分类

  • 摩尔计算器

  • 稀释计算器

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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.

Keywords:

Amibegron121524-08-1SR-58611SR58611SR 58611Adrenergic ReceptorBeta ReceptorInhibitorinhibitorinhibit

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