2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. GABA Receptor
  4. 2-Hydroxysaclofen

2-Hydroxysaclofen 是一种有效的 γ 氨基丁酸转氨酶 B (GABAB) 受体拮抗剂。2-Hydroxysaclofen 可消除尼古丁诱导的低运动效应，增加其镇痛作用。2-Hydroxysaclofen 可刺激雌性大鼠促黄体生成素 (LH) 分泌。

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2-Hydroxysaclofen Chemical Structure

2-Hydroxysaclofen Chemical Structure

CAS No. : 117354-64-0

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10 mg ￥5742
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2-Hydroxysaclofen 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

2-Hydroxysaclofen is a potent γ-amino-butyric-acid-B (GABAB) receptor antagonist. 2-Hydroxysaclofen can abolish nicotine-induced hypolocomotor effects and increases the antinociceptive effects. 2-Hydroxysaclofen can stimulate luteinizing hormone (LH) secretion in female rats[1][2][3].

IC50 & Target

GABAB receptor[1]
体内研究
(In Vivo)

2-Hydroxysaclofen (0.25-1 mg/kg; IP; single dosage) abolishes nicotine hypolocomotor effects and increases the antinociceptive effects of nicotine[1].
2-Hydroxysaclofen (0.3-3 mg/kg; IP; single dosage) reduces the effects of Baclofen (a GABA receptor agonist) on d-amphetamine-induced discriminative cue[2].
2-Hydroxysaclofen (0-100 μg/2 μl; ICV; single dosage) produces a rapid elevation in the serum LH concentration in the estrogen-primed ovariectomized rat[3].

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

Animal Model: Male Swiss Webster mice (22-24 g; treated with 3 mg/kg nicotine)[1]
Dosage: 0.25, 0.5 and 1 mg/kg
Administration: IP; single dosage; after 10 or 45 min of nicotine administration
Result: Abolished nicotine hypolocomotor effects at 1 mg/kg, and increased the antinociceptive effects of nicotine at 1 mg/kg.
Animal Model: Male Wistar rats[2]
Dosage: 0.3, 1 and 3 mg/kg
Administration: IP; single dosage
Result: Reduced the effects of Baclofen on d-amphetamine-induced discriminative cue.
Animal Model: Female Wistar rats (8 weeks)[3]
Dosage: 0, 20, 50 or 100 μg/2 μL
Administration: ICV; single dosage
Result: Produced a rapid elevation in the serum LH concentration in the estrogen-primed ovariectomized rat with a dose-dependent manner, and the peak LH values were observed 10 min after the injection.
The effect was dose-dependent, as 0 or 20 μg of the antagonist was ineffective while a pronounced effect was observed after the injection of 50 or 100 μg.
分子量

265.71

Formula

C9H12ClNO4S
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

2-Hydroxysaclofen 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

2-Hydroxysaclofen117354-64-0GABA ReceptorGamma-aminobutyric acid Receptorγ-Aminobutyric acid ReceptorNicotinehypolocomotorantinociceptiveluteinizing hormoneInhibitorinhibitorinhibit

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目录号：
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