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/ GABA受体 / Baclofen

巴氯芬 /Baclofen {[allProObj[0].p_purity_real_show]}

货号：A190802 同义名： 巴氯酚 / (±)-Baclofen

Baclofen是一种 γ-氨基丁酸衍生物，是一种选择性的 GABAB 激动剂，IC50 为 200 nM，用作骨骼肌松弛剂。

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Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
Baclofen 化学结构 CAS号：1134-47-0
Baclofen 化学结构
CAS号：1134-47-0
Baclofen 3D分子结构
CAS号：1134-47-0
Baclofen 化学结构 CAS号：1134-47-0
Baclofen 3D分子结构 CAS号：1134-47-0
规格 价格 会员价 库存 数量
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Baclofen 纯度/质量文件 产品仅供科研

货号：A190802 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 GABA receptor ↓ GABAA receptor ↓ 其他靶点 纯度
Niflumic Acid ✔ 98%
Ginkgolide A ++

GABA receptor, Ki: 14.5 μM

 		98%
Valproic acid sodium ✔ Autophagy,HDAC 97%
Flumazenil ✔ 95%
Bemegride ✔ 98%
Bicuculline +++

GABAA receptor, IC50: 2 μM

 		99%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Baclofen 生物活性

描述 Baclofen, a lipophilic derivative of γ-aminobutyric acid (GABA), is an orally active, selective metabotropic GABA-B receptor (GABABR) agonist. Baclofen has high blood brain barrier penetrance. Baclofen has the potential for muscle spasticity research[3]. Intrathecal baclofen infusion is an accepted treatment for spasticity[4]. Baclofen pretreatment (3 mg/kg) not only prolonged the time taken for animals to reach a core body temperature of 40 degrees C[5]. Moreover, repeated pretreatment attenuates baclofen-attributed neurotoxicity in overdose and results in post-discontinuation withdrawal syndrome[6]. In high-dose baclofen participants only, there was a predictive effect of lower baseline heart rate variability and fewer post-test percentage of heavy drinking days. There was a dose-specific rescuing effect of high-dose baclofen on the dynamic modulation of cardiovascular responses to eliciting cues[7].

Baclofen 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00814632 Vulvodynia Phase 2 Completed - United States, Michigan ... 展开 >> William Beaumont Hospital Royal Oak, Michigan, United States, 48073 收起 <<
NCT01244113 Cerebral Palsy Not Applicable Completed - Korea, Republic of ... 展开 >> Severance Hospital Seoul, Korea, Republic of, 120-752 收起 <<
NCT02771925 Alcohol Dependence Phase 4 Unknown May 2018 India ... 展开 >> Dyanand Medical College and Hospital Recruiting Ludhiana, Punjab, India, 141001 Contact: Sandeep Singh Sidhu, MD,DM    +919814025085    sandeepsidhu1963@gmail.com    Contact: Omesh Goyal, MD,DM    +919914821155    goyalomesh@yahoo.co.in    Principal Investigator: Sandeep Singh Sidhu, MD,DM 收起 <<

Baclofen 参考文献

[1]Bexis S, Phillis BD, et al. Baclofen prevents MDMA-induced rise in core body temperature in rats. Drug Alcohol Depend. 2004 Apr 9;74(1):89-96.

[2]Perry HE, Wright RO, et al. Baclofen overdose: drug experimentation in a group of adolescents. Pediatrics. 1998 Jun;101(6):1045-8.

[3]Farokhnia M, Deschaine SL, Sadighi A, Farinelli LA, Lee MR, Akhlaghi F, Leggio L. A deeper insight into how GABA-B receptor agonism via baclofen may affect alcohol seeking and consumption: lessons learned from a human laboratory investigation. Mol Psychiatry. 2021 Feb;26(2):545-555

[4]Lake W, Shah H. Intrathecal Baclofen Infusion for the Treatment of Movement Disorders. Neurosurg Clin N Am. 2019 Apr;30(2):203-209

[5]Bexis S, Phillis BD, Ong J, White JM, Irvine RJ. Baclofen prevents MDMA-induced rise in core body temperature in rats. Drug Alcohol Depend. 2004 Apr 9;74(1):89-96

[6]Chartier M, Tannous S, Benturquia N, Labat L, Reis R, Risède P, Chevillard L, Mégarbane B. Baclofen-Induced Neuro-Respiratory Toxicity in the Rat: Contribution of Tolerance and Characterization of Withdrawal Syndrome. Toxicol Sci. 2018 Jul 1;164(1):153-165

[7]Logge WB, Baillie AJ, Haber PS, Morley KC. Baclofen modulates cardiovascular responses to appetitive cues in treatment-seeking alcohol use disorder individuals. Hum Psychopharmacol. 2020 Mar;35(2):e2722

Baclofen 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

4.68mL

0.94mL

0.47mL

23.40mL

4.68mL

2.34mL

46.80mL

9.36mL

4.68mL

Baclofen 技术信息

CAS号1134-47-0
分子式C10H12ClNO2
分子量 213.661
别名 巴氯酚 ;(±)-Baclofen
运输蓝冰
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Keep in dark place,Inert atmosphere,Room temperature
溶解度

DMSO: 4 mg/mL(18.72 mM)，配合低频超声，水浴加热至45℃，并调节pH至4，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 2 mg/mL(9.36 mM)，配合低频超声助溶

0.1 M HCL: 10 mg/mL(46.8 mM)，配合低频超声助溶
动物实验配方

Tags: Baclofen | (±)-Baclofen | 巴氯酚 | GABA Receptor | AmBeed-信号通路专用抑制剂 | Baclofen 纯度/质量文件 | Baclofen 亚型比较 | Baclofen 生物活性 | Baclofen 临床数据 | Baclofen 参考文献 | Baclofen 实验方案 | Baclofen 技术信息

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