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/ GABA受体 / Baclofen/巴氯芬

Baclofen/巴氯芬 {[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+
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Accessible (Haz class 3, 4, 5 or 8), International USD 200+
Baclofen/巴氯芬 化学结构 CAS号：1134-47-0
Baclofen/巴氯芬 化学结构
CAS号：1134-47-0
Baclofen/巴氯芬 3D分子结构
CAS号：1134-47-0
Baclofen/巴氯芬 化学结构 CAS号：1134-47-0
Baclofen/巴氯芬 3D分子结构 CAS号：1134-47-0
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Baclofen/巴氯芬 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 ✔ HDAC,Autophagy 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/巴氯芬 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/巴氯芬 细胞实验

Cell Line
Concentration Treated Time Description References
Dopamine neurons in rat midbrain slices 0.01, 0.1, 0.3, 1 μM 10 min Baclofen depressed the spontaneous firing rate of DA neurons in a concentration-dependent manner with an EC50 of 0.27 μM Br J Pharmacol. 2005 Apr;144(7):926-32

Baclofen/巴氯芬 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Baboons Alcohol self-administration model Intramuscular injection 0.1–1.8 mg/kg Once daily for 5 days To examine the effects of baclofen on alcohol seeking and self-administration when treatment was initiated during alcohol abstinence or ongoing alcohol access. Results showed that baclofen significantly reduced total alcohol intake when administered during ongoing alcohol access but not during abstinence. Drug Alcohol Depend. 2017 Oct 1;179:47-54
Female musk shrews Postoperative nausea and vomiting model Intraperitoneal injection 5 mg/kg Single dose Baclofen eliminated emetic behaviors in the shrew PONV model CNS Neurosci Ther. 2022 Jun;28(6):922-931
Sprague-Dawley rats Morphine-induced behavioral sensitization model Subcutaneous injection 1.25, 2.5, 5 mg/kg 8 continuous days To investigate the effects of baclofen on morphine-induced behavioral sensitization and dopamine release. Results showed that baclofen significantly inhibited morphine-induced behavioral sensitization and dopamine release. Behav Brain Funct. 2012 Jul 10;8:20
Mice Models of anxiety-like behavior, learning, and memory Intraperitoneal injection 0.5, 1.5, and 2.5 mg/kg Single administration, 30 minutes before testing To evaluate the effects of Baclofen on anxiety-like behavior, learning, and memory in mice. Results showed that Baclofen exhibited sedation-like effects (i.e., reduced locomotor activity) at the highest dose (2.5 mg/kg) but had no significant effects on anxiety-like behavior at other doses. Neuropharmacology. 2013 Jul;70:156-67
Rats Sprague-Dawley rats Intraperitoneal injection 5 mg/kg Three times daily for five days To evaluate the effects of acute and chronic baclofen treatments on GABA B-activated G-proteins and signaling protein phosphorylation. Results showed that chronic baclofen treatment significantly reduced GABA B-stimulated GTP γS binding and increased phosphorylation of FAK and GSK3 β. Neuropharmacology. 2015 Aug;95:492-502
Sprague-Dawley rats Self-administration model Intraperitoneal injection or VTA microinjection 3 mg/kg (ip) or 50 and 100 ng/side (VTA microinjection) Single administration, tested 20 minutes later To investigate the effects of GABA B receptor agonist baclofen on propofol reinforcement. Results showed that baclofen significantly reduced the number of propofol self-administrations and active responses, without affecting food-maintained behavior or locomotor activity. Acta Pharmacol Sin. 2011 Dec;32(12):1460-5

Baclofen/巴氯芬 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/巴氯芬 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/巴氯芬 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/巴氯芬 技术信息

CAS号1134-47-0
分子式C10H12ClNO2
分子量 213.66
SMILES Code O=C(CC(CN)C1=CC=C(C=C1)Cl)O
MDL No. MFCD00055143
别名 巴氯酚 ;(±)-Baclofen
运输蓝冰
InChI Key KPYSYYIEGFHWSV-UHFFFAOYSA-N
Pubchem ID 2284
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry,2-8°C
溶解方案

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

配制的工作液建议现用现配，短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶。
方案 一

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

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