B5399
(±)-巴氯芬
≥98% (HPLC), GABAB receptor agonist, solid
别名:
(±)-β-（氨甲基）-4-氯苯丙酸, 巴氯芬片
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关于此项目
经验公式（希尔记法）:
C10H12ClNO2
化学文摘社编号:
分子量:
213.66
EC 号:
MDL编号:
UNSPSC代码:
12352200
PubChem化学物质编号:
NACRES:
NA.32
产品名称
(±)-巴氯芬, ≥98% (HPLC), solid
质量水平
方案
≥98% (HPLC)
表单
solid
颜色
white to very faintly yellow
溶解性
1 M HCl: 50 mg/mL
储存温度
2-8°C
SMILES字符串
ClC1=CC=C(C(CN)CC(O)=O)C=C1
InChI
1S/C10H12ClNO2/c11-9-3-1-7(2-4-9)8(6-12)5-10(13)14/h1-4,8H,5-6,12H2,(H,13,14)
InChI key
KPYSYYIEGFHWSV-UHFFFAOYSA-N
基因信息
human ... GABBR1(2550), GABBR2(9568)
rat ... Gabbr1(81657), Gabra2(29706)
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应用
(±)-巴氯芬作为γ-氨基丁酸B受体（GABAB受体）激动剂已用于：
- 作为GABA能药物对照,检测其对1-甲基-4-苯基-1,2,3,6-四氢吡啶(MPTP)诱导的多巴胺能毒性的保护作用
- 检测其对突变小鼠体内运动能力测试和表现的影响
- 检测其对腹侧被盖区多巴胺能(DA)神经元的兴奋作用
- 检测其对浦肯野神经元树突兴奋性降低的作用
生化/生理作用
GABA B 受体激动剂；骨骼肌松弛剂；解痉剂。
巴氯芬(Baclofen)，是一种γ-氨基丁酸(GABA)类似物，具有肌肉松弛作用。作为一种γ-氨基丁酸受体B(GABAB)激动剂，巴氯芬可增强树突钾K+ 通道的活动。它可用于抑制胃食管反流病(GERD)的一过性食管下括约肌松弛(TLESR)。巴氯芬也可用于治疗成瘾症，尤其是酒精使用障碍(AUD)。
警示用语：
Danger
危险声明
危险分类
Acute Tox. 3 Oral
储存分类代码
6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
个人防护装备
Eyeshields, Faceshields, Gloves, type P3 (EN 143) respirator cartridges
The effects of baclofen for the treatment of gastroesophageal reflux disease: a meta-analysis of randomized controlled trials.
Li, et al.
Gastroenterology Research and Practice, 2014, 307805-307805 (2020)
The Use of Baclofen as a Treatment for Alcohol Use Disorder: A Clinical Practice Perspective.
de Beaurepaire, et al.
Frontiers in Psychiatry, 9, 708-708 (2021)
Abhiram Pushparaj et al.
Behavioural brain research, 290, 77-83 (2015-05-03)
Our prior work demonstrated the involvement of the caudal granular subregion of the insular cortex in a rat model of nicotine self-administration. Recent studies in various animal models of addiction for nicotine and other drugs have identified a role for
What's better for me? Fundamental role for lateral habenula in promoting subjective decision biases.
Colin M Stopper et al.
Nature neuroscience, 17(1), 33-35 (2013-11-26)
The lateral habenula (LHb) is believed to convey an aversive or 'anti-reward' signal, but its contribution to reward-related action selection is unknown. We found that LHb inactivation abolished choice biases, making rats indifferent when choosing between rewards associated with different
Jie Liu et al.
Scientific reports, 5, 15720-15720 (2015-10-27)
Microglial activation and inflammation are associated with progressive neuronal apoptosis in neurodegenerative disorders such as Parkinson's disease (PD). γ-Aminobutyric acid (GABA), the major inhibitory neurotransmitter in the central nervous system, has recently been shown to play an inhibitory role in
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