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
NACRES:
NA.32
PubChem Substance ID:
UNSPSC Code:
12352200
EC Number:
214-486-9
MDL number:
产品名称
(±)-巴氯芬, ≥98% (HPLC), solid
InChI key
KPYSYYIEGFHWSV-UHFFFAOYSA-N
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)
SMILES string
ClC1=CC=C(C(CN)CC(O)=O)C=C1
assay
≥98% (HPLC)
form
solid
color
white to very faintly yellow
solubility
1 M HCl: 50 mg/mL
storage temp.
2-8°C
Quality Level
Gene Information
human ... GABBR1(2550), GABBR2(9568)
rat ... Gabbr1(81657), Gabra2(29706)
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Application
(±)-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
Biochem/physiol Actions
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)。
signalword
Danger
hcodes
Hazard Classifications
Acute Tox. 3 Oral
存储类别
6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
ppe
Eyeshields, Faceshields, Gloves, type P3 (EN 143) respirator cartridges
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)
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)
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
Ravi Chopra et al.
PloS one, 13(5), e0198040-e0198040 (2018-05-31)
Purkinje neuron dendritic degeneration precedes cell loss in cerebellar ataxia, but the basis for dendritic vulnerability in ataxia remains poorly understood. Recent work has suggested that potassium (K+) channel dysfunction and consequent spiking abnormalities contribute to Purkinje neuron degeneration, but
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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