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Merck

B5399

Sigma-Aldrich

(±)-巴氯芬

≥98% (HPLC), solid

别名:

(±)-β-(氨甲基)-4-氯苯丙酸, 巴氯芬片

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About This Item

经验公式(希尔记法):
C10H12ClNO2
CAS号:
分子量:
213.66
EC號碼:
MDL號碼:
分類程式碼代碼:
12352200
PubChem物質ID:
NACRES:
NA.32

化驗

≥98% (HPLC)

形狀

solid

顏色

white to very faintly yellow

溶解度

1 M HCl: 50 mg/mL

儲存溫度

2-8°C

SMILES 字串

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 密鑰

KPYSYYIEGFHWSV-UHFFFAOYSA-N

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應用

(±)-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

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)。
GABA B 受体激动剂;骨骼肌松弛剂;解痉剂。

象形圖

Skull and crossbones

訊號詞

Danger

危險聲明

危險分類

Acute Tox. 3 Oral

儲存類別代碼

6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects

水污染物質分類(WGK)

WGK 3

閃點(°F)

Not applicable

閃點(°C)

Not applicable

個人防護裝備

Eyeshields, Faceshields, Gloves, type P3 (EN 143) respirator cartridges


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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
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)
Amanda McIntyre et al.
The journal of spinal cord medicine, 37(1), 11-18 (2013-10-05)
To review the available evidence on the effectiveness of intrathecal baclofen in the treatment of spasticity in individuals with spinal cord injuries (SCIs) at least 6 months post-injury or diagnosis. A literature search of multiple databases (Pub Med, CINAHL, EMBASE)
Mohamed-Ali Gorsane et al.
Substance abuse, 33(4), 336-349 (2012-09-20)
Baclofen, a γ-aminobutyric acid (GABA)-B receptor agonist, represents a promising drug in alcohol addiction management. Animal models have shown its action at various stages of the process of alcohol addiction. Moreover, initial open and randomized controlled trials have shown the
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)

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