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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
基因資訊
human ... GABBR1(2550) , GABBR2(9568)
rat ... Gabbr1(81657) , Gabra2(29706)
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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。
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
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.
Gastroenterology Research and Practice, 2014, 307805-307805 (2020)
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)
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.
Frontiers in Psychiatry, 9, 708-708 (2021)
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