您好,欢迎来到化工原料网! [登录] [免费注册]
化工原料网
位置:首页 > 产品库 > (±)-Baclofen
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
(±)-Baclofen
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
(±)-Baclofen图片
CAS NO:1134-47-0
规格:98%
分子量:213.7
包装与价格:
包装价格(元)
5g电议
10g电议
25g电议

产品介绍
GABAB agonist
CAS:1134-47-0
分子式:C10H12ClNO2
分子量:213.7
纯度:98%
存储:Store at -20°C

Background:

IC50: 200 nM: a selective agonist of γ-Aminobutyric acid metabotropic receptor (B) (GABAB).


(±)-Baclofen, a selective agonist of GABAB, causes skeletal muscle relaxation and inhibits spasticity via triggering GABAB. (±)-Baclofen, as an active anti-craving medication, modifies animal responses to alcohol and cocaine. γ-Aminobutyric acid (GABA), an inhibitory neurotransmitter, acts via heteromeric ligand-gated ion channels, GABAA and GABAC, and a G protein-coupled receptor, GABAB.


In vitro: (±)-Baclofen dampened cell growth in human hepatocellular carcinoma (HCC) cells in a dose-dependent manner. (±)-Baclofen also caused cell cycle arrest at G0/G1 phase without inducing cell death. Additionally, (±)-baclofen-evoked HCC cells proliferation was associated with down-regulation of the intracellular cAMP level, up-regulation of p21WAF1 protein expression and its phosphorylation level, which could be reversed by pretreatment with the GABAB antagonist, phaclofen, indicating that (±)-baclofen-evoked growth blockade was exerted in a GABAB-dependent fashion [1].


In vivo: The mice, subcutaneously injected with Bel-7402 cells, were given an intraperitoneal injection of (±)-baclofen 30 mg/kg every day for 30 days. Compared with the control, (±)-baclofen remarkably blocked the Bel-7402 xenograft tumor growth without causing toxic effects via measuring the relative tumor volume and the mean body weight change in (±)-baclofen-treated groups, which could make (±)-baclofen as an effective and relatively safe potential drug for the treatment of HCC [1].


Reference:
[1].  Wang, T., Huang, W., & Chen, F. Baclofen, a GABAB receptor agonist, inhibits human hepatocellular carcinoma cell growth in vitro and in vivo. Life Sciences. 2008; 82(9-10): 536-541.