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Baclofen

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Chemical Structure| 1134-47-0 同义名 : 巴氯酚 ;(±)-Baclofen
CAS号 : 1134-47-0
货号 : A190802
分子式 : C10H12ClNO2
纯度 : 98%
分子量 : 213.661
MDL号 : MFCD00055143
存储条件:

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 4 mg/mL(18.72 mM),配合低频超声,水浴加热至45℃,并调节pH至4,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

H2O: 2 mg/mL(9.36 mM),配合低频超声助溶

0.1 M HCL: 10 mg/mL(46.8 mM),配合低频超声助溶

动物实验配方:
生物活性
描述 Baclofen, a lipophilic derivative of γ-aminobutyric acid (GABA), is an orally active, selective metabotropic GABA-B receptor (GABABR) agonist. Baclofen has high blood brain barrier penetrance. Baclofen has the potential for muscle spasticity research[3]. Intrathecal baclofen infusion is an accepted treatment for spasticity[4]. Baclofen pretreatment (3 mg/kg) not only prolonged the time taken for animals to reach a core body temperature of 40 degrees C[5]. Moreover, repeated pretreatment attenuates baclofen-attributed neurotoxicity in overdose and results in post-discontinuation withdrawal syndrome[6]. In high-dose baclofen participants only, there was a predictive effect of lower baseline heart rate variability and fewer post-test percentage of heavy drinking days. There was a dose-specific rescuing effect of high-dose baclofen on the dynamic modulation of cardiovascular responses to eliciting cues[7].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00814632 Vulvodynia Phase 2 Completed - United States, Michigan ... 展开 >> William Beaumont Hospital Royal Oak, Michigan, United States, 48073 收起 <<
NCT01244113 Cerebral Palsy Not Applicable Completed - Korea, Republic of ... 展开 >> Severance Hospital Seoul, Korea, Republic of, 120-752 收起 <<
NCT02771925 Alcohol Dependence Phase 4 Unknown May 2018 India ... 展开 >> Dyanand Medical College and Hospital Recruiting Ludhiana, Punjab, India, 141001 Contact: Sandeep Singh Sidhu, MD,DM    +919814025085    sandeepsidhu1963@gmail.com    Contact: Omesh Goyal, MD,DM    +919914821155    goyalomesh@yahoo.co.in    Principal Investigator: Sandeep Singh Sidhu, MD,DM 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

4.68mL

0.94mL

0.47mL

23.40mL

4.68mL

2.34mL

46.80mL

9.36mL

4.68mL

参考文献

[1]Bexis S, Phillis BD, et al. Baclofen prevents MDMA-induced rise in core body temperature in rats. Drug Alcohol Depend. 2004 Apr 9;74(1):89-96.

[2]Perry HE, Wright RO, et al. Baclofen overdose: drug experimentation in a group of adolescents. Pediatrics. 1998 Jun;101(6):1045-8.

[3]Farokhnia M, Deschaine SL, Sadighi A, Farinelli LA, Lee MR, Akhlaghi F, Leggio L. A deeper insight into how GABA-B receptor agonism via baclofen may affect alcohol seeking and consumption: lessons learned from a human laboratory investigation. Mol Psychiatry. 2021 Feb;26(2):545-555

[4]Lake W, Shah H. Intrathecal Baclofen Infusion for the Treatment of Movement Disorders. Neurosurg Clin N Am. 2019 Apr;30(2):203-209

[5]Bexis S, Phillis BD, Ong J, White JM, Irvine RJ. Baclofen prevents MDMA-induced rise in core body temperature in rats. Drug Alcohol Depend. 2004 Apr 9;74(1):89-96

[6]Chartier M, Tannous S, Benturquia N, Labat L, Reis R, Risède P, Chevillard L, Mégarbane B. Baclofen-Induced Neuro-Respiratory Toxicity in the Rat: Contribution of Tolerance and Characterization of Withdrawal Syndrome. Toxicol Sci. 2018 Jul 1;164(1):153-165

[7]Logge WB, Baillie AJ, Haber PS, Morley KC. Baclofen modulates cardiovascular responses to appetitive cues in treatment-seeking alcohol use disorder individuals. Hum Psychopharmacol. 2020 Mar;35(2):e2722