形式
solid
质量水平
旋光性
[α]28/D +3.8°, c = 0.9 in methanol(lit.)
储存条件
desiccated
颜色
white
溶解性
DMSO: >20 mg/mL
H2O: 26 mg/mL (Solutions may be stored for several weeks at 4 °C.)
SMILES字符串
Cl[H].NC[C@H](CC(O)=O)c1ccc(Cl)cc1
InChI
1S/C10H12ClNO2.ClH/c11-9-3-1-7(2-4-9)8(6-12)5-10(13)14;/h1-4,8H,5-6,12H2,(H,13,14);1H/t8-;/m0./s1
InChI key
WMNUVYYLMCMHLU-QRPNPIFTSA-N
基因信息
human ... GABBR1(2550)
mouse ... GABBR1(54393)
rat ... GABBR1(81657)
应用
R(+)-盐酸巴氯芬已用作GABAB受体激动剂,以研究其对大鼠模型中M43068诱导的镇痛作用的影响。它还被用作GABAB受体激动剂,以研究其对鼠纹状体中安非他命诱导的行为和神经化学反应的影响。
生化/生理作用
巴氯芬是一种γ-氨基丁酸(GABA)的衍生物,可用作4-氨基丁酸受体(GABAB)激动剂。它与GABA受体立体定向相互作用并表现出抗痉挛作用。巴氯芬对三叉神经痛和脊柱痉挛的阵发性疼痛有治疗作用。R(+)-巴氯芬是一种活性更强的对映体。
其他说明
对映异构体与 R(−)-巴氯芬游离碱相同。
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
个人防护装备
Eyeshields, Gloves, type N95 (US)
Synthesis of both enantiomers of baclofen using (R)-and (S)-N-phenylpantolactam as chiral auxiliaries
Tetrahedron Asymmetry, 15(13) (2004)
European journal of pharmacology, 837, 88-95 (2018-08-08)
The nucleus accumbens contains delta-opioid receptors that may decrease inhibitory neurotransmission. As GABAB receptors inhibit dopamine release, decrease in activation of GABAB receptors may be a mediator of delta-opioid receptor-induced accumbal dopamine efflux. If so, accumbal dopamine efflux induced by
The Journal of physiology, 592(19), 4247-4256 (2014-08-03)
It has recently been shown that dynorphin A (Dyn A), an endogenous agonist of the κ-opioid receptor (KOR), directly inhibits proopiomelanocortin (POMC) neurons in the hypothalamus through activation of G-protein-coupled inwardly rectifying K(+) channels (GIRKs). This effect has been proposed
Intracerebral Baclofen Administration Decreases Amphetamine-Induced Behavior and Neuropeptide Gene Expression in the Striatum
Neuropsychopharmacology, 880?890-880?890 (2004)
An efficient synthesis of (R)-and (S)-baclofen via desymmetrization
Tetrahedron Letters, 50(45), 6166-6168 (2009)
实验方案
Qualitative Thin Layer Chromatography Analysis of Flavonoids and Quantification of Terpene Lactones in Ginkgo Biloba Extracts and Tablets
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