G013
R (+)-巴氯芬 盐酸盐
solid
别名:
R(+)-β-（氨甲基）-4-氯苯丙酸 盐酸盐, STX209, 巴氯芬 盐酸盐
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关于此项目
经验公式（希尔记法）:
C10H12ClNO2 · HCl
化学文摘社编号:
分子量:
250.12
NACRES:
NA.32
PubChem Substance ID:
UNSPSC Code:
12352200
MDL number:
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
SMILES string
Cl[H].NC[C@H](CC(O)=O)c1ccc(Cl)cc1
InChI key
WMNUVYYLMCMHLU-QRPNPIFTSA-N
form
solid
optical activity
[α]28/D +3.8°, c = 0.9 in methanol(lit.)
storage condition
desiccated
color
white
solubility
DMSO: >20 mg/mL, H2O: 26 mg/mL (Solutions may be stored for several weeks at 4 °C.)
Quality Level
Gene Information
human ... GABBR1(2550)
mouse ... GABBR1(54393)
rat ... GABBR1(81657)
Application
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。
Biochem/physiol Actions
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。
Other Notes
对映异构体与 R（−）-巴氯芬游离碱相同。
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
ppe
Eyeshields, Gloves, type N95 (US)
Yuriko Watanabe et al.
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
Synthesis of both enantiomers of baclofen using (R)-and (S)-N-phenylpantolactam as chiral auxiliaries
Camps P, et al.
Tetrahedron Asymmetry, 15(13) (2004)
Reagan L Pennock et al.
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
Wenxia Z, et al.
Neuropsychopharmacology, 880?890-880?890 (2004)
An efficient synthesis of (R)-and (S)-baclofen via desymmetrization
Ji L, et al.
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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