S166
Saclofen
solid
别名:
β-（氨甲基）-4-氯苯乙磺酸
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关于此项目
经验公式（希尔记法）:
C9H12ClNO3S
化学文摘社编号:
分子量:
249.71
NACRES:
NA.32
PubChem Substance ID:
UNSPSC Code:
51111800
MDL number:
产品名称
Saclofen, solid
InChI key
JYLNVJYYQQXNEK-UHFFFAOYSA-N
SMILES string
NCC(CS(O)(=O)=O)c1ccc(Cl)cc1
InChI
1S/C9H12ClNO3S/c10-9-3-1-7(2-4-9)8(5-11)6-15(12,13)14/h1-4,8H,5-6,11H2,(H,12,13,14)
form
solid
color
white
solubility
0.1 M NaOH: 20 mg/mL
Quality Level
Gene Information
human ... GABBR1(2550), GABBR2(9568)
mouse ... GABBR1(54393), GABBR2(242425)
rat ... GABBR1(81657), GABBR2(83633)
Application
Saclofen已被用于阻止催产素对辣椒素诱导的谷氨酸自发兴奋性传递的抑制作用。
使用Saclofen作为GABAB受体拮抗剂以研究大鼠反复注射羟考酮的镇痛作用。
Biochem/physiol Actions
Saclofen可能具有交感神经系统依赖性抗炎作用。
Saclofen是巴氯芬的磺酸类似物，是一种选择性GABAB受体拮抗剂。
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)
David P Archer et al.
Anesthesia and analgesia, 104(4), 840-846 (2007-03-23)
Synaptic plasticity is thought to provide a molecular mechanism for learning and memory. N-methyl-d-aspartate receptor-mediated plasticity requires that N-methyl-d-aspartate receptor activation coincides with postsynaptic depolarizing potentials (DPSP(A)'s). Pentobarbital, in high concentrations, enhances DPSP(A)'s, but high concentrations suppress synaptic plasticity, probably
Eisuke Koya et al.
Neuropharmacology, 56 Suppl 1, 177-185 (2008-06-21)
Cue-induced drug-seeking in rodents progressively increases after withdrawal from cocaine, suggesting that cue-induced cocaine craving incubates over time. Here, we explored the role of the medial prefrontal cortex (mPFC, a brain area previously implicated in cue-induced cocaine seeking) in this
Molecular Mechanisms Underlying the Enhanced Analgesic Effect of Oxycodone Compared to Morphine in Chemotherapy-Induced Neuropathic Pain
Karine T
PLoS ONE (2014)
Antagonism at GABAB receptors by saclofen and related sulphonic analogues of baclofen and GABA
David I.B.Kerr
Neuroscience Letters (1989)
D I Kerr et al.
Neuroscience letters, 107(1-3), 239-244 (1989-12-15)
Saclofen (the direct sulphonic analogue of baclofen) is a competitive antagonist of baclofen at GABAB receptors in guinea pig ileum and rat cortical slices (estimated pA2 = 5.3), at least twice as potent as 2-hydroxy-saclofen (pA2 = 5). A series
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