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S166

Sigma-Aldrich

Saclofen

solid

Synonym(s):

β-(Aminomethyl)-4-chlorobenzeneethanesulfonic acid

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About This Item

Empirical Formula (Hill Notation):
C9H12ClNO3S
CAS Number:
125464-42-8
Molecular Weight:
249.71
MDL number:
MFCD00216817
UNSPSC Code:
12352200
PubChem Substance ID:
329824485
NACRES:
NA.32

form

solid

Quality Level

200

color

white

solubility

0.1 M NaOH: 20 mg/mL

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)

InChI key

JYLNVJYYQQXNEK-UHFFFAOYSA-N

Gene Information

human ... GABBR1(2550) , GABBR2(9568)
mouse ... GABBR1(54393) , GABBR2(242425)
rat ... GABBR1(81657) , GABBR2(83633)

Application

Saclofen has been used as a GABAB receptor antagonist to study the analgesic effect of repeated injections of oxycodone in rats.
Saclofen has been used to prevent the inhibitory action of oxytocin on capsaicin-induced glutamatergic spontaneous excitatory transmission in rat neurons.

Biochem/physiol Actions

Saclofen is the sulphonic analog of baclofen and is a selective GABAB receptor antagonist.
Saclofen might possess sympathetic nervous system-dependent anti-inflammatory action.

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Personal Protective Equipment

dust mask type N95 (US), Eyeshields, Gloves

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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Ginsenoside Rb1 (Rb1), one of the most abundant protopanaxadiol-type ginsenosides, exerts excellent neuroprotective effects even though it has low intracephalic exposure. The present study aimed to elucidate the apparent contradiction between the pharmacokinetics and pharmacodynamics of Rb1 by studying the
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
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
Antagonism at GABAB receptors by saclofen and related sulphonic analogues of baclofen and GABA
David I.B.Kerr
Neuroscience Letters (1989)
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
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