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2-HYDROXYSACLOFEN

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2-HYDROXYSACLOFEN Basic information

Product Name:
2-HYDROXYSACLOFEN
Synonyms:
  • HYDROXYSACLOFEN
  • 3-amino-2-(4-chlorophenyl)-2-hydroxy-*propanesulf
  • 2-HYDROXYSACLOFEN GABA(B) RECEPTOR ANTA
  • 3-AMINO-2-(4-CHLOROPHENYL)-2-HYDROXY-PRO PANESULFON
  • 2-HYDROXYSACLOFEN, >99%
  • 3-Amino-2-(4-chlorophenyl)-2-hydroxypropane-1-sulfonic acid
  • 3-Amino-2-hydroxy-2-(4-chlorophenyl)propane-1-sulfonic acid
  • 2-Oh-saclofen
CAS:
117354-64-0
MF:
C9H12ClNO4S
MW:
265.71
Product Categories:
  • GABA/Glycine receptor
Mol File:
117354-64-0.mol
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2-HYDROXYSACLOFEN Chemical Properties

Melting point:
267-269 °C
RTECS 
DA0359200
storage temp. 
2-8°C
solubility 
H2O: 1 mg/mL
form 
solid
color 
white
Water Solubility 
Soluble in water at 1mg/ml. Also soluble in DMSO, 0.1M HCl and methanol
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Safety Information

Hazard Codes 
C
Risk Statements 
34
Safety Statements 
26-27-36/37/39-45
RIDADR 
UN 1759 8/PG 3
WGK Germany 
3
HazardClass 
8

MSDS

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2-HYDROXYSACLOFEN Usage And Synthesis

Uses

2-Hydroxysaclofen is a GABA-B receptor antagonist in the ventral tegmental area and may play a role in the mechanisms of cocaine usage. Affects specific acute nicotine responses in mice, abolishing hypolocomotion and increasing antinociception.

Definition

ChEBI: 3-amino-2-(4-chlorophenyl)-2-hydroxy-1-propanesulfonic acid is an organochlorine compound.

Biological Activity

Selective antagonist at GABA B receptors.

in vivo

2-Hydroxysaclofen (0.25-1 mg/kg; IP; single dosage) abolishes nicotine hypolocomotor effects and increases the antinociceptive effects of nicotine[1].
2-Hydroxysaclofen (0.3-3 mg/kg; IP; single dosage) reduces the effects of Baclofen (a GABA receptor agonist) on d-amphetamine-induced discriminative cue[2].
2-Hydroxysaclofen (0-100 μg/2 μl; ICV; single dosage) produces a rapid elevation in the serum LH concentration in the estrogen-primed ovariectomized rat[3].

Animal Model:Male Swiss Webster mice (22-24 g; treated with 3 mg/kg nicotine)[1]
Dosage:0.25, 0.5 and 1 mg/kg
Administration:IP; single dosage; after 10 or 45 min of nicotine administration
Result:Abolished nicotine hypolocomotor effects at 1 mg/kg, and increased the antinociceptive effects of nicotine at 1 mg/kg.
Animal Model:Male Wistar rats[2]
Dosage:0.3, 1 and 3 mg/kg
Administration:IP; single dosage
Result:Reduced the effects of Baclofen on d-amphetamine-induced discriminative cue.
Animal Model:Female Wistar rats (8 weeks)[3]
Dosage:0, 20, 50 or 100 μg/2 μL
Administration:ICV; single dosage
Result:Produced a rapid elevation in the serum LH concentration in the estrogen-primed ovariectomized rat with a dose-dependent manner, and the peak LH values were observed 10 min after the injection.
The effect was dose-dependent, as 0 or 20 μg of the antagonist was ineffective while a pronounced effect was observed after the injection of 50 or 100 μg.

storage

Store at RT

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