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117354-64-0

117354-64-0 structure
117354-64-0 structure
  • Name: 2-hydroxysaclofen
  • Chemical Name: 3-amino-2-(4-chlorophenyl)-2-hydroxypropane-1-sulfonic acid
  • CAS Number: 117354-64-0
  • Molecular Formula: C9H12ClNO4S
  • Molecular Weight: 265.71400
  • Catalog: Organic raw materials Amino compound Sulfonic acid amino compound
  • Create Date: 2018-12-24 11:23:37
  • Modify Date: 2024-01-03 10:05:39
  • 2-Hydroxysaclofen is a potent γ-amino-butyric-acid-B (GABAB) receptor antagonist. 2-Hydroxysaclofen can abolish nicotine-induced hypolocomotor effects and increases the antinociceptive effects. 2-Hydroxysaclofen can stimulate luteinizing hormone (LH) secretion in female rats[1][2][3].

Name 3-amino-2-(4-chlorophenyl)-2-hydroxypropane-1-sulfonic acid
Synonyms 2-Hydroxysaclofen
2-OH-Saclofen
Dimaprit dihydrochloride
MFCD00069282
Description 2-Hydroxysaclofen is a potent γ-amino-butyric-acid-B (GABAB) receptor antagonist. 2-Hydroxysaclofen can abolish nicotine-induced hypolocomotor effects and increases the antinociceptive effects. 2-Hydroxysaclofen can stimulate luteinizing hormone (LH) secretion in female rats[1][2][3].
Related Catalog
Target

GABAB receptor[1]

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.
References

[1]. Varani AP, et al. Baclofen and 2-hydroxysaclofen modify acute hypolocomotive and antinociceptive effects of nicotine. Eur J Pharmacol. 2014 Sep 5;738:200-5.

[2]. Miranda F, et al. The GABA-B antagonist 2-hydroxysaclofen reverses the effects of baclofen on the discriminative stimulus effects of D-amphetamine in the conditioned taste aversion procedure. Pharmacol Biochem Behav. 2009 Jul;93(1):25-30.

[3]. Akema T, et al. 2-Hydroxysaclofen, a potent GABAB receptor antagonist, stimulates luteinizing hormone secretion in female rats. Brain Res. 1991 Apr 12;546(1):143-5.

Density 1.551 g/cm3
Melting Point 267-269ºC
Molecular Formula C9H12ClNO4S
Molecular Weight 265.71400
Exact Mass 265.01800
PSA 109.00000
LogP 2.15520
Index of Refraction 1.63
Symbol GHS05
GHS05
Signal Word Danger
Hazard Statements H314
Precautionary Statements P280-P305 + P351 + P338-P310
Personal Protective Equipment Eyeshields;Faceshields;full-face particle respirator type N100 (US);Gloves;respirator cartridge type N100 (US);type P1 (EN143) respirator filter;type P3 (EN 143) respirator cartridges
Hazard Codes C: Corrosive;
Risk Phrases R34
Safety Phrases 26-27-36/37/39-45
RIDADR UN 1759 8/PG 3
WGK Germany 3