2-hydroxysaclofen

Modify Date: 2024-01-03 10:05:39

2-hydroxysaclofen Structure
2-hydroxysaclofen structure
Common Name 2-hydroxysaclofen
CAS Number 117354-64-0 Molecular Weight 265.71400
Density 1.551 g/cm3 Boiling Point N/A
Molecular Formula C9H12ClNO4S Melting Point 267-269ºC
MSDS Chinese USA Flash Point N/A
Symbol GHS05
GHS05
Signal Word Danger

 Use of 2-hydroxysaclofen


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].

 Names

Name 3-amino-2-(4-chlorophenyl)-2-hydroxypropane-1-sulfonic acid
Synonym More Synonyms

 2-hydroxysaclofen Biological Activity

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.

 Chemical & Physical Properties

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

 Safety Information

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

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 Synonyms

2-Hydroxysaclofen
2-OH-Saclofen
Dimaprit dihydrochloride
MFCD00069282