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编 号：F055241
分子式：C9H12ClNO4S
分子量：265.71
分子式：C9H12ClNO4S
分子量：265.71
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CAS No: 117354-64-0
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生物活性：
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.
体内研究：
2-Hydroxysaclofen (0.25-1 mg/kg; IP; single dosage) abolishes nicotine hypolocomotor effects and increases the antinociceptive effects of nicotine.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-Hydroxysaclofen (0-100 μg/2 μl; ICV; single dosage) produces a rapid elevation in the serum LH concentration in the estrogen-primed ovariectomized rat.Animal Model:Male Swiss Webster mice (22-24 g; treated with 3 mg/kg nicotine)
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
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)
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.
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.
体内研究：
2-Hydroxysaclofen (0.25-1 mg/kg; IP; single dosage) abolishes nicotine hypolocomotor effects and increases the antinociceptive effects of nicotine.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-Hydroxysaclofen (0-100 μg/2 μl; ICV; single dosage) produces a rapid elevation in the serum LH concentration in the estrogen-primed ovariectomized rat.Animal Model:Male Swiss Webster mice (22-24 g; treated with 3 mg/kg nicotine)
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
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)
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.
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