Gabaculine
Gabaculine is an amino acid neurotoxin and blood-brain barrier-permeable GABA transaminase inhibitor, with an IC50 of 1 μM in beef and Pseudomonas ovalis. Gabaculine elevates endogenous synaptic and brain GABA levels and enhances GABA activity. Gabaculine induces sedation, hypothermia, loss of righting reflex, and prevents convulsions in mice. Gabaculine is applicable to research related to neurological disorders.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 59556-18-2
- 分子式: C7H9NO2
- 分子量:139.15
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
製品説明
体外実験
Gabaculine potently and irreversibly inhibits GABA transaminase in mouse brain in vitro[1].
Gabaculine potently inhibits GABA transaminase from bovine brain, Pseudomonas ovalis and mouse brain in vitro, with an IC50 of 1 μM against the enzyme derived from bovine brain and Pseudomonas ovalis[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
体内実験
Gabaculine (intracerebroventricular injection, 0.12-2.0 μg; intraperitoneal injection, 60 mg/kg; single administration) dose-dependently and time-dependently increases GABA levels in the brain of mice, and exerts a preventive effect on convulsions induced by Picrotoxin (HY-101391) and Thiosemicarbazide (HY-Y0032)[2].
Gabaculine (i.p., 10-400 mg/kg) induces loss of righting reflex in male ddY mice at doses ≥200 mg/kg, but produces no antinociceptive effects at doses up to 100 mg/kg and shows no tonic immobility response to tail-clinch noxious stimulation at doses up to 400 mg/kg[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:ddy mice (male, body weight 26-30 g)[2]
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Dosage:0.12-2.0 μg (i.c.v., GABA elevation; picrotoxin-induced convulsions; thiosemicarbazide-induced convulsions); 60 mg/kg (i.p., GABA elevation)
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Administration:i.c.v.; i.p.; 3 hours prior to convulsant/electroshock application
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Result:Gradually increased brain GABA content starting at 2 hours post-injection, reaching a maximum ~15 times the control level at 18 hours, and remaining elevated at 24 hours (1.0 μg i.c.v.).
Increased brain GABA content with a similar time course to intraventricular 1.0 μg gabaculine (60 mg/kg i.p.).
Produced a dose-dependent elevation in brain GABA content at 3 hours post-injection (0.12, 0.25, 0.5, 1.0, 2.0 μg i.c.v.).
Prevented picrotoxin-induced convulsions with an ED50 of 0.50 μg (95% confidence limits 0.34-0.78) (i.c.v.).
Prevented thiosemicarbazide-induced convulsions with an ED50 of 0.18 μg (95% confidence limits 0.11-0.22) (i.c.v.).
化学情報
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CAS 番号 59556-18-2
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分子量 139.15
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分子式 C7H9NO2
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SMILES
O=C(C1=CC=CC(C1)N)O
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Structure Classification
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Initial Source
Streptomyces togocaensis subspecies 1039
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Gabaculine 関連分類
HY-N15001 関連分類
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