生物活性 | |||
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描述 | 4-Aminobutyric acid (γ-Aminobutyric acid) is a major inhibitory neurotransmitter in the adult mammalian brain, binding to the ionotropic GABA receptors (GABAA receptors) and metabotropic receptors (GABAB receptors)[3]. Incubation of rat brain 4-aminobutyrate aminotransferase (0.1 mM) with 4-amino-hex-5-enoic acid results in a time-dependent irreversible loss of enzymatic activity.[4]. GME (4-Aminobutyric methyl ester hydrochloride) is hydrolyzed to 4-aminobutyric acid (GABA) by brain homogenates, acts as an inhibitor of GABA binding to crude synaptic plasma membranes, activates the release and inhibits the uptake of GABA by rat synaptosomes and acts as a competitive inhibitor of the so-called GABAse system in vitro[5]. |
临床研究 | |||||
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NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
NCT02330094 | Aneurysmal Subarachnoid Hemorr... 展开 >>hage 收起 << | Phase 4 | Completed | - | United States, Florida ... 展开 >> Mayo Clinic in Florida Jacksonville, Florida, United States, 32224 收起 << |
NCT02349477 | Alcohol Use Disorder ... 展开 >> Alcohol Withdrawal 收起 << | Phase 2 | Active, not recruiting | December 2018 | United States, South Carolina ... 展开 >> Medical University of South Carolina Charleston, South Carolina, United States, 29425 收起 << |
NCT00312260 | Pain | Phase 3 | Unknown | December 2016 | Canada, Ontario ... 展开 >> The Hospital for Sick Children Toronto, Ontario, Canada, M5G 1X8 收起 << |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
9.70mL 1.94mL 0.97mL |
48.49mL 9.70mL 4.85mL |
96.97mL 19.39mL 9.70mL |
参考文献 |
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[3]Kowalczyk P, Kulig K. GABA system as a target for new drugs. Curr Med Chem. 2014;21(28):3294-309. |