γ-Aminobutyric acid (4-Aminobutyric acid) 是成年哺乳动物大脑中主要的抑制性神经递质,能够与离子移变GABAA受体和促代谢GABAB受体结合发挥作用。γ-Aminobutyric acid 能够阻断中枢神经系统的特定信号,并带来镇静效果。
生物活性 | γ-Aminobutyric acid (4-Aminobutyric acid) is a major inhibitory neurotransmitter in the adult mammalian brain, binding to the ionotropic GABA receptors (GABAAreceptors) and metabotropic receptors (GABABreceptors. γ-Aminobutyric acid shows calming effect by blocking specific signals of central nervous system[1][2]. |
IC50& Target | Human Endogenous Metabolite | Microbial Metabolite |
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体外研究 (In Vitro) | γ-Aminobutyric acid (30 μM) depolarizes cortical progenitor cells (E16 cells), results an inward current in ventricular zone (VZ) cells, and induces DNA synthesis inhibition, with half-maximal response concentration of 5 μM[3]. Cortical plate (cp) neurons expresses glutamic acid decarboxylase (GAD), γ-Aminobutyric acid (1-5 μM; 18 h) stimulates the motility and arrests the migration of cp cells, while the chemotropic signal is involved G-protein activation[4]. γ-Aminobutyric acid activates GABAAreceptors, causing cell cycle arrest in S phase and limiting growth[5].
Cell Migration Assay[4] Cell Line: | Cortical plate (cp) neurons | Concentration: | 1-5 μM | Incubation Time: | 18 hours | Result: | Promoted motility via G-protein activation and arrested attractantinduced migration via GABAA receptor-mediated depolarization. |
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体内研究 (In Vivo) | γ-Aminobutyric acid (33.95, 102.25, 306.75 mg/kg; p.o.; single dose) can enhance the sleep of mice[6]. γ-Aminobutyric acid (1, 2, 4 mg/kg/d; p.o.; 30 d) alleviates anxiety and restored food utilization rate in rats, with impairment induced by Di(2-ethylhexyl) phthalate (DEHP) exposure[7].
Animal Model: | Pathogens free (SPF) Bagg’s albino (Balb/c) mice (18–20 g, 8 weeks old)[6] | Dosage: | 33.95, 102.25, 306.75 mg/kg | Administration: | Oral gavage; single dose; 20 mL/kg administration; measured in an hour | Result: | Prolonged the sleep duration, increased sleep rate, and shorten the sleep latency more effectively. |
Animal Model: | Sprague-Dawley rat indued byDEHP(HY-B1945) (500 mg/kg)[7] | Dosage: | 1, 2, 4 mg/kg | Administration: | Oral gavage; combined administration; for 30 consecutive days | Result: | Reduced the levels of nitric oxide and nitric oxide synthase in rats treated with DEHP. |
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结构分类 | - Ketones, Aldehydes, Acids
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来源 | mammalian central nervous system |
运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Powder | -20°C | 3 years | | 4°C | 2 years | In solvent | -80°C | 6 months | | -20°C | 1 month |
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溶解性数据 | In Vitro: H2O : 50 mg/mL(484.87 mM;Need ultrasonic) 配制储备液 1 mM | 9.6974 mL | 48.4872 mL | 96.9744 mL | 5 mM | 1.9395 mL | 9.6974 mL | 19.3949 mL | 10 mM | 0.9697 mL | 4.8487 mL | 9.6974 mL |
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