| 规格: | 98% |
| 分子量: | 91.1 |
| 包装 | 价格(元) |
| 100mg | 电议 |
| 250mg | 电议 |
| 500mg | 电议 |
| 1g | 电议 |
Background:
Aminooxyacetic acid is a GABA transaminase (GABA-T) inhibitor (Ki = 9.16 μM) that induces GABA accumulation in the brain.1 It also inhibits cystathionine β synthase (CBS) and cystathionine γ lyase (CSE; IC50s = 8.5 and 1.1 μM, respectively).2 Aminooxyacetic acid (100 mg/kg) decreases GABA-T activity, without affecting glutamic acid decarboxylase (GAD) activity, and increases GABA levels in all regions of rat brain.3 It also decreases GABA-T activity and increases GABA in mouse brain when administered at a dose of 13 mg/kg.4 Aminooxyacetic acid inhibits 3-mercaptopropionic acid-, strychnine-, and pentetrazole-induced seizures in mice (ED50s = 53, 130, and 85 mg/kg, respectively), however, it exhibits neurotoxicity in the chimney test (ED50 = 62 mg/kg) and is lethal (LD50 = 105 mg/kg) to mice.
参考文献
1. Wallach, D.P. Studies on the GABA pathway. I. The inhibition of γ-aminobutyric acid-α-ketoglutaric acid transaminase in vitro and in vivo by U-7524 (amino-oxyacetic acid). Biochem. Pharmacol. 5(4), 323-331 (1961).
2. Asimakopoulou, A., Panopoulos, P., Chasapis, C.T., et al. Selectivity of commonly used pharmacological inhibitors for cystathionine β synthase (CBS) and cystathionine γ lyase (CSE). Br. J. Pharmacol. 169(4), 922-932 (2013).
3. L?scher, W., H?nack, D., and Gramer, M. Use of inhibitors of gamma-aminobutyric acid (GABA) transaminase for the estimation of GABA turnover in various brain regions of rats: A reevaluation of aminooxyacetic acid. J. Neurochem. 53(6), 1737-1750 (1989).
4. L?scher, W. A comparative study of the pharmacology of inhibitors of GABA-metabolism. Naunyn Schmiedebergs Arch. Pharmacol. 315(2), 119-128 (1980).
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