2,4-二氨基丁酸对4-氨基丁酸摄取和结合抑制作用的立体特异性。
Stereospecificity of 2,4-diaminobutyric acid with respect to inhibition of 4-aminobutyric acid uptake and binding.
作者信息
Johnston G A, Twitchin B
出版信息
Br J Pharmacol. 1977 Jan;59(1):218-9. doi: 10.1111/j.1476-5381.1977.tb06998.x.
Abstract
S(+)-2,4-Diaminobutyric acid is at least 20 times more potent than the R(-) stereoisomer as an inhibitor of the sodium-dependent uptake of 4-aminobutyric acid (GABA) in rat brain slices. Both isomers, however, are equipotent as inhibitors of sodium-independent binding of GABA to membranes from rat brain. The latter finding may be relevant to the reported neurotoxicity in rats of both isomers of 2,4-diaminobutyric acid after intracisternal injection.
摘要
作为大鼠脑切片中4-氨基丁酸（GABA）钠依赖性摄取的抑制剂，S(+)-2,4-二氨基丁酸的效力至少是R(-)立体异构体的20倍。然而，两种异构体作为GABA与大鼠脑膜钠非依赖性结合的抑制剂时效力相当。后一发现可能与脑池内注射2,4-二氨基丁酸两种异构体后在大鼠中报道的神经毒性有关。
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