氨基丁酸(GABA)运输在人类肠道上皮细胞(Caco-2)层。

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Thwaites DT, Basterfield L, McCleave点,卡特SM,西蒙斯问

氨基丁酸(GABA)运输在人类肠道上皮细胞(Caco-2)层。

Br J杂志。2000年2月,129 (3):457 - 64。

PubMed ID

10711343 (在PubMed

]

文摘

1。Transintestinal吸收γ-氨基丁酸(GABA)通过pH-dependent机制在人类肠道上皮细胞系Caco-2模型。2。实验BCECF [2 ', 7 ', bis (2-carboxyethyl) 5 (6) - carboxyfluorescein])下载Caco-2细胞表明GABA运输在顶端膜耦合质子流进细胞。3所示。短路电流(ISC)测量使用Caco-2 voltage-clamped条件下单层细胞表明pH-dependent GABA运输是一个rheogenic过程即使没有细胞外钠+,符合H + / GABA同向转移。4所示。一系列GABA类似物进行测试的能力:(A)抑制pH-dependent [3 h] GABA摄取在顶端膜;(b)刺激H +流在顶端表面BCECF-loaded Caco-2细胞层;(c)内增加ISC跨voltage-clamped Caco-2细胞单层膜。 5. Nipecotic acid, isonipecotic acid, D,L-beta-aminobutyric acid, and 3-amino-1-propanesulphonic acid each caused a marked acidification of intracellular pH and an increase in ISC when superfused at the apical surface of Caco-2 cell monolayers. In contrast L-alpha-amino-n-butyric acid failed to induce proton flow or ISC. The ability of these compounds to induce proton or current flow across the apical surface of this intestinal epithelium was closely related to the relative inhibitory effects on [3H]GABA uptake. 6. These observations demonstrate H+/GABA symport and suggest that this transport mechanism may be accessible as a route for oral absorption of therapeutically-useful GABA analogues.

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药物转运蛋白

药物	转运体	类	生物	药理作用	行动
γ-氨基丁酸	Proton-coupled氨基酸转运体1	蛋白质	人类	未知的	不可用	细节
Nipecotic酸	Proton-coupled氨基酸转运体1	蛋白质	人类	未知的	不可用	细节