磺酰脲类药物相互作用与胆汁酸的运输到肝细胞。

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Fuckel D, Petzinger E

磺酰脲类药物相互作用与胆汁酸的运输到肝细胞。

欧元J杂志。1992年3月31日,213 (3):393 - 404。

PubMed ID

1618280 (在PubMed

]

文摘

磺酰脲类化合物glisoxepide和格列本脲抑制吸收胆汁酸进入分离大鼠肝细胞。Ki值抑制胆盐吸收与格列本脲和200 9 microM microM glisoxepide。胆盐的抑制吸收由磺脲类非竞争性。吸收结合胆汁酸的牛磺胆酸盐抑制了格列本脲,Ki = 75 microM。又非竞争性抑制。Glisoxepide抑制牛磺胆酸盐摄入钠离子的缺乏。钠的条件下glisoxepide还强烈抑制胆盐吸收。抑制竞争,Ki = 42 microM。两种胆汁酸干扰[3 h] glisoxepide的肝细胞吸收,与375年和467年的IC50值microM胆盐和牛磺胆酸盐,分别。的吸收[3 h]格列本脲抑制胆盐,IC50 = 328 microM,但不是由牛磺胆酸盐。 Glisoxepide uptake was further inhibited by blockers of the hepatocellular monocarboxylate transporter, by the loop diuretic bumetanide, by 4,4'-diisothiocyano-2,2'-stilbenedisulfonate (DIDS) and by sulfate. Glibenclamide uptake was weakly inhibited by DIDS and by anthracene-9-carboxylic acid (A-9-C) but not by bumetanide and sulfate. Neither bromosulfophthalein nor the fatty acid oleate inhibited glisoxepide or glibenclamide uptake. These results are consistent with the transport of glisoxepide via the transport system for the unconjugated bile acid cholate. Glibenclamide uptake is mediated by a still unknown hepatocellular transport system.

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药物

Glisoxepide