Levine S D, Franki N, Einhorn R, Hays R M
Kidney Int. 1976 Jan;9(1):30-5. doi: 10.1038/ki.1976.4.
Vasopressin is known to increase the permeability of the toad bladder, an analogue of the mammalian collecting duct, to water and hydrophilic solutes such as urea. In the present study, the effect of vasopressin on the permeability of a series of lipophilic compounds, including many commonly used drugs, has been determined. In all cases, permeability increased from 50 to 100%. The response to vasopressin was mediated by cyclic adenosine monophosphate (cAMP), and was generally not altered by phloretin, an agent that inhibits amide movement through the amide transport pathway. Evidence that these compounds move directly through the lipid phase of the membrane was provided in studies of phenobarbital permeability at low and high luminal pH. We would conclude from these studies that the effect of vasopressin on the luminal cell membrane is a widespread one, modifying both lipid components and components involved in amide, sodium and water transport. This may be of importance in the renal tubular reabsorption of many drugs, including barbiturates, glutethimide and antibiotics.
已知血管加压素可增加蟾蜍膀胱(类似于哺乳动物集合管)对水和亲水性溶质(如尿素)的通透性。在本研究中,已确定血管加压素对一系列亲脂性化合物(包括许多常用药物)通透性的影响。在所有情况下,通透性增加了50%至100%。对血管加压素的反应由环磷酸腺苷(cAMP)介导,并且通常不受根皮素(一种抑制酰胺通过酰胺转运途径移动的物质)的影响。在低管腔pH值和高管腔pH值下对苯巴比妥通透性的研究中,提供了这些化合物直接通过膜脂质相移动的证据。从这些研究中我们可以得出结论,血管加压素对管腔细胞膜的作用是广泛的,它会改变脂质成分以及参与酰胺、钠和水转运的成分。这可能对包括巴比妥类药物、格鲁米特和抗生素在内的许多药物的肾小管重吸收具有重要意义。