Fraser R, Holloway C D, Kenyon C J
J Steroid Biochem. 1986 Mar;24(3):777-8. doi: 10.1016/0022-4731(86)90857-5.
The potassium entry blocker, 4-aminopyridine has been used to evaluate the importance of this cation in several tissues including the adrenal cortex. Since it inhibited corticosteroidogenesis, an important role for potassium entry in the control of this process has been implied. In the present in vitro study, 4-aminopyridine inhibited cortisol and corticosterone production and, at high concentrations, that of 11-deoxycortisol and 11-deoxycorticosterone. However, at lower concentrations, 11-deoxycorticosteroid production increased suggesting that 4-aminopyridine acts as an inhibitor of 11 beta hydroxylation. Its slight resemblance to metyrapone may suggest that it acts, at least in part, by competing for cytochrome P450. However, its use as a potassium inhibitor in studies of the adrenal cortex may give ambiguous results.
钾离子进入阻滞剂4-氨基吡啶已被用于评估这种阳离子在包括肾上腺皮质在内的多种组织中的重要性。由于它抑制了皮质类固醇生成,这意味着钾离子进入在该过程的控制中起着重要作用。在目前的体外研究中,4-氨基吡啶抑制了皮质醇和皮质酮的产生,在高浓度时,还抑制了11-脱氧皮质醇和11-脱氧皮质酮的产生。然而,在较低浓度下,11-脱氧皮质类固醇的产生增加,这表明4-氨基吡啶是11β-羟化作用的抑制剂。它与甲吡酮有轻微相似之处,这可能表明它至少部分地通过与细胞色素P450竞争而起作用。然而,在肾上腺皮质研究中把它用作钾离子抑制剂可能会得出不明确的结果。