Miyazaki H, Takayama H, Minatogawa Y, Miyano K
Biomed Mass Spectrom. 1976 Jun;3(3):140-5. doi: 10.1002/bms.1200030309.
The metabolism of 5-(4'-chloro-n-butyl)picolinic acid, which inhibits dopamine beta-hydroxylase and exhibits an antihypertensive effect, has been studied by gas chromatography mass spectrometry, utilising characteristic reaction products after derivatization. In rat urine five metabolities were identified by mass spectral analysis. It is found that four were elongated by a C2 unit in the carboxyl group at the 2-position on the pyridine ring and accounted for approximately 50% of the radioactivity in the 24 hour urine. The facts show that the metabolic pathway corresponding to the chain elongation of fatty acids is the major route of metabolism for this drug in the rat. Furthermore, this pathway would be confirmed in man, rabbit, guinea pig and mouse.
5-(4'-氯正丁基)吡啶甲酸可抑制多巴胺β-羟化酶并具有降压作用，利用衍生化后的特征反应产物，通过气相色谱-质谱联用技术对其代谢情况进行了研究。通过质谱分析在大鼠尿液中鉴定出了五种代谢物。发现其中四种在吡啶环2位的羧基上通过一个C2单元进行了链延长，约占24小时尿液中放射性的50%。这些事实表明，与脂肪酸链延长相对应的代谢途径是该药物在大鼠体内的主要代谢途径。此外，在人、兔、豚鼠和小鼠中也证实了这一途径。
