Varga L, Sasvári M, Penke B, Baláspiri L, Varró V
Acta Hepatogastroenterol (Stuttg). 1979 Dec;26(6):499-503.
The metabolism of labelled BOC-14 C-glycine-pentapetide was investigated in rats, both in blood and urine. We report on the following findings: --radioactivity could be measured in the blood even after the disappearance of the bioactive- and immunoreactive pentapeptide. --the bulk of the radioactivity in the blood after 8 minutes originates from a metabolite which, after subsequent systematic chemical identification, proved to be the BOC-14C-glycine fragment of the pentapeptide. --the radioactivity in the urine comes entirely from this split product of the labelled pentapeptide --the organ distribution of radioactivity of labelled pentapeptide was checked after i.v. administration; 1 minute after the injection, most of the radioactivity was found in the liver, followed by the kidney, pancreas, jejunum and lung. After 1 hour, radioactivity could be detected only in the kidneys. It was concluded that the N-terminal amino-acid of the naturally occurring pentagastrin (glycine) remains linked to the BOC protecting group in the course of the catabolism of the molecule and this fragment is excreted in the urine.
在大鼠体内对标记的BOC-¹⁴C-甘氨酸五肽的代谢进行了血液和尿液方面的研究。我们报告以下发现:——即使生物活性和免疫反应性五肽消失后,血液中仍可检测到放射性。——8分钟后血液中的大部分放射性来自一种代谢物,经后续系统化学鉴定,证明是五肽的BOC-¹⁴C-甘氨酸片段。——尿液中的放射性完全来自标记五肽的这种裂解产物。——静脉注射后检查了标记五肽放射性的器官分布;注射后1分钟,大部分放射性见于肝脏,其次是肾脏、胰腺、空肠和肺。1小时后,仅在肾脏中可检测到放射性。得出的结论是,天然存在的五肽胃泌素(甘氨酸)的N端氨基酸在分子分解代谢过程中仍与BOC保护基团相连,且该片段经尿液排出。