Checler F, Kostolanska B, Fox J A
Centre de Biochimie du Centre National de la Recherche Scientifique, Nice, France.
J Pharmacol Exp Ther. 1988 Mar;244(3):1040-4.
The metabolism of tritiated neurotensin (NT) after close i.a. perfusion in ileal segments of anesthetized dog was studied. Venous effluents containing labeled metabolites and intact NT were collected and analyzed by high-performance liquid chromatography. The apparent half-life of the peptide was between 2 and 6 min. The tritiated metabolites of NT were identified as free tyrosine, NT-(1-7), NT-(1-8), NT-(1-10), NT-(11-13) and NT-(1-11). Pretreatment of dog ileum with thiorphan or captopril indicated that endopeptidase 24-11 inactivated NT by cleaving the peptide at the Pro10-Tyr11 and Tyr11-Ile12 bonds. Angiotensin-converting enzyme only participated in the secondary conversion of NT-(1-10) into NT-(1-8). The metabolisms of NT occurring in vivo and in vitro in central and peripheral organs are compared.
研究了在麻醉犬回肠段进行紧密动脉内灌注后,氚标记神经降压素(NT)的代谢情况。收集含有标记代谢产物和完整NT的静脉流出物,并通过高效液相色谱法进行分析。该肽的表观半衰期在2至6分钟之间。NT的氚标记代谢产物被鉴定为游离酪氨酸、NT-(1-7)、NT-(1-8)、NT-(1-10)、NT-(11-13)和NT-(1-11)。用硫磷酰胺或卡托普利预处理犬回肠表明,内肽酶24-11通过在Pro10-Tyr11和Tyr11-Ile12键处切割肽来使NT失活。血管紧张素转换酶仅参与NT-(1-10)向NT-(1-8)的二次转化。比较了NT在中枢和外周器官体内和体外的代谢情况。