Wang X C, Burbach J P
FEBS Lett. 1986 Mar 3;197(1-2):164-8. doi: 10.1016/0014-5793(86)80319-2.
[Cyt6]AVP-(3-9), an intermediate in the metabolism of AVP-(1-9) in vitro, was used to investigate the mechanism of formation of centrally active AVP metabolites. Exposure of [Cyt6]AVP-(3-9) to rat brain membranes resulted in formation of [Cyt6]AVP-(4-9), -(5-9), [pGlu4, Cyt6]AVP-(4-9) and AVP-(3-5), which were isolated and chemically identified. Products derived from cleavage of the C-terminus of the substrate were absent. Time-course experiments further indicated that the conversion process is predominantly mediby an aminopeptidase-like mechanism. The conversion of [Cyt6]AVP-(3-9) by membranes from hippocampus, amygdala and septum was quantitatively and qualitatively similar. The results point to a major role of aminopeptidase activity in the metabolic conversion of AVP and the formation of centrally active AVP metabolites.
[Cyt6]精氨酸加压素-(3-9)是精氨酸加压素-(1-9)体外代谢的中间产物，用于研究中枢活性精氨酸加压素代谢产物的形成机制。将[Cyt6]精氨酸加压素-(3-9)与大鼠脑膜一起孵育，结果形成了[Cyt6]精氨酸加压素-(4-9)、-(5-9)、[焦谷氨酸4，Cyt6]精氨酸加压素-(4-9)和精氨酸加压素-(3-5)，这些产物经过分离和化学鉴定。未发现底物C末端裂解产生的产物。时间进程实验进一步表明，转化过程主要由一种氨肽酶样机制介导。海马、杏仁核和隔区的膜对[Cyt6]精氨酸加压素-(3-9)的转化在数量和质量上相似。结果表明氨肽酶活性在精氨酸加压素的代谢转化和中枢活性精氨酸加压素代谢产物的形成中起主要作用。
