Stark H, Burbach J P, Van der Kleij A A, De Wied D
Rudolf Magnus Institute, Medical Faculty, University of Utrecht, The Netherlands.
Peptides. 1989 Jul-Aug;10(4):717-20. doi: 10.1016/0196-9781(89)90102-2.
The nonapeptide [Arg8]vasopressin was rapidly degraded with a half-life of lower than 1 minute after local administration into the hippocampus. During the conversion of vasopressin C-terminal fragments were transiently generated. The profile of these metabolites indicated that they were formed by aminopeptidase activity. The aminopeptidase inhibitor amastatin partially inhibited the conversion of vasopressin. A minor pathway involved cleavages in the C-terminus. The results indicate a predominant involvement of aminopeptidase activity in the in vivo metabolism of exogenous vasopressin in the brain. Since products of this metabolic route have been shown to have potent behavioral activities, the behavioral effects seen after microinjection of vasopressin in the brain may be partially due to generation of vasopressin fragments.
九肽[精氨酸8]加压素在局部注入海马体后迅速降解，半衰期低于1分钟。在加压素的转化过程中，C末端片段会短暂生成。这些代谢物的特征表明它们是由氨肽酶活性形成的。氨肽酶抑制剂抑氨肽酶素部分抑制了加压素的转化。一条次要途径涉及C末端的裂解。结果表明氨肽酶活性在脑中外源性加压素的体内代谢中起主要作用。由于这条代谢途径的产物已被证明具有强大的行为活性，因此在脑内微量注射加压素后观察到的行为效应可能部分归因于加压素片段的生成。
