Formation of metabolites of [Arg8]vasopressin (AVP) by brain peptidases

FEBS Letters

Burbach, J.Peter H.¹  Wang, Xin-Chang¹ 

[1] Rudolf Magnus Institute for Pharmacology, Medical Faculty, University of Utrecht, Vondellaan 6, 3521 GD Utrecht, The Netherlands

关键词: Vasopressin;    Neuropeptide;    Peptidase;    Peptide metabolism;    AVP;    [Arg8]vasopressin (H-Cys-Tyr-PheGln-Asn-Cys-Pro-Leu-Glu-NH2);   

DOI  :  10.1016/0014-5793(86)80319-2

学科分类：生物化学/生物物理

来源: John Wiley & Sons Ltd.

【 摘 要 】

[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), [pGlu⁶,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.

【 授权许可】

Unknown