Abstract:
:Prolyl endopeptidase (PEP; EC 3.4.21.26) cleaves the Pro-Arg bond of arginine-vasopressin (AVP). This study investigated the effects of PEP inhibitors, 1-[1-(benzyloxycarbonyl)-L-prolyl]prolinal (Z-Pro-prolinal) and 1-[3-(2-indanylacetyl)-L-thioprolyl]pyrrolidine (Z-321), on the AVP content in the septum of rats. Oral administration of Z-Pro-prolinal (100 mg/kg) and Z-321 (100 mg/kg) significantly increased the septal AVP content. At 10 mg/kg, Z-321 slightly increased the content. In contrast, the D-thioprolyl form of Z-321 (100 mg/kg), which lacks an inhibitory effect on the enzyme, failed to affect the AVP content. These results indicate that PEP inhibitors increase the content of AVP through inhibition of the enzyme activity in vivo. Therefore, it is suggested that PEP may contribute to the degradation of endogenous AVP in the brain.
journal_name
Neurosci Lettjournal_title
Neuroscience lettersauthors
Miura N,Shibata S,Watanabe Sdoi
10.1016/0304-3940(95)11821-dsubject
Has Abstractpub_date
1995-08-18 00:00:00pages
128-30issue
1-2eissn
0304-3940issn
1872-7972pii
0304-3940(95)11821-Djournal_volume
196pub_type
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