Increase in the septal vasopressin content by prolyl endopeptidase inhibitors in rats

Naoyoshi Miura, Shigenobu Shibata, Shigenori Watanabe

研究成果: Article

39 引用 (Scopus)

抄録

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.

元の言語English
ページ(範囲)128-130
ページ数3
ジャーナルNeuroscience Letters
196
発行部数1-2
DOI
出版物ステータスPublished - 1995 8 18
外部発表Yes

Fingerprint

prolyl oligopeptidase
Arginine Vasopressin
Protease Inhibitors
Vasopressins
prolylarginine
Enzymes
Oral Administration
1-(3-(2-indanylacetyl)-L-thioprolyl)pyrrolidine
Peptamen

ASJC Scopus subject areas

  • Neuroscience(all)

これを引用

Increase in the septal vasopressin content by prolyl endopeptidase inhibitors in rats. / Miura, Naoyoshi; Shibata, Shigenobu; Watanabe, Shigenori.

:: Neuroscience Letters, 巻 196, 番号 1-2, 18.08.1995, p. 128-130.

研究成果: Article

Miura, Naoyoshi ; Shibata, Shigenobu ; Watanabe, Shigenori. / Increase in the septal vasopressin content by prolyl endopeptidase inhibitors in rats. :: Neuroscience Letters. 1995 ; 巻 196, 番号 1-2. pp. 128-130.
@article{8a257af4c22b4183ab1f62437b493f11,
title = "Increase in the septal vasopressin content by prolyl endopeptidase inhibitors in rats",
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.",
keywords = "Arginine-vasopressin, Inhibitors, Metabolism, Prolyl endopeptidase, Septum",
author = "Naoyoshi Miura and Shigenobu Shibata and Shigenori Watanabe",
year = "1995",
month = "8",
day = "18",
doi = "10.1016/0304-3940(95)11821-D",
language = "English",
volume = "196",
pages = "128--130",
journal = "Neuroscience Letters",
issn = "0304-3940",
publisher = "Elsevier Ireland Ltd",
number = "1-2",

}

TY - JOUR

T1 - Increase in the septal vasopressin content by prolyl endopeptidase inhibitors in rats

AU - Miura, Naoyoshi

AU - Shibata, Shigenobu

AU - Watanabe, Shigenori

PY - 1995/8/18

Y1 - 1995/8/18

N2 - 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.

AB - 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.

KW - Arginine-vasopressin

KW - Inhibitors

KW - Metabolism

KW - Prolyl endopeptidase

KW - Septum

UR - http://www.scopus.com/inward/record.url?scp=0029125636&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=0029125636&partnerID=8YFLogxK

U2 - 10.1016/0304-3940(95)11821-D

DO - 10.1016/0304-3940(95)11821-D

M3 - Article

C2 - 7501240

AN - SCOPUS:0029125636

VL - 196

SP - 128

EP - 130

JO - Neuroscience Letters

JF - Neuroscience Letters

SN - 0304-3940

IS - 1-2

ER -