Document Detail

Biological half-life and organ distribution of [3H]8-arginine vasopressin following administration of vasopressin receptor antagonist OPC-31260.
MedLine Citation:
PMID:  17258819     Owner:  NLM     Status:  MEDLINE    
The effects of the antidiuretic (V(2)) non-peptide receptor antagonist OPC-31260 on the plasma vasopressin level and the biological half-life and organ distribution of radiochemically pure, biologically active [(3)H]8-arginine vasopressin [spec. act.: 15.9 mCi/mmol (588 GBq/mmol)] were studied in Wistar rats. The plasma vasopressin level increased significantly throughout the whole experimental period (24 h). There was no change in the fast phase of the curves of total radioactivity disappearance from the plasma after the administration of [(3)H]arginine vasopressin (control: 1.51+/-0.17 min, OPC-31260-treated: 1.42+/-0.12 min, n=10). The fast phase of the disappearance curves of intact [(3)H]arginine vasopressin did not change either following the administration of OPC-31260 in a dose of 30 mg/kg p.o. (control: 1.06+/-0.19 min, OPC-31260-treated: 1.00+/-0.15 min, n=6). The slow phase of the biological half-life, which is characteristic for the examined compound, proved to be significantly longer (total radioactivity control: 9.29+/-0.61 min, OPC-31260-treated: 12.33+/-0.42 min, P<0.05, n=10; [(3)H]arginine vasopressin radioactivity: control: 5.96+/-0.58 min, OPC-31260-treated: 8.90+/-0.37 min, P<0.05, n=6). In the control rats, the radioactivity was accumulated to the greatest extent in the neurohypophysis, adenohypophysis and kidney. Following OPC-31260 administration, significantly more radioactive compounds accumulated in the kidney (control: 0.30+/-0.052 total radioactivity %/100 mg organ weight, OPC-31260-treated: 0.50+/-0.133 total radioactivity %/100 mg organ weight, P<0.05, n=10) and neurohypophysis (control: 0.37+/-0.053 total radioactivity %/100 mg organ weight, OPC-31260-treated: 0.52+/-0.076 total radioactivity %/100 mg organ weight, P<0.05, n=10). Our results permit the conclusion that the antidiuretic antagonist OPC-31260 not only blocks the V(2) receptors, but also increases the biological half-life of vasopressin. The longer biological half-life of vasopressin following OPC-31260 administration may play a role in the elevation of the plasma vasopressin level.
Andor H Molnár; Csaba Varga; Tamás Janáky; Gábor Tóth; Géza Tóth; Judit Farkas; Ferenc László; Ferenc A László
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Publication Detail:
Type:  Comparative Study; Journal Article; Research Support, Non-U.S. Gov't     Date:  2007-01-04
Journal Detail:
Title:  Regulatory peptides     Volume:  141     ISSN:  0167-0115     ISO Abbreviation:  Regul. Pept.     Publication Date:  2007 Jun 
Date Detail:
Created Date:  2007-04-02     Completed Date:  2007-07-17     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  8100479     Medline TA:  Regul Pept     Country:  Netherlands    
Other Details:
Languages:  eng     Pagination:  12-8     Citation Subset:  IM    
Department of Comparative Physiology, University of Szeged, Szeged, Középfasor 52, H-6726, Hungary.
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MeSH Terms
Arginine Vasopressin / blood,  pharmacokinetics*
Benzazepines / administration & dosage,  pharmacology*
Kidney / metabolism*
Pituitary Gland, Anterior / metabolism*
Pituitary Gland, Posterior / metabolism*
Rats, Wistar
Receptors, Vasopressin / antagonists & inhibitors*
Tissue Distribution
Reg. No./Substance:
0/Benzazepines; 0/Receptors, Vasopressin; 10028-17-8/Tritium; 113-79-1/Arginine Vasopressin; 137975-06-5/OPC 31260

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