[3H]desGly-NH29-d(CH2)5[D-Ileu2,Ileu4]AVP: An AVP V2 receptor antagonist radioligand

D. Trinder, J. M. Stephenson, X. Gao, P. A. Phillips, J. Risvanis, C. I. Johnston

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21 Citations (Scopus)

Abstract

Binding characteristics of the selective V2 antagonist radioligand [3H]desGly-NH29-d(CH2)5[D-Ileu2,Ileu4]AVP to rat kidney were determined. Binding was specific, saturable and reversible. The peptide bound to a single class of high-affinity binding sites with Bmax 69.4±6.8 fmol/mg protein and KD 2.8±0.3 nM. AVP and other related peptides displaced [3H]desGly-NH29-d(CH2)5[D-Ileu2,Ileu4]AVP binding. The order of potency of inhibition was desamino-D-AVP > AVP > d(CH2)5[D-Ileu2,Ileu4]AVP > oxytocin > d(CH2)3[Tyr(Me)2]AVP > d(CH2)5[sarcosine7]AVP, which is typical of a selective V2 radioligand. Autoradiographic localization of [3H]desGly-NH29-d(CH2)5[D-Ileu2,Ileu4]AVP binding sites in kidney showed dense binding in the inner and outer medulla with less binding in the cortex, which is consistent with known renal V2 receptor distribution.

Original languageEnglish
Pages (from-to)1195-1200
Number of pages6
JournalPeptides
Volume12
Issue number6
DOIs
Publication statusPublished - 1991
Externally publishedYes

Keywords

  • AVP antagonist
  • Kidney
  • V receptor
  • Vasopressin

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    Trinder, D., Stephenson, J. M., Gao, X., Phillips, P. A., Risvanis, J., & Johnston, C. I. (1991). [3H]desGly-NH29-d(CH2)5[D-Ileu2,Ileu4]AVP: An AVP V2 receptor antagonist radioligand. Peptides, 12(6), 1195-1200. https://doi.org/10.1016/0196-9781(91)90194-T