A selective biotinylated probe for V1a vasopressin receptors

John Howl, Ian D. Kerr, Conrad H.W. Chan, Mark Wheatley

Research output: Contribution to journalArticlepeer-review

13 Citations (Scopus)


We have designed and synthesized a biotinylated vasopressin antagonist which is a selective probe for studying the V1a subtype of vasopressin receptor. Initially we synthesized the novel vasopressin analogue d(CH2)5Tyr(Me)2LysNH29AVP (ALVP). Biotinamidocaproate was subsequently coupled to the ε{lunate}-amino group of ALVP to generate the novel biotinylated probe d(CH2)5Tyr(Me)2Lys(Nε{lunate}-biotinamidocaproate) NH29AVP (ALBtnVP). Pharmacological characterization of ALVP and ALBtnVP established that both ligands were high affinity antagonists at V1a receptors, and that both displayed marked V1a/V2 selectivity. The observation that receptor-bound ALBtnVP was bi-functional, and thereby able to bind conjugated derivatives of avidin or streptavidin, allowed ALBtnVP to be utilized as a selective probe for V1a receptors. This strategy allowed the visualization of V1a receptors on the surface of WRK-1 cells and hippocampal neurons, by using streptavidin-gold with electron microscopy and fluorescein-avidin with light microscopy. We conclude that ALBtnVP is a useful probe for V1a receptors.

Original languageEnglish
Pages (from-to)123-131
Number of pages9
JournalMolecular and Cellular Endocrinology
Issue number1-3
Publication statusPublished - May 1991
Externally publishedYes


  • Biotin
  • V receptor
  • Vasopressin

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Biology
  • Endocrinology


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