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Title: [3H]desGly-NH2(9)-d(CH2)5[D-Ileu2,Ileu4]AVP: an AVP V2 receptor antagonist radioligand.
Austin Authors: Trinder, D;Stephenson, J M;Gao, X;Phillips, P A;Risvanis, John;Johnston, Colin I
Affiliation: University of Melbourne, Department of Medicine, Austin Hospital, Heidelberg, Victoria, Australia
Issue Date: 12-Nov-1991
Publication information: Peptides; 12(6): 1195-200
Abstract: Binding characteristics of the selective V2 antagonist radioligand [3H]desGly-NH2(9)-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-NH2(9)-d(CH2)5[D-Ileu2,Ileu4]AVP binding. The order of potency of inhibition was desamino-D-AVP greater than AVP greater than d(CH2)5[D-Ileu2,Ileu4]AVP greater than oxytocin greater than d(CH2)5[Tyr(Me)2]AVP greater than d(CH2)5[sarcosine7]AVP, which is typical of a selective V2 radioligand. Autoradiographic localization of [3H]desGly-NH2(9)-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.
Gov't Doc #: 1815207
Type: Journal Article
Subjects: Angiotensin Receptor Antagonists
Arginine Vasopressin.analogs & derivatives.metabolism
In Vitro Techniques
Kidney Medulla.metabolism
Radioligand Assay
Receptors, Angiotensin.classification.metabolism
Receptors, Vasopressin
Appears in Collections:Journal articles

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