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|Title:||[3H]desGly-NH2(9)-d(CH2)5[D-Ileu2,Ileu4]AVP: an AVP V2 receptor antagonist radioligand.|
|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|
|Citation:||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.|
|Internal ID Number:||1815207|
|Subjects:||Angiotensin Receptor Antagonists|
Arginine Vasopressin.analogs & derivatives.metabolism
In Vitro Techniques
|Appears in Collections:||Journal articles|
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