Properties of a new radioiodinated antagonist for human vasopressin V2 and V1a receptors.
A vasopressin receptor antagonist, [1-(beta-mercapto-beta,beta-pentamethylenepropionic acid), 2-o-ethyl-D-tyrosine, 4-valine, 9-tyrosylamide] arginine vasopressin (d(CH2)5[o-ethyl-D-Tyr2,Val4,Tyr-NH9(2)]AVP), has been prepared. This antagonist is a potent antiantidiuretic, antivasopressor and antioxytocic peptide with pA2 values of 7.69-7.94 and affinities of 1.12-11.0 nM. When radioiodinated at the phenyl moiety of the tyrosylamide residue at position 9, this peptide was demonstrated to bind to vasopressin V2 and V1a receptors with a dissociation constant of 0.22-0.75 nM. This ligand is a good tool for further studies on human vasopressin V2 receptor localization and characterization, when used in combination with a selective vasopressin V1a ligand.
Ala
Y
Y
Unité INSERM 469, Centre CNRS-INSERM de Pharmacologie-Endocrinologie, Montpellier, France.
Morin
D
D
Mahé
E
E
Cotte
N
N
Mouillac
B
B
Jard
S
S
Barberis
C
C
Tribollet
E
E
Dreifuss
J J
JJ
Sawyer
W H
WH
Wo
N C
NC
Chan
W Y
WY
Kolodziejczyk
A S
AS
Cheng
L L
LL
Manning
M
M
D000818:Animals; D065092:Antidiuretic Hormone Receptor Antagonists; D001127:Arginine Vasopressin / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D001345:Autoradiography; D004247:DNA / Q000096:biosynthesis; D004231:Diuresis / Q000187:drug effects; D006801:Humans; D007293:Inosine Triphosphate / Q000378:metabolism; D007457:Iodine Radioisotopes; D051381:Rats; D018045:Receptors, Oxytocin / Q000187:drug effects / Q000378:metabolism; D017483:Receptors, Vasopressin / Q000096:biosynthesis / Q000378:metabolism
D065092:Antidiuretic Hormone Receptor Antagonists; D007457:Iodine Radioisotopes; D018045:Receptors, Oxytocin; D017483:Receptors, Vasopressin; C108519:argipressin, d(CH2)5-O-ethyl-Tyr(2)-Val(4)-Tyr-NH2(9)-; D001127:Arginine Vasopressin; D007293:Inosine Triphosphate; D004247:DNA