125I-d(CH2)5[Tyr(Me)2, Tyr(NH2)9]AVP: iodination and binding characteristics of a vasopressin receptor ligand.
A radioiodinated vasopressin antagonist, d(CH2)5[Tyr(NH2)9]AVP has been prepared. Iodination was carried out at the phenyl moiety of the tyrosylamide residue at position 9, followed by HPLC purification. Non-radiolabelled monoiodinated antagonist was used as a reference for identification. 125I-d(CH2)5[Tyr(Me)2, Tyr(NH2)9]AVP binding appeared to take place with a dissociation constant of 0.28 +/- 0.09 nM (Kd +/- SD) to V1 vasopressin receptors on rat liver membranes.
Elands
J
J
Centre CNRS-INSERM de Pharmacologie-Endocrinologie, Montpellier, France.
Barberis
C
C
Jard
S
S
Lammek
B
B
Manning
M
M
Sawyer
W H
WH
de Kloet
E R
ER
D000818:Animals; D001127:Arginine Vasopressin / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000378:metabolism* / Q000494:pharmacology; D002462:Cell Membrane / Q000378:metabolism; D005260:Female; D007202:Indicators and Reagents; D007457:Iodine Radioisotopes; D007668:Kidney / Q000378:metabolism; D007700:Kinetics; D008099:Liver / Q000378:metabolism; D051381:Rats; D011919:Rats, Inbred Strains; D011945:Receptors, Angiotensin / Q000378:metabolism*; D017483:Receptors, Vasopressin; D014599:Uterus / Q000378:metabolism
D007202:Indicators and Reagents; D007457:Iodine Radioisotopes; D011945:Receptors, Angiotensin; D017483:Receptors, Vasopressin; D001127:Arginine Vasopressin; C055245:argipressin, beta mercapto-beta,beta-cyclopentamethylenepropionic acid(1)-O-methyl-Tyr(2)-TyrNH2(9)-