Elands J, Barberis C, Jard S, Lammek B, Manning M, Sawyer W H, de Kloet E R
Centre CNRS-INSERM de Pharmacologie-Endocrinologie, Montpellier, France.
FEBS Lett. 1988 Mar 14;229(2):251-5. doi: 10.1016/0014-5793(88)81135-9.
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.
一种放射性碘化血管加压素拮抗剂d(CH2)5[Tyr(NH2)9]AVP已被制备出来。碘化反应在第9位酪氨酰胺残基的苯基部分进行，随后通过高效液相色谱法进行纯化。未标记的单碘化拮抗剂用作鉴定的参考物。125I-d(CH2)5[Tyr(Me)2, Tyr(NH2)9]AVP与大鼠肝细胞膜上的V1血管加压素受体结合，解离常数为0.28±0.09 nM（Kd±标准差）。
