Haloperidol‐succinylglycyl[125I]iodotyrosine, a novel iodinated ligand for dopamine D2 receptors

FEBS Letters

Delaage, M.¹  Gehelmann, F.¹  Girault, J.M.¹  Labouesse, J.¹  Garrigues, A.M.¹ 

[1] IBCN-CNRS, 1 rue Camille Saint-Saëns, 33077 Bordeaux Cedex and Immunotech, Lumigny, 13288 Marseille Cedex 9, France

关键词: Dopamine D2 receptor;    Radioiodinated ligand;    (Striatum);   

DOI  :  10.1016/0014-5793(87)80467-2

学科分类：生物化学/生物物理

来源: John Wiley & Sons Ltd.

【 摘 要 】

A novel radioiodinated ligand of the butyrophenone type has been synthesized for the quantification and characterization of dopamine D₂ receptors. This haloperidol-derived ligand, haloperidol-succinylglycyl-[¹²⁵I]iodotyrosine ([¹²⁵I]HSGTI), binds rapidly (equilibrium is reached within 30 min, at 10 pM and 37°C) and with high affinity (K _d=0.3 nM) to bovine striatal membranes. Its pharmacology, determined by competitive displacement with dopaminergic and non-dopaminergic drugs, is characteristic of binding to dopamine D₂ receptors.

【 授权许可】

Unknown