A novel radioiodinated high affinity ligand for the D2‐dopamine receptor

FEBS Letters

Amlaiky, Nourdine¹  Kilpatrick, Brian F.¹  Caron, Marc G.¹ 

[1] Departments of Physiology and Medicine, Howard Hughes Medical Institute, Duke University Medical Center, Durham, NC 27710, USA

关键词: D2-dopamine receptor;    Radioiodinated ligand;    High affinity radioligand;    Anterior pituitary;   

DOI  :  10.1016/0014-5793(84)81213-2

学科分类：生物化学/生物物理

来源: John Wiley & Sons Ltd.

【 摘 要 】

A novel high affinity dopaminergic ligand, N-(p-aminophenethyl)spiroperidol, has been synthesized and radioiodinated to a specific radioactivity of 2175 . Binding of this ligand to bovine anterior pituitary membranes is: (i) rapid (40–60 min to equilibrium at 25°C) and reversible t = 1 h at 25°C); (ii) saturable and of high affinity (K _D ~ 20 pM) and (iii) displays a typical D₂-dopaminergic specificity. The ligand, which identifies the same number of receptor sites as other tritiated antagonist ligands, can be used in different tissues and preparations to delineate the characteristics of the D₂ receptor. Thus, this high affinity, high specific radioactivity ligand (N-(p-amino-m-[¹²⁵I]iodophenethyl)spiroperidol) represents a tool which until now had not been available for the characterization of the D₂-dopamine receptor.

【 授权许可】

Unknown