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A novel radioiodinated high affinity ligand for the D 2 ‐dopamine receptor
Author(s) -
Amlaiky Nourdine,
Kilpatrick Brian F.,
Caron Marc G.
Publication year - 1984
Publication title -
febs letters
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.593
H-Index - 257
eISSN - 1873-3468
pISSN - 0014-5793
DOI - 10.1016/0014-5793(84)81213-2
Subject(s) - ligand (biochemistry) , dopaminergic , receptor , chemistry , dopamine , dopamine receptor d2 , dopamine receptor , spiperone , antagonist , stereochemistry , biochemistry , biology , endocrinology
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 D 2 ‐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 D 2 receptor. Thus, this high affinity, high specific radioactivity ligand ( N ‐( p ‐amino‐ m ‐[ 125 I]iodophenethyl)spiroperidol) represents a tool which until now had not been available for the characterization of the D 2 ‐dopamine receptor.