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Haloperidol‐succinylglycyl[ 125 I]iodotyrosine, a novel iodinated ligand for dopamine D 2 receptors
Author(s) -
Garrigues A.M.,
Gehelmann F.,
Girault J.M.,
Delaage M.,
Labouesse J.
Publication year - 1987
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(87)80467-2
Subject(s) - butyrophenone , haloperidol , chemistry , dopaminergic , ligand (biochemistry) , dopamine receptor , dopamine receptor d2 , receptor , dopamine , dopamine antagonist , apomorphine , stereochemistry , endocrinology , biochemistry , biology
A novel radioiodinated ligand of the butyrophenone type has been synthesized for the quantification and characterization of dopamine D 2 receptors. This haloperidol‐derived ligand, haloperidol‐succinylglycyl‐[ 125 I]iodotyrosine ([ 125 I]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 D 2 receptors.