Ponchant M, Beaucourt J P, Vanhove A, Daval G, Vergé D, Hamon M, Gozlan H
Service des Molécules marquées, C.E.A.-Saclay, Gif-sur-Yvette.
C R Acad Sci III. 1988;306(4):147-52.
Specific radioactive ligands are needed for studying the pharmacological properties and the regional distribution of the different classes of 5-HT1 receptors within the central nervous system. We describe here the synthesis and some characteristics of the first iodinated specific ligand of 5-HT1A receptors. Like its parent compound, the agonist 8-hydroxy-2-(di-n-propylamino)tetralin or 8-OH-DPAT, [125I]-BH-8-MeO-N-PAT, exhibits a high affinity and excellent selectivity for 5-HT1A sites. Its high specific radioactivity makes this ligand a useful tool for studying 5-HT1A receptors in membranes and sections of the rat brain.