[125I-BH-8-MeO-N-PAT, a new ligand for the study of 5-HT1A receptors in the central nervous system].
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.
Ponchant
M
M
Service des Molécules marquées, C.E.A.-Saclay, Gif-sur-Yvette.
Beaucourt
J P
JP
Vanhove
A
A
Daval
G
G
Vergé
D
D
Hamon
M
M
Gozlan
H
H
D017371:8-Hydroxy-2-(di-n-propylamino)tetralin; D000818:Animals; D001667:Binding, Competitive; D001921:Brain / Q000378:metabolism*; D006624:Hippocampus / Q000378:metabolism; D007457:Iodine Radioisotopes; D008024:Ligands; D009281:Naphthalenes / Q000378:metabolism*; D051381:Rats; D011985:Receptors, Serotonin / Q000378:metabolism*; D013764:Tetrahydronaphthalenes / Q000138:chemical synthesis / Q000378:metabolism*
D007457:Iodine Radioisotopes; D008024:Ligands; D009281:Naphthalenes; D011985:Receptors, Serotonin; D013764:Tetrahydronaphthalenes; C055126:8-methoxy-2-(N-propyl-N-(3'-iodo-4'-hydroxyphenyl)-propionamido-N'-propylamino)tetralin; D017371:8-Hydroxy-2-(di-n-propylamino)tetralin
125I-BH-8-MeO-N-PAT, un nouveau ligand pour l'étude des récepteurs 5-HT1A dans le système nerveux central.