title: [Synthesis and pharmacological study of radioiodinated serotonin derivative specific of 5-HT1B and 5-HT1D binding sites of the central nervous system].
abstract: We describe here the synthesis of a new serotonin conjugate, S-CM-GTNH2, and its radioiodinated derivative. Quantitative autoradiographic studies on rat and guinea pig brain sections incubated with 2 nM [3H]5-HT showed a preferential affinity of S-CM-GTNH2 for 5-HT1B and 5-HT1D sites. Autoradiograms from brain sections incubated with 0.02 nM S-CM-G[125I]TNH2 showed a heterogeneous anatomical distribution of the labelling with high densities in regions rich in 5-HT1B or 5-HT1D binding sites, and with no labelling of those rich in 5-HT1A or 5-HT1C sites. The pharmacological profiles of the binding sites corresponded to those of 5-HT1B and 5-HT1D receptor subtypes. The radioligand S-CM-G[125I]TNH2 is a good probe for the study of these sites and will be used for their subcellular localization in electron microscopy.
authors.affiliation: C.N.R.S. Laboratoire de Neurobiologie, Marseille.
authors.forename: L
authors.initials: L
authors.lastname: Segu
authors.forename: J
authors.initials: J
authors.lastname: Chauveau
authors.forename: P
authors.initials: P
authors.lastname: Boulenguez
authors.forename: A
authors.initials: A
authors.lastname: Morel
authors.forename: J
authors.initials: J
authors.lastname: Lanoir
authors.forename: M
authors.initials: M
authors.lastname: Delaage
mesh_terms: D000818:Animals; D002490:Central Nervous System / Q000378:metabolism*; D006168:Guinea Pigs; D007457:Iodine Radioisotopes; D008024:Ligands; D051381:Rats; D011985:Receptors, Serotonin / Q000378:metabolism*; D012701:Serotonin / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology
chemical_list: D007457:Iodine Radioisotopes; D008024:Ligands; D011985:Receptors, Serotonin; D012701:Serotonin
vernacular_title: Synthèse et étude pharmacologique d'un dérivé radioiodé de la sérotonine spécifique des sites de liaison 5-HT1B et 5-HT1D du système nerveux central.