[Synthesis and pharmacological study of radioiodinated serotonin derivative specific of 5-HT1B and 5-HT1D binding sites of the central nervous system].
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.
Segu
L
L
C.N.R.S. Laboratoire de Neurobiologie, Marseille.
Chauveau
J
J
Boulenguez
P
P
Morel
A
A
Lanoir
J
J
Delaage
M
M
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
D007457:Iodine Radioisotopes; D008024:Ligands; D011985:Receptors, Serotonin; D012701:Serotonin
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.