[3H]-GR113808 labels 5-HT4 receptors in the human and guinea-pig brain.
A tritiated specific and highly potent 5-HT4 antagonist: [3H]-GR113808 was used to label specific binding sites in human brain and for comparison in guinea-pig brain. [3H]-GR113808 association and dissociation were rapid, the binding was saturable and displaced by various serotoninergic agents with an affinity corresponding to their previously reported 5-HT4 receptor mediated effects. In vitro ligand binding autoradiography was used to investigate the distribution of [3H]-GR113808 recognition sites on human brain sections. The highest density was observed in the striato-nigral system. Low densities of binding sites were also found in hippocampus, neocortex and colliculus. This distribution of [3H]-GR113808 binding sites is similar to that found in the guinea-pig brain.
Waeber
C
C
CNRS, UPR 9023, CCIPE, Montpellier, France.
Sebben
M
M
Grossman
C
C
Javoy-Agid
F
F
Bockaert
J
J
Dumuis
A
A
D000368:Aged; D000369:Aged, 80 and over; D000818:Animals; D001345:Autoradiography; D001667:Binding, Competitive / Q000187:drug effects; D001923:Brain Chemistry / Q000187:drug effects*; D005260:Female; D006168:Guinea Pigs; D006801:Humans; D066298:In Vitro Techniques; D007211:Indoles / Q000493:pharmacokinetics / Q000494:pharmacology*; D008566:Membranes / Q000378:metabolism; D011869:Radioligand Assay; D012702:Serotonin Antagonists; D013449:Sulfonamides / Q000493:pharmacokinetics / Q000494:pharmacology*
D007211:Indoles; D012702:Serotonin Antagonists; D013449:Sulfonamides; C082871:GR 113808