In vivo binding of [3H]ketanserin on serotonin S2-receptors in rat brain.
In vivo binding of [3H]ketanserin was studied in various brain regions in rats. After i.v. injection of [3H]ketanserin (5 micrograms . kg-1), the highest labelling was found in the frontal cortex. Brain disposition of labelled drug correlated with the distribution of serotonin S2-receptors detected in vitro. The binding was saturable in the serotonergic areas but not in the cerebellum. Various drugs were tested for their ability to displace or to prevent [3H]ketanserin binding: these results were then compared to those obtained with [3H]spiperone in the frontal cortex. Although [3H]spiperone can be used to differentiate the affinity of a drug for serotonin (frontal cortex) and dopamine (striatum) receptors, the great advantage of [3H]ketanserin is that it labels serotonin S2-receptors exclusively.
D000818:Animals; D001921:Brain / Q000378:metabolism*; D007650:Ketanserin; D008297:Male; D010880:Piperidines / Q000378:metabolism*; D051381:Rats; D011919:Rats, Inbred Strains; D011985:Receptors, Serotonin / Q000378:metabolism*; D012702:Serotonin Antagonists / Q000378:metabolism*; D013134:Spiperone / Q000378:metabolism; D014316:Tritium
D010880:Piperidines; D011985:Receptors, Serotonin; D012702:Serotonin Antagonists; D014316:Tritium; D013134:Spiperone; D007650:Ketanserin