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The kinetic and pharmacological characteristics of the binding of [³H]ketanserin and [³H]mesulergine to frontal cortical brain membranes from rat, pig and human were studied. In the 3 species [³H]ketanserin labeled sites with the characteristics of the 5-HT₂ receptors previously described in the rat. In contrast, [³H]mesulergine labeled 5-HT₂ receptors in rat, but not in pig and human cortices. The characteristics of the sites labeled by [³H]mesulergine in pig cortex were similar to those of sites in the choroid plexus of rats, pigs and humans. While several reputed 5-HT₂ ligands presented a similar affinity for the [³H]ketanserin binding sites in the 3 species, other such ligands, e.g. mesulergine, methysergide, cinanserin and LSD which displaced these sites with high affinity in rat brain, had lower affinities in pig and human brain. These results indicate that 5-HT₂ receptors show different pharmacologial profiles in …