Synthesis, in vitro binding profile, and CNS penetrability of the highly potent 5-HT3 receptor antagonist [3H]-4-(2-methoxyphenyl)-2-[4 (5)-methyl-5 (4)- …
4-(2-Methoxyphenyl)-2-[4 (5)-methyl-5 (4)-imidazolylmethyl] thiazole (5) is a highly potent member of a structurally novel series of selective serotonin-3 receptor antagonists. The synthesis of tritiated 5 and its binding profile in neuroblastoma-glioma 108-15 cells are described. Furthermore, in vivo studies in rat with this radioligand indicate that it effectively penetrates the blood-brain barrier upon peripheral administration. Thus, 5 should be a ...
