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W2013095956 abstract "Starting from the potent and selective but poorly brain penetrant 5-HT6 receptor antagonist SB-271046, a successful strategy for improving brain penetration was adopted involving conformational constraint with concomitant reduction in hydrogen bond count. This provided a series of bicyclic heteroarylpiperazines with high 5-HT6 receptor affinity. 5-Chloroindole 699929 combined high 5-HT6 receptor affinity with excellent brain penetration and also had good oral bioavailability in both rat and dog." @default.
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W2013095956 date "2005-11-01" @default.
W2013095956 modified "2023-10-16" @default.
W2013095956 title "Bicyclic heteroarylpiperazines as selective brain penetrant 5-HT6 receptor antagonists" @default.
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W2013095956 doi "https://doi.org/10.1016/j.bmcl.2005.06.107" @default.
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