Novel selective and potent 5-HT reuptake inhibitors with 5-HT1D antagonist activity: chemistry and pharmacological evaluation of a series of thienopyran derivatives.

The synthesis and in vitro activity of a novel series of thienopyran derivatives is described. The compounds exhibit dual potency as 5-HT reuptake inhibitors and 5-HT1D antagonists, and feature desirable selectivity with respect to 5-HT1B, α1 and D2.