Novel selective and potent 5-HT reuptake inhibitors with 5-HT1D antagonist activity: chemistry and pharmacological evaluation of a series of thienopyran derivatives |
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| Authors: | Torrado Alicia Lamas Carlos Agejas Javier Jiménez Alma Diaz Nuria Gilmore Jeremy Boot John Findlay Jeremy Hayhurst Lorna Wallace Louise Broadmore Richard Tomlinson Rosemarie |
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| Affiliation: | Lilly, S. A., Avenida de la Industria, 30, 28108 Alcobendas, Madrid, Spain. torrado_alicia@lilly.com |
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| Abstract: | A series of compounds combining the naphthylpiperazine and thienopyran scaffolds has been prepared and evaluated for 5-HT reuptake inhibition with 5-HT1D antagonist activity. The design of these compounds has been based on the 'overlapping type' strategy where two pharmacophores are linked in a single molecule. The resultant dual pharmacological profile has the potential to deliver a more efficient treatment for depression. |
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