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Silanes SP, Orus L, Oficialdegui AM, Martinez Esparza J, Lasheras B, Del Rio J, Monge A: New 3-[4-(2,3-dihydro-14-benzodioxin-5-yl) piperazin-1-yl]-1-(5-substituted benzo [b] thiophen-3-yl) propanol derivatives with dual action at 5-HT (1A) serotonin receptors and serotonin transporter as a new class of antidepressants. Pharmazie. 2004 Jul;59(7):499-501.
Compounds derived from 2,3-dihydro-(1,4-benzodioxin-5-yl) piperazine and benzo [b] thiophene with different substituents in 5 position (H, F, NO2, NH2, CH3 and OH) have been synthesized in order to obtain new dual antidepressant drugs. The final compounds were evaluated for in vitro 5-HT (1A) receptor affinity and serotonin reuptake inhibition by radioligand assays. Compounds 1-(5-nitrobenzo [b] thiophen-3-yl)-3-[4-(2,3-dihydro-1,4-benzodioxin-5-yl) pi perazin-1-yl] propan-1-ol (4c) (Ki = 6.8 for 5-HT (1A) receptor and Ki = 14 for 5-HT transporter) and 1-(5-hydroxybenzo [b] thiophen-3-yl)-3-[4-(2,3-dihydro-1,4-benzodioxin-5-yl) piperazin-1-yl] propan-1-ol (4f) (Ki = 6.2 for 5-HT (1A) receptor and Ki = 18.2 for 5-HT transporter) showed the best results for both activities. |
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