780744-67-4Relevant academic research and scientific papers
Benzothiophene derivatives and corresponding use and composition
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, (2008/06/13)
Benzothiophene derivative compounds and corresponding use and composition; the compounds respond to formula (I): where Z is: —CO—, —CH(OR6)—, —C(NOR7)—; R1is: H, C1-C6alkyl, halogen, or —OR8/sub
New 3-[4-(aryl)piperazin-1-yl]-1-(benzo[b]thiophen-3-yl)propane derivatives with dual action at 5-HT1A serotonin receptors and serotonin transporter as a new class of antidepressants
Martinez, Javier,Perez, Silvia,Oficialdegui, Ana M,Heras, Begona,Orus, Lara,Villanueva, Helena,Palop, Juan A,Roca, Joan,Mourelle, Marisa,Bosch, Ana,Del Castillo, Juan-C,Lasheras, Berta,Tordera, Rosa,Del Rio, Joaquin,Monge, Antonio
, p. 55 - 61 (2007/10/03)
A series of new 3-[4-(aryl)piperazin-1-yl]-1-(benzo[b]thiophen-3-yl)propane derivatives were synthesized in an attempt to find a new class of antidepressant drugs with dual activity at 5-HT1A serotonin receptors and serotonin transporter. Title compounds were evaluated for in vitro activity on 5-HT1A receptor and 5-HT transporter. They show high nanomolar affinity for both activities, and in particular, compounds 1-(5-chlorobenzo[b]thiophen-3-yl)-3-[4-(2-methoxyphenyl)piperazin-1-yl] propan-1-ol (7) and 1-(5-fluorobenzo[b]thiophen-3-yl)-3-[4-(2-methoxyphenyl)piperazin-1-yl] propan-1-ol (8) show values (nM) of Ki = 30 and 2.3 for 5-HT1A receptors and Ki = 30 and 12 for serotonin transporters, respectively. In GTPγS binding assays, compound 8 revealed antagonist properties to 5-HT1A receptors. Such a pharmacological profile could lead to potent antidepressant agents with new dual mechanism of action.
