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Titolo:
New 3-[4-(aryl)piperazin-1-yl]-1(benzo[b]thiophen3-yl) propane derivativeswith dual action at 5-HT1A serotonin receptors and serotonin transporter as a new class of antidepressants
Autore:
Martinez, J; Perez, S; Oficialdegui, AM; Heras, B; Orus, L; Villanueva, H; Palop, JA; Roca, J; Mourelle, M; Bosch, A; Del Castillo, JC; Lasheras, B; Tordera, R; del Rio, J; Monge, A;
Indirizzi:
Univ Navarra, Dept Med Chem, E-31080 Pamplona, Spain Univ Navarra Pamplona Spain E-31080 pt Med Chem, E-31080 Pamplona, Spain Univ Navarra, CIFA, E-31080 Pamplona, Spain Univ Navarra Pamplona Spain E-31080 varra, CIFA, E-31080 Pamplona, Spain Univ Navarra, Dept Pharmacol, E-31080 Pamplona, Spain Univ Navarra Pamplona Spain E-31080 t Pharmacol, E-31080 Pamplona, Spain Vita Invest SA, Barcelona 08970, Spain Vita Invest SA Barcelona Spain 08970 a Invest SA, Barcelona 08970, Spain
Titolo Testata:
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
fascicolo: 1, volume: 36, anno: 2001,
pagine: 55 - 61
SICI:
0223-5234(200101)36:1<55:N3PD>2.0.ZU;2-Q
Fonte:
ISI
Lingua:
ENG
Soggetto:
EXTRACELLULAR 5-HT; REUPTAKE INHIBITOR; IN-VIVO; PINDOLOL; AUTORECEPTORS; COMBINATION; ANTAGONIST; PAROXETINE;
Keywords:
arylpiperazines; antidepressant; 5-HT1A antagonist; serotonin reuptake inhibitor;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
22
Recensione:
Indirizzi per estratti:
Indirizzo: Monge, A Univ Navarra, Dept Med Chem, C Irunlarrea S-N, E-31080 Pamplona, Spain Univ Navarra C Irunlarrea S-N Pamplona Spain E-31080 lona, Spain
Citazione:
J. Martinez et al., "New 3-[4-(aryl)piperazin-1-yl]-1(benzo[b]thiophen3-yl) propane derivativeswith dual action at 5-HT1A serotonin receptors and serotonin transporter as a new class of antidepressants", EUR J MED C, 36(1), 2001, pp. 55-61

Abstract

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) piperain-1-yl]propan-1-ol (8) showvalues (nM) of K-i = 30 and 2.3 for 5-HT1A receptors and K-i = 30 and 12 for serotonin transporters, respectively. In GTP gammaS 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. (C) 2001 Editions scientifiques et medicales Elsevier SAS.

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Documento generato il 25/09/20 alle ore 22:42:47