Document Detail


New 3-[4-(3-substituted phenyl)piperazin-1-yl]-1-(benzo[b]thiophen-3-yl)propanol derivatives with dual action at 5-HT1A serotonin receptors and serotonin transporter as a new class of antidepressants.
MedLine Citation:
PMID:  12227188     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
In this paper a series of new 3-[4-(3-substituted phenyl)piperazin-1-yl]-1-(benzo[b]thiophen-3-yl)propanol derivatives is presented as a new class of antidepressant drugs with dual activity at 5-HT1A serotonin receptors and serotonin transporter. The 5-HT1A receptor and 5-HT transporter binding affinities of hydroxylic compounds 4 a-e have been determined. The new compounds present nanomolar affinity for both activities, and 1-(benzo[b]thiophen-3-yl)-3-[4-(3-methoxyphenyl)piperazin-1-yl]propan-1-ol (4d) shows values (nM) of Ki = 86 for 5-HT1A receptors and Ki = 76 for the serotonin transporter, respectively.
Authors:
L Orús; J Martínez; S Pérez; A M Oficialdegui; J C del Castillo; M Mourelle; B Lasheras; J del Río; A Monge
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Die Pharmazie     Volume:  57     ISSN:  0031-7144     ISO Abbreviation:  Pharmazie     Publication Date:  2002 Aug 
Date Detail:
Created Date:  2002-09-13     Completed Date:  2002-10-08     Revised Date:  2007-01-29    
Medline Journal Info:
Nlm Unique ID:  9800766     Medline TA:  Pharmazie     Country:  Germany    
Other Details:
Languages:  eng     Pagination:  515-8     Citation Subset:  IM    
Affiliation:
Department of Medicinal Chemistry, Centro de Investigación en Farmacobiología Aplicada, Universidad de Navarra, Pamplona, Spain.
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MeSH Terms
Descriptor/Qualifier:
Antidepressive Agents, Second-Generation / chemical synthesis*,  metabolism,  pharmacology*
Carrier Proteins / drug effects*
Indicators and Reagents
Kinetics
Membrane Glycoproteins / drug effects*
Membrane Transport Proteins*
Nerve Tissue Proteins*
Propanols / chemistry*
Protein Binding
Receptors, Serotonin / drug effects*
Receptors, Serotonin, 5-HT1
Serotonin Plasma Membrane Transport Proteins
Thiophenes / chemistry*
Chemical
Reg. No./Substance:
0/3-(4-(3-phenyl)piperazin-1-yl)-1-(benzo(b)thiophen-3-yl)propanol; 0/Antidepressive Agents, Second-Generation; 0/Carrier Proteins; 0/Indicators and Reagents; 0/Membrane Glycoproteins; 0/Membrane Transport Proteins; 0/Nerve Tissue Proteins; 0/Propanols; 0/Receptors, Serotonin; 0/Receptors, Serotonin, 5-HT1; 0/Serotonin Plasma Membrane Transport Proteins; 0/Thiophenes

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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