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Synthesis and monoamine transporter affinity of new 2β-carbomethoxy-3β-[4-(substituted thiophenyl)]phenyltropanes: discovery of a selective SERT antagonist with picomolar potency

Author
TAMAGNAN, Gilles1 2 ; ALAGILLE, David1 ; XING FU1 ; KULA, Nora S3 ; BALDESSARINI, Ross J3 ; INNIS, Robert B1 ; BALDWIN, Ronald M1
[1] Department of Psychiatry, Yale University and VA Connecticut/116A2, 950 Campbell Avenue, West Haven, CT 06516, United States
[2] Institute for Neurodegenerative Disorders, 60 Temple Street, Suite 8A, New Haven, CT 06510, United States
[3] Department of Psychiatry and Neuroscience Program, Harvard Medical School and Mailman Research Center, McLean Division of Massachusetts General Hospital, Belmont, MA 02478-9106, United States
Source

Bioorganic & medicinal chemistry letters (Print). 2005, Vol 15, Num 4, pp 1131-1133, 3 p

ISSN
0960-894X
Scientific domain
Biochemistry, molecular biology, biophysics; Pharmacology drugs
Publisher
Elsevier, Oxford
Publication country
United Kingdom
Document type
Article
Language
English
Keyword (fr)
Affinité Amine biogène Antagoniste In vitro Neurotransmetteur Relation structure activité Synthèse chimique Sélectivité Sérotonine Thiophène dérivé Transport biologique Transport membranaire Tropane dérivé 8-Azabicyclo[3.2.1]octane dérivé Transporteur sérotonine Tropane-2β-carboxylique acide(3β-[4-(3-thiényl)phényl]) ester méthyle
Keyword (en)
Affinity Biogenic amine Antagonist In vitro Neurotransmitter Structure activity relation Chemical synthesis Selectivity Serotonin Thiophene derivatives Biological transport Membrane transport Tropane derivatives
Keyword (es)
Afinidad Amina biógena Antagonista In vitro Neurotransmisor Relación estructura actividad Síntesis química Selectividad Serotonina Tiofeno derivado Transporte biológico Transporte membranal
Classification
Pascal
002 Biological and medical sciences / 002B Medical sciences / 002B02 Pharmacology. Drug treatments / 002B02B Neuropharmacology / 002B02B09 Neurotransmitters. Neurotransmission. Receptors / 002B02B09C Serotoninergic system

Discipline
Pharmacological treatments
Origin
Inist-CNRS
Database
PASCAL
INIST identifier
16480705

Sauf mention contraire ci-dessus, le contenu de cette notice bibliographique peut être utilisé dans le cadre d’une licence CC BY 4.0 Inist-CNRS / Unless otherwise stated above, the content of this bibliographic record may be used under a CC BY 4.0 licence by Inist-CNRS / A menos que se haya señalado antes, el contenido de este registro bibliográfico puede ser utilizado al amparo de una licencia CC BY 4.0 Inist-CNRS

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