Literature DB >> 11128642

Serotonin transporter inhibitors: synthesis and binding potency of 2'-methyl- and 3'-methyl-6-nitroquipazine.

J M Gerdes1, S C DeFina, P A Wilson, S E Taylor.   

Abstract

Racemic 2'-methyl- and 3'-methyl-6-nitroquipazine ligands were selected as targets, synthesized and evaluated at the serotonin transporter employing an in vitro competitive inhibition assay with [3H]paroxetine and rat cortical membrane. The 2'-methyl-6-nitroquipazine was found to be 50 times more potent than the 3'-methyl-substituted counterpart and of comparable potency to the known high affinity agent 5-iodo-6-nitroquipazine.

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Year:  2000        PMID： 11128642     DOI： 10.1016/s0960-894x(00)00546-1

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  2 in total

1.  Synthesis, in vitro binding studies and docking of long-chain arylpiperazine nitroquipazine analogues, as potential serotonin transporter inhibitors.

Authors:  Małgorzata Jarończyk; Karol Wołosewicz; Mari Gabrielsen; Gabriel Nowak; Irina Kufareva; Aleksander P Mazurek; Aina W Ravna; Ruben Abagyan; Andrzej J Bojarski; Ingebrigt Sylte; Zdzisław Chilmonczyk
Journal:  Eur J Med Chem       Date:  2012-01-15       Impact factor: 6.514

2.  Synthesis, antidepressant evaluation and docking studies of long-chain alkylnitroquipazines as serotonin transporter inhibitors.

Authors:  Mari Gabrielsen; Karol Wołosewicz; Anna Zawadzka; Jerzy Kossakowski; Gabriel Nowak; Małgorzata Wolak; Katarzyna Stachowicz; Agata Siwek; Aina W Ravna; Irina Kufareva; Lech Kozerski; Elżbieta Bednarek; Jerzy Sitkowski; Wojciech Bocian; Ruben Abagyan; Andrzej J Bojarski; Ingebrigt Sylte; Zdzisław Chilmonczyk
Journal:  Chem Biol Drug Des       Date:  2013-04-11       Impact factor: 2.817
  2 in total

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