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Azepines and piperidines with dual norepinephrine dopamine uptake inhibition and antidepressant activity.
Brown, Dean G; Bernstein, Peter R; Wu, Ye; Urbanek, Rebecca A; Becker, Christopher W; Throner, Scott R; Dembofsky, Bruce T; Steelman, Gary B; Lazor, Lois A; Scott, Clay W; Wood, Michael W; Wesolowski, Steven S; Nugiel, David A; Koch, Stephanie; Yu, Jian; Pivonka, Donald E; Li, Shuang; Thompson, Carol; Zacco, Anna; Elmore, Charles S; Schroeder, Patricia; Liu, JianWei; Hurley, Christopher A; Ward, Stuart; Hunt, Hazel J; Williams, Karen; McLaughlin, Joseph; Hoesch, Valerie; Sydserff, Simon; Maier, Donna; Aharony, David.
Afiliação
  • Brown DG; CNS Discovery Research, AstraZeneca Pharmaceuticals , 1800 Concord Pike, Wilmington, Delaware 19850-5437, United States.
  • Bernstein PR; CNS Discovery Research, AstraZeneca Pharmaceuticals , 1800 Concord Pike, Wilmington, Delaware 19850-5437, United States.
  • Wu Y; CNS Discovery Research, AstraZeneca Pharmaceuticals , 1800 Concord Pike, Wilmington, Delaware 19850-5437, United States.
  • Urbanek RA; CNS Discovery Research, AstraZeneca Pharmaceuticals , 1800 Concord Pike, Wilmington, Delaware 19850-5437, United States.
  • Becker CW; CNS Discovery Research, AstraZeneca Pharmaceuticals , 1800 Concord Pike, Wilmington, Delaware 19850-5437, United States.
  • Throner SR; CNS Discovery Research, AstraZeneca Pharmaceuticals , 1800 Concord Pike, Wilmington, Delaware 19850-5437, United States.
  • Dembofsky BT; CNS Discovery Research, AstraZeneca Pharmaceuticals , 1800 Concord Pike, Wilmington, Delaware 19850-5437, United States.
  • Steelman GB; CNS Discovery Research, AstraZeneca Pharmaceuticals , 1800 Concord Pike, Wilmington, Delaware 19850-5437, United States.
  • Lazor LA; CNS Discovery Research, AstraZeneca Pharmaceuticals , 1800 Concord Pike, Wilmington, Delaware 19850-5437, United States.
  • Scott CW; CNS Discovery Research, AstraZeneca Pharmaceuticals , 1800 Concord Pike, Wilmington, Delaware 19850-5437, United States.
  • Wood MW; CNS Discovery Research, AstraZeneca Pharmaceuticals , 1800 Concord Pike, Wilmington, Delaware 19850-5437, United States.
  • Wesolowski SS; CNS Discovery Research, AstraZeneca Pharmaceuticals , 1800 Concord Pike, Wilmington, Delaware 19850-5437, United States.
  • Nugiel DA; CNS Discovery Research, AstraZeneca Pharmaceuticals , 1800 Concord Pike, Wilmington, Delaware 19850-5437, United States.
  • Koch S; CNS Discovery Research, AstraZeneca Pharmaceuticals , 1800 Concord Pike, Wilmington, Delaware 19850-5437, United States.
  • Yu J; CNS Discovery Research, AstraZeneca Pharmaceuticals , 1800 Concord Pike, Wilmington, Delaware 19850-5437, United States.
  • Pivonka DE; CNS Discovery Research, AstraZeneca Pharmaceuticals , 1800 Concord Pike, Wilmington, Delaware 19850-5437, United States.
  • Li S; CNS Discovery Research, AstraZeneca Pharmaceuticals , 1800 Concord Pike, Wilmington, Delaware 19850-5437, United States.
  • Thompson C; CNS Discovery Research, AstraZeneca Pharmaceuticals , 1800 Concord Pike, Wilmington, Delaware 19850-5437, United States.
  • Zacco A; CNS Discovery Research, AstraZeneca Pharmaceuticals , 1800 Concord Pike, Wilmington, Delaware 19850-5437, United States.
  • Elmore CS; CNS Discovery Research, AstraZeneca Pharmaceuticals , 1800 Concord Pike, Wilmington, Delaware 19850-5437, United States.
  • Schroeder P; CNS Discovery Research, AstraZeneca Pharmaceuticals , 1800 Concord Pike, Wilmington, Delaware 19850-5437, United States.
  • Liu J; CNS Discovery Research, AstraZeneca Pharmaceuticals , 1800 Concord Pike, Wilmington, Delaware 19850-5437, United States.
  • Hurley CA; Argenta , 8/9 Spire Green Centre, Flex Meadow, Harlow, Essex, CM19 5TR, United Kingdom.
  • Ward S; Argenta , 8/9 Spire Green Centre, Flex Meadow, Harlow, Essex, CM19 5TR, United Kingdom.
  • Hunt HJ; Argenta , 8/9 Spire Green Centre, Flex Meadow, Harlow, Essex, CM19 5TR, United Kingdom.
  • Williams K; Argenta , 8/9 Spire Green Centre, Flex Meadow, Harlow, Essex, CM19 5TR, United Kingdom.
  • McLaughlin J; CNS Discovery Research, AstraZeneca Pharmaceuticals , 1800 Concord Pike, Wilmington, Delaware 19850-5437, United States.
  • Hoesch V; CNS Discovery Research, AstraZeneca Pharmaceuticals , 1800 Concord Pike, Wilmington, Delaware 19850-5437, United States.
  • Sydserff S; CNS Discovery Research, AstraZeneca Pharmaceuticals , 1800 Concord Pike, Wilmington, Delaware 19850-5437, United States.
  • Maier D; CNS Discovery Research, AstraZeneca Pharmaceuticals , 1800 Concord Pike, Wilmington, Delaware 19850-5437, United States.
  • Aharony D; CNS Discovery Research, AstraZeneca Pharmaceuticals , 1800 Concord Pike, Wilmington, Delaware 19850-5437, United States.
ACS Med Chem Lett ; 4(1): 46-51, 2013 Jan 10.
Article em En | MEDLINE | ID: mdl-24900562
Herein, we describe the discovery of inhibitors of norepinephrine (NET) and dopamine (DAT) transporters with reduced activity relative to serotonin transporters (SERT). Two compounds, 8b and 21a, along with nomifensine were tested in a rodent receptor occupancy study and demonstrated dose-dependent displacement of radiolabeled NET and DAT ligands. These compounds were efficacious in a rat forced swim assay (model of depression) and also had activity in rat spontaneous locomotion assay.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Idioma: En Ano de publicação: 2013 Tipo de documento: Article
Texto completo
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XML
PubMed Links
Buscar no Google

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Idioma: En Ano de publicação: 2013 Tipo de documento: Article