Design, synthesis, and pharmacological evaluation of azetedine and pyrrolidine derivatives as dual norepinephrine reuptake inhibitors and 5-HT 1A partial agonists

Bioorganic and Medicinal Chemistry Letters

Volumn 21, Issue 2, 2011, Pages 865-868

  Pettersson, Martin ^a   Campbell, Brian M ^a   Dounay, Amy B ^a   Gray, David L ^a   Xie, Longfei ^a   O'Donnell, Christopher J ^a   Stratman, Nancy C ^a   Zoski, Kim ^a   Drummond, Elena ^a   Bora, Gary ^a   Probert, Al ^a   Whisman, Tammy ^a  

^a PFIZER INC   (United States)

Author keywords

5 HT 1A agonist; ADHD; DAT; Depression; NET; Norepinephrine reuptake inhibitor; NRI; SERT

Indexed keywords

AZETIDINE DERIVATIVE; DOPAMINE TRANSPORTER; NORADRENALIN UPTAKE INHIBITOR; PYRROLIDINE DERIVATIVE; SEROTONIN 1A RECEPTOR;

ARTICLE; DOSE RESPONSE; DRUG DESIGN; DRUG PENETRATION; DRUG RECEPTOR BINDING; DRUG SYNTHESIS; EXPERIMENTAL DOG; MAXIMUM PLASMA CONCENTRATION; NONHUMAN; RECEPTOR OCCUPANCY;

ADRENERGIC UPTAKE INHIBITORS; ANIMALS; ANXIETY; ATTENTION DEFICIT DISORDER WITH HYPERACTIVITY; AZETIDINES; BRAIN; DEPRESSIVE DISORDER; DOGS; HUMANS; NOREPINEPHRINE; PYRROLIDINES; RECEPTOR, SEROTONIN, 5-HT1A; SEROTONIN 5-HT1 RECEPTOR AGONISTS;

EID: 78651258987     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2010.11.066     Document Type: Article

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19. Anhydrous HCl was generated by the addition of AcCl to MeOH at 0 °C.
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21. 3H]citalopram, respectively, using a scintillation proximity assay. Assay protocol is described in Ref. 14
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25. 1A receptor occupancy using competitive agonist binding assays.
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29. Monoamine functional assay conducted as described in Ref. 13