Aminotriazine 5-HT7 antagonists

Bioorganic and Medicinal Chemistry Letters

Volumn 14, Issue 16, 2004, Pages 4245-4248

  Mattson, Ronald J ^a   Denhart, Derek J ^a   Catt, John D ^a   Dee, Michael F ^a   Deskus, Jeffrey A ^a   Ditta, Jonathan L ^a   Epperson, James ^a   Dalton King, H ^a   Gao, Aiming ^a   Poss, Michael A ^a   Purandare, Ashok ^a   Tortolani, David ^a   Zhao, Yufen ^a   Yang, Hua ^a   Yeola, Suresh ^a   Palmer, Jane ^a   Torrente, John ^a   Stark, Arlene ^a   Johnson, Graham ^a  

^a BRISTOL MYERS SQUIBB   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

SEROTONIN 2C RECEPTOR; SEROTONIN 6 RECEPTOR; SEROTONIN 7 RECEPTOR ANTAGONIST; SEROTONIN ANTAGONIST; UNCLASSIFIED DRUG; SEROTONIN 7 RECEPTOR; SEROTONIN RECEPTOR; TRIAZINE DERIVATIVE;

ANIMAL EXPERIMENT; ARTICLE; CONTROLLED STUDY; DOSE RESPONSE; DRUG BIOAVAILABILITY; DRUG RECEPTOR BINDING; DRUG SYNTHESIS; NONHUMAN; RAT; RECEPTOR AFFINITY; DRUG EFFECT;

DOSE-RESPONSE RELATIONSHIP, DRUG; RECEPTORS, SEROTONIN; SEROTONIN ANTAGONISTS; TRIAZINES;

EID: 16644377481     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2004.06.008     Document Type: Article

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20. +) 269.1 obsd.
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22. i values are determined using nonlinear regression by Exel-fit
23. + ion at m/z 367, 16 amu greater than parent, suggesting that they result from monohydroxylation. The MS/MS analysis of M2 (major) and M4 (minor) gave the same fragment ions at m/z 263 and 153 consistent with ortho- and para-hydroxylation on the phenoxy moiety. The fragment ions ( m/z 247 and 153) of metabolite M3 (minor) is identical to the parent compound, suggesting the hydroxyl group may be on the 2-phenylethyl moiety
24. i=4 ± 0.3 nM ( n=25 )
25. 125I]cAMP bound to fluomicrospheres was determined the following day by counting (2 min per well) in a Trilux MicroBeta counter. Counts (CPM's) from the assay were converted to picomoles using an Excel macro and the data plotted using GraphPad Prism