Reboxetine and (2E,13Z)-Octadecadienal

Reboxetine and (2E,13Z)-Octadecadienal

Posted by Ada Brown on Dec 15, 2016 3:35 am


Reboxetine, also called as Vestra, 2-((2-ethoxyphenoxy)benzyl)morpholine methanesulfonate, exists as two enantiomers, (R,R)-(-)- and (S,S)-(+)-reboxetine. Ti is a selective norepinephrine reuptake inhibitor used in the treatment of clinical depression, panic disorder and ADD/ADHD which has been approved for treatment of major depression. In vitro: it inhibits noradrenaline reuptake in vitro to a similar extent to the tricyclic antidepressant desmethylimipramine and does not inhibit the activity of the following isozymes of cytochrome P450: CYP1A2, CYP2C9, CYP2C19, and CYP2E1; In vivo: Reboxetine does not affect dopamine or serotonin reuptake and it has low in vivo and in vitro affinity for adrenergic, cholinergic, histaminergic, dopaminergic and serotonergic receptors.Besides, it inhibits both CYP2D6 and CYP3A4 with low binding affinities, but has shown no effect on the in vivo clearance of drugs metabolized by these enzymes. Inhibits (±)-epibatidine-induced Ca(2+) influx in human (h) muscle embryonic (hα1β1γδ) and adult (hα1β1εδ) AChRs in a non-competitive manner , with potencies IC50= 3.86±0.49 and 1.92±0.48 μM, respectively.

2'-DEOXY-2'-FLUORO-5-IODOCYTIDINE, also called AC1NQP33, SCHEMBL138935, under the IUPAC name 4-amino-1-[(2R,3R,4R,5R)-3-fluoro-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]-5-iodopyrimidin-2-one; 80791-93-1, is a potent anti-​hepatitis C virus (HCV) agent.Several 2'-​deoxy-​2'-​halogenoarabinofuranosylcytosines and -​uracils substituted at C-​5 of the aglycon with Br or I were prepd. and evaluated for antiherpetic activity against both herpes virus type 1 and 2 on monolayers of Vero cells by the plaque redn. assay. A dose that reduced the no. of virus plaques by 50​% (ED50) was detd. The 2'-​F function showed better antiviral activity than the corresponding 2'-​Br or Cl congeners.

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