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| 【主 题】 ： |
Reboxetine |
| 【联系人名】 ： |
Linna Green |
| 【电子邮件】 ： |
account@bocsci.com |
| 【联系电话】 ： |
15166698109 |
| 【发布日期】 ： |
2016-9-6 |
| 【详细说明】 ： |
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.
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English
