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nisoxetine

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Also known as DL-N-Methyl-3-(o-methoxyphenoxy)-N-methyl-3-phenylpropylamine, N-Methyl-gamma-(2-methylphenoxy)phenylpropanolamine, 3-(o-Methoxyphenoxy)-N-methyl-3-phenylpropylamine, 3-(2-Methoxyphenoxy)-N-methyl-3-phenylpropylamine

Nisoxetine (developmental code name LY-94939), originally synthesized in the Lilly research laboratories during the early 1970s, is a potent and selective inhibitor for the reuptake of norepinephrine (noradrenaline) into synapses. It currently has no clinical applications in humans, although it was originally researched as an antidepressant. Nisoxetine is now widely used in scientific research as a standard selective norepinephrine reuptake inhibitor. It has been used to research obesity and energy balance, and exerts some local analgesia effects.

Wikidata facts

Mass
271.157229
Show 4 more facts
chemical formula
C₁₇H₂₁NO₂
canonical SMILES
CNCCC(C1=CC=CC=C1)OC2=CC=CC=C2OC
World Health Organisation international non-proprietary name
nisoxetine
Commons category
Nisoxetine
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~14 min read

Encyclopedic overview

11 sections
Contents
  • History
  • Research
  • Obesity
  • Analgesia effects
  • <sup>3</sup>H-nisoxetine
  • NET imaging using PET
  • Pharmacological properties
  • Adverse effects
  • Chemical properties
  • See also
  • References

Nisoxetine (developmental code name LY-94939), originally synthesized in the Lilly research laboratories during the early 1970s, is a potent and selective inhibitor for the reuptake of norepinephrine (noradrenaline) into synapses. It currently has no clinical applications in humans, although it was originally researched as an antidepressant. Nisoxetine is now widely used in scientific research as a standard selective norepinephrine reuptake inhibitor. It has been used to research obesity and energy balance, and exerts some local analgesia effects.

Researchers have attempted to use a carbon-labeled form of nisoxetine for positron emission tomography (PET) imaging of the norepinephrine transporter (NET), with little success. However, it seems that tritium-labeled nisoxetine (3H-nisoxetine, 3H-NIS) is a useful radioligand for labeling norepinephrine uptake sites in vitro, which nisoxetine and other antagonists for NET are able to inhibit.

Excerpted from Wikipedia’s “nisoxetine” article, available under the CC BY-SA 4.0 licence.

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