γ-aminobutyric acid amides of nortriptyline and fluoxetine display improved pain suppressing activity

Ada Rephaeli; Irit Gil-Ad; Ana Aharoni; Igor Tarasenko; Nataly Tarasenko; Yona Geffen; Efrat Halbfinger; Yotam Nisemblat; Abraham Weizman; Abraham Nudelman

doi:10.1021/jm900143u

γ-aminobutyric acid amides of nortriptyline and fluoxetine display improved pain suppressing activity

Ada Rephaeli^*, Irit Gil-Ad, Ana Aharoni, Igor Tarasenko, Nataly Tarasenko, Yona Geffen, Efrat Halbfinger, Yotam Nisemblat, Abraham Weizman, Abraham Nudelman

^*Corresponding author for this work

Clinical Departments

Research output: Contribution to journal › Article › peer-review

14 Scopus citations

Abstract

The GABA amides of the antidepressants nortriptyline and fluoxetine, 1 and 2, were compared to their respective parent compounds in rodent models of pain. The amides significantly reduced early nociceptive and late inflammatory responses compared to nortriptyline or fluoxetine, where 1 exhibited overall better efficacy than 2. Amide 1 was most efficacious in lowering cytokine secretion, edema and hyperalgesia induced by formalin and λ-carrageenan, respectively. Thus, 1 is a promising candidate for the treatment of pain.

Original language	English
Pages (from-to)	3010-3017
Number of pages	8
Journal	Journal of Medicinal Chemistry
Volume	52
Issue number	9
DOIs	https://doi.org/10.1021/jm900143u
State	Published - 14 May 2009

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title = "γ-aminobutyric acid amides of nortriptyline and fluoxetine display improved pain suppressing activity",

abstract = "The GABA amides of the antidepressants nortriptyline and fluoxetine, 1 and 2, were compared to their respective parent compounds in rodent models of pain. The amides significantly reduced early nociceptive and late inflammatory responses compared to nortriptyline or fluoxetine, where 1 exhibited overall better efficacy than 2. Amide 1 was most efficacious in lowering cytokine secretion, edema and hyperalgesia induced by formalin and λ-carrageenan, respectively. Thus, 1 is a promising candidate for the treatment of pain.",

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AU - Rephaeli, Ada

AU - Gil-Ad, Irit

AU - Aharoni, Ana

AU - Tarasenko, Igor

AU - Tarasenko, Nataly

AU - Geffen, Yona

AU - Halbfinger, Efrat

AU - Nisemblat, Yotam

AU - Weizman, Abraham

AU - Nudelman, Abraham

PY - 2009/5/14

Y1 - 2009/5/14

N2 - The GABA amides of the antidepressants nortriptyline and fluoxetine, 1 and 2, were compared to their respective parent compounds in rodent models of pain. The amides significantly reduced early nociceptive and late inflammatory responses compared to nortriptyline or fluoxetine, where 1 exhibited overall better efficacy than 2. Amide 1 was most efficacious in lowering cytokine secretion, edema and hyperalgesia induced by formalin and λ-carrageenan, respectively. Thus, 1 is a promising candidate for the treatment of pain.

AB - The GABA amides of the antidepressants nortriptyline and fluoxetine, 1 and 2, were compared to their respective parent compounds in rodent models of pain. The amides significantly reduced early nociceptive and late inflammatory responses compared to nortriptyline or fluoxetine, where 1 exhibited overall better efficacy than 2. Amide 1 was most efficacious in lowering cytokine secretion, edema and hyperalgesia induced by formalin and λ-carrageenan, respectively. Thus, 1 is a promising candidate for the treatment of pain.

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JO - Journal of Medicinal Chemistry

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IS - 9

ER -

γ-aminobutyric acid amides of nortriptyline and fluoxetine display improved pain suppressing activity

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