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

…, I Tarasenko, N Tarasenko, Y Geffen…

Index: Nudelman, Abraham; Gil-Ad, Irit; Shpaisman, Nava; Terasenko, Igor; Ron, Hanna; Savitsky, Kinneret; Geffen, Yona; Weizman, Abraham; Rephaeli, Ada Journal of Medicinal Chemistry, 2008 , vol. 51, # 9 p. 2858 - 2862

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Citation Number: 10

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 ...