Spinal noradrenaline transporter inhibition by reboxetine and Xen2174 reduces tactile hypersensitivity after surgery in rats.

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Obata H, Conklin D, Eisenach JC

Spinal noradrenaline transporter inhibition by reboxetine and Xen2174 reduces tactile hypersensitivity after surgery in rats.

Pain. 2005 Feb;113(3):271-6.

PubMed ID
15661433 [ View in PubMed
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Abstract

Spinal noradrenaline (NA) released in response to noxious stimuli may play an important role in suppression of nociceptive transmission. Here, we investigated the efficacy of a competitive NA transporter inhibitor (reboxetine) and a noncompetitive NA transporter inhibitor peptide, Xen2174, isolated from the Pacific cone snail, to treat tactile hypersensitivity following paw incisional surgery. Male Sprague-Dawley rats were anesthetized, an incision of the plantar aspect of the hind paw was performed, and withdrawal threshold to von Frey filaments near the surgical site determined. Reboxetine (0.5-5 microg) and Xen2174 (0.3-100 microg) increased withdrawal threshold when injected 24h after paw incision, with a peak effect at 15-60 min, for Xen2174, an ED50 value of 0.64 microg. Administration of Xen2174 (3-30 microg) 15 min before incision also reduced hypersensitivity in a dose-dependent manner. Withdrawal threshold after the single 30 microg dose was greater than vehicle control even at 2, 3, and 5 days after incision. Doses

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