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Biotech / Medical : ACADIA Pharmaceuticals Inc (ACAD)
ACAD 26.56+2.6%3:59 PM EST

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To: scaram(o)uche who wrote (46)11/10/2004 5:22:34 PM
From: scaram(o)uche   of 588
 
Neuroreport. 2004 Sep 15;15(13):2071-5.

Stimulation of PAR-2 excites and sensitizes rat cutaneous C-nociceptors to heat.

Ding-Pfennigdorff D, Averbeck B, Michaelis M.

Aventis Pharma Deutschland GmbH, DG Thrombosis and Degenerative Joint Diseases, Industriepark Hoechst, D-65929 Frankfurt, Germany.

Proteinase-activated receptor 2 (PAR-2) is expressed on many nociceptive neurons. Application of PAR-2 agonists has been shown to induce behavioral signs of hyperalgesia. We investigated effects of the rat PAR-2 agonist SLIGRL-NH2 in the isolated rat skin-saphenous nerve preparation. SLIGRL-NH2 (100 microM) excited 20% of all C-fiber nociceptors tested. In addition, C-fiber nociceptors were sensitized to heat after SLIGRL-NH2 application resulting in an increase in response magnitude and a decrease of heat threshold. The PAR-2-inactive control peptide LRGILS-NH2 had no effect. The mechanical sensitivity of C-fibers was not affected by SLIGRL-NH2. PAR-2-mediated excitation and sensitization of primary nociceptors may contribute to PAR-2-mediated hyperalgesia.
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