title: Antinociceptive activities of lidocaine and the nav1.8 blocker a803467 in diabetic rats.
abstract: The streptozocin-induced diabetic rat is a model of chronic pain that shows signs of hyperalgesia and allodynia and may replicate signs in diabetic humans. Here we investigated the antinociceptive effects of A803467, a highly selective blocker of Nav1.8 channels, in diabetic rats with  painful neuropathy. We systemically (intraperitoneal) or locally (intraplantar) administered A803467 (or lidocaine, a nonselective sodium channel blocker, as a control) to diabetic rats with hyperalgesia and allodynia and then measured thermal latencies and mechanical thresholds. With intraperitoneal  administration, A803467 led to 6-fold greater reduction of hyperalgesia and 2-fold greater reduction of allodynia than did lidocaine. Whereas the antihyperalgesic effects of lidocaine and A803467 were similar after intraplantar administration, A803467 (1 mg) was at least 2 times more effective  as an antiallodynic than was lidocaine (0.5 mg). These results suggest that compared with lidocaine, systemic or local blockade of Nav1.8 channels by A803467 may more effectively relieve hyperalgesia and allodynia in diabetic neuropathy.
authors: Department of Biophysics, School of Medicine, Kahramanmaras Sutcu Imam University, Kahramanmaras, Turkey. tufanmert@yahoo.com
authors: Tufan
authors: T
authors: Mert
authors: Yasemin
authors: Y
authors: Gunes
mesh_terms: D000700:Analgesics / Q000627:therapeutic use*; D000814:Aniline Compounds / Q000627:therapeutic use*; D000818:Animals; D003921:Diabetes Mellitus, Experimental / Q000150:complications; D003929:Diabetic Neuropathies / Q000188:drug therapy*; D005260:Female; D005663:Furans / Q000627:therapeutic use*; D006801:Humans; D006930:Hyperalgesia / Q000188:drug therapy* / Q000209:etiology; D008012:Lidocaine / Q000627:therapeutic use*; D062559:NAV1.8 Voltage-Gated Sodium Channel / Q000187:drug effects; D051381:Rats; D017208:Rats, Wistar; D026941:Sodium Channel Blockers / Q000627:therapeutic use*
chemical_list: C520740:A 803467; D000700:Analgesics; D000814:Aniline Compounds; D005663:Furans; D062559:NAV1.8 Voltage-Gated Sodium Channel; D026941:Sodium Channel Blockers; D008012:Lidocaine