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Antinociceptive activities of lidocaine and the nav1.8 blocker a803467 in diabetic rats.
J Am Assoc Lab Anim Sci. 2012; 51(5):579-85.JA

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+Show Affiliations

Department of Biophysics, School of Medicine, Kahramanmaras Sutcu Imam University, Kahramanmaras, Turkey. tufanmert@yahoo.comNo affiliation info available

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

23312086

Citation

Mert, Tufan, and Yasemin Gunes. "Antinociceptive Activities of Lidocaine and the Nav1.8 Blocker A803467 in Diabetic Rats." Journal of the American Association for Laboratory Animal Science : JAALAS, vol. 51, no. 5, 2012, pp. 579-85.
Mert T, Gunes Y. Antinociceptive activities of lidocaine and the nav1.8 blocker a803467 in diabetic rats. J Am Assoc Lab Anim Sci. 2012;51(5):579-85.
Mert, T., & Gunes, Y. (2012). Antinociceptive activities of lidocaine and the nav1.8 blocker a803467 in diabetic rats. Journal of the American Association for Laboratory Animal Science : JAALAS, 51(5), 579-85.
Mert T, Gunes Y. Antinociceptive Activities of Lidocaine and the Nav1.8 Blocker A803467 in Diabetic Rats. J Am Assoc Lab Anim Sci. 2012;51(5):579-85. PubMed PMID: 23312086.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Antinociceptive activities of lidocaine and the nav1.8 blocker a803467 in diabetic rats. AU - Mert,Tufan, AU - Gunes,Yasemin, PY - 2013/1/15/entrez PY - 2013/1/15/pubmed PY - 2013/11/14/medline SP - 579 EP - 85 JF - Journal of the American Association for Laboratory Animal Science : JAALAS JO - J Am Assoc Lab Anim Sci VL - 51 IS - 5 N2 - 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. SN - 1559-6109 UR - https://www.unboundmedicine.com/medline/citation/23312086/Antinociceptive_activities_of_lidocaine_and_the_nav1_8_blocker_a803467_in_diabetic_rats_ L2 - https://www.ingentaconnect.com/openurl?genre=article&issn=1559-6109&volume=51&issue=5&spage=579&aulast=Mert DB - PRIME DP - Unbound Medicine ER -