Antihyperalgesic activity of a novel synthesized analogue of lidocaine in diabetic rats

J Pharm Pharmacol. 2013 May;65(5):689-96. doi: 10.1111/jphp.12025. Epub 2013 Jan 31.

Abstract

Objectives: The purpose of this study was to assess the antinociceptive and antihyperalgesic effects of a lidocaine analogue N-(2,6-dichlorophenyl)-2-(4-methyl-1-piperidinyl)acetamide (LIA).

Methods: The structure of LIA was established by elemental analysis and compatible IR, (1) H NMR, (13) C NMR, and spectral data. Nociceptive and hyperalgesic activity were evaluated in normoglycaemic and streptozocin-induced diabetic rats using the formalin test. Formalin-evoked flinching, an indication of nociception and hyperalgesia, was increased in diabetic rats (using 0.5% formalin) compared with nondiabetic rats (using 1% formalin).

Key findings: Local administration of LIA into the dorsal surface of the right hind paw (0.18-5.6 mg per paw) significantly reduced the formalin-induced nociceptive and hyperalgesic behaviour of nondiabetic and diabetic rat. The antinociceptive effect of LIA was higher than that of lidocaine injection, furthermore this effect was higher than that of gabapentin.

Conclusions: LIA may have potential as a treatment for diabetic hyperalgesia. Further investigations of the antinociceptive mechanisms and the safety of this new compound are necessary.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amines / pharmacology
  • Amines / therapeutic use
  • Analgesics / chemistry
  • Analgesics / pharmacology
  • Analgesics / therapeutic use*
  • Animals
  • Behavior, Animal / drug effects
  • Cyclohexanecarboxylic Acids / pharmacology
  • Cyclohexanecarboxylic Acids / therapeutic use
  • Diabetes Complications / drug therapy*
  • Diabetes Mellitus, Experimental / complications
  • Diabetes Mellitus, Experimental / drug therapy*
  • Formaldehyde
  • Gabapentin
  • Hyperalgesia / chemically induced
  • Hyperalgesia / drug therapy*
  • Lidocaine / analogs & derivatives
  • Lidocaine / chemistry
  • Lidocaine / pharmacology
  • Lidocaine / therapeutic use*
  • Molecular Structure
  • Nociceptive Pain / chemically induced
  • Nociceptive Pain / drug therapy
  • Pain / chemically induced
  • Pain / drug therapy*
  • Pain Measurement
  • Rats
  • Reference Values
  • gamma-Aminobutyric Acid / pharmacology
  • gamma-Aminobutyric Acid / therapeutic use

Substances

  • Amines
  • Analgesics
  • Cyclohexanecarboxylic Acids
  • Formaldehyde
  • gamma-Aminobutyric Acid
  • Gabapentin
  • Lidocaine