Tapentadol, but not morphine, selectively inhibits disease-related thermal hyperalgesia in a mouse model of diabetic neuropathic pain

Thomas Christoph, Jean De Vry, Thomas M Tzschentke
Neuroscience Letters 2010 February 12, 470 (2): 91-4
Neuropathic pain in diabetic patients is a common distressing symptom and remains a challenge for analgesic treatment. Selective inhibition of pathological pain sensation without modification of normal sensory function is a primary aim of analgesic treatment in chronic neuropathic pain. Tapentadol is a novel analgesic with two modes of action, mu-opioid receptor (MOR) agonism and noradrenaline (NA) reuptake inhibition. Mice were rendered diabetic by means of streptozotocin, and neuropathic hyperalgesia was assessed in a 50 degrees C hot plate test. Normal nociception was determined in control mice. Tapentadol (0.1-1mg/kg i.v.) and morphine (0.1-3.16 mg/kg i.v.) dose-dependently attenuated heat-induced nociception in diabetic animals with full efficacy, reaching >80% at the highest doses tested. Tapentadol was more potent than morphine against heat hyperalgesia, with ED(50) (minimal effective dose) values of 0.32 (0.316) and 0.65 (1)mg/kg, respectively. Non-diabetic controls did not show significant anti-nociception with tapentadol up to the highest dose tested (1mg/kg). In contrast, 3.16 mg/kg morphine, the dose that resulted in full anti-hyperalgesic efficacy under diabetic conditions, produced significant anti-nociception in non-diabetic controls. Selective inhibition of disease-related hyperalgesia by tapentadol suggests a possible advantage in the treatment of chronic neuropathic pain when compared with classical opioids, such as morphine. It is hypothesized that this superior efficacy profile of tapentadol is due to simultaneous activation of MOR and inhibition of NA reuptake.

Full Text Links

Find Full Text Links for this Article


You are not logged in. Sign Up or Log In to join the discussion.

Related Papers

Remove bar
Read by QxMD icon Read

Save your favorite articles in one place with a free QxMD account.


Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"