Abstract
The efficacy of some aminoadamantane derivatives used as neurodegeneration treatments is due to their ability to block NMDA receptors. But this mechanism of pharmacological action can also produce analgesic activity. Analgesic properties of two aminoadamantanes, amantadine (20 mg/kg) and hemantane (20 mg/kg), which were uncompetitive NMDA receptor antagonists, were assessed in rodent models of pain induced by different pain stimuli (tail-flick test, acetic twitches test in mice and formalin test in rats). Additionally, the anti-inflammatory properties of hemantane and amantadine were evaluated in mice with acetic peritonitis and in rats with hind paw edema induced by formalin injection. The results of our study demonstrate that the analgesic activity of the 1-aminoadamantane amantadine differs from the 2-aminoadamantane hemantane. The analgesic activity of amantadine administered intraperitoneally was more pronounced in the case of acute thermal pain in mice compared to hemantane, and only amantadine had a significant analgesic effect on the acute early phase of formalin pain in rats induced by the effect of the algogen on the primary sensory afferents. Hemantane was more effective than amantadine for relieving pain produced by inflammation owing to its pronounced anti-inflammatory activity: only hemantane decreased the amount of acetic twitches in mice that received drugs orally and was effective in the tonic phase of formalin pain in rats.
Highlights
Some derivatives of aminoadamantane are known as efficient treatments for neurodegenerative diseases [1]
Mice were used in the tail-flick test and the acetic twitches test; the formalin test was done in rats
Our results demonstrate that the analgesic activity of amantadine (20 mg/kg), a derivative of 1aminoadamantane, differs from the effect of hemantane (20 mg/kg), a 2-aminoadamantane derivative
Summary
Some derivatives of aminoadamantane are known as efficient treatments for neurodegenerative diseases [1]. Amantadine, a derivative of 1-aminoadamantane, is useful as an antiparkinsonian and antidyskinetic drug [2]-[4]. Benefits of therapy with memantine, another 1-aminoadamantane, are confirmed in clinical trials investigating the treatment of Alzheimer’s disease [5] [6], vascular dementia [7], and Parkinson’s disease [8]. A derivative of 2-aminoadamantane, is a new antiparkinsonian and antidyskinetic agent [9] [10] and currently undergoing clinical trials in the Russian Federation. The aminoadamantane derivatives act by blocking NMDA receptors [11]-[13]. In addition to the neuroprotective effect, the blocking of NMDA receptors could produce analgesic activity [14]. Activation of NMDAtype ionotropic glutamate receptors is required for long-term potentiation of nociceptive neurons [15]-[17] and plays a major role in the amplification of a nociceptive input in post-inflammatory conditions [18]
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