Abstract
Neuronal nicotinic acetylcholine receptors are cell membrane-bound ion channels that are widely distributed in the central nervous system. The α4β2 subtype of neuronal nicotinic acetylcholine receptor plays an important role in modulating the signaling pathways for pain. Previous studies have shown that agonists, partial agonists, and positive allosteric modulators for the α4β2 receptors are effective in relieving pain. Desformylflustrabromine is a compound that acts as an allosteric modulator of α4β2 receptors. The aim of this study was to assess the effects of desformylflustrabromine on chemically induced pain. For this purpose, the formalin-induced pain test and the acetic acid-induced writhing response test were carried out in CD-1 mice. Both tests represent chemical assays for nociception. The results show that desformylflustrabromine is effective in producing an analgesic effect in both tests used for assessing nociception. These results suggest that desformylflustrabromine has the potential to become a clinically used drug for pain relief.
Highlights
Pain is an unpleasant sensation that can influence the physical as well as the mental wellbeing of an individual [1,2]
Non-steroidal anti-inflammatory drugs (NSAIDs) and opioid analgesics are the main stay for pain relief in clinical settings; both drug classes have some drawbacks associated with their use [3,4]
While the chronic use of non-steroidal anti-inflammatory drugs (NSAIDs) increases the likelihood of injury to the gastrointestinal tract mucosa, opioid analgesics have a very high addictive liability [5,6]
Summary
Pain is an unpleasant sensation that can influence the physical as well as the mental wellbeing of an individual [1,2]. Non-steroidal anti-inflammatory drugs (NSAIDs) and opioid analgesics are the main stay for pain relief in clinical settings; both drug classes have some drawbacks associated with their use [3,4]. Newer pharmacological agents with increased analgesic efficacy and relatively fewer side effects are needed for pain relief. One potential target for developing clinically useful drugs for pain relief are the nicotinic acetylcholine receptors (nAChRs) [7,8]. The α4β2 subtype of nAChRs are located in the brain and the spinal cord where they are involved in modulating neuropathic and inflammatory pain [9]. Α4β2 receptors are widely distributed in regions that are associated with the descending monoaminergic inhibitory pain pathway [10]
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