Acute Administration of Desformylflustrabromine Relieves Chemically Induced Pain in CD-1 Mice

• Published in: Molecules (Basel, Switzerland) Switzerland), 2019-03, Vol.24 (5), p.944
• Main Authors: Weggel, Loni A, Pandya, Anshul A
• Format: Article
• Language: English
• Subjects: Acetic acid; Acetic Acid - adverse effects; Acetylcholine receptors (nicotinic); Agonists; Allosteric properties; Allosteric Regulation; Analgesics; Analgesics - administration & dosage; Analgesics - chemistry; Analgesics - pharmacology; Animals; Anxiety; Cell membranes; Central nervous system; desformylflustrabromine (dFBr); Dopamine; Drug dosages; Formaldehyde - adverse effects; Hydrocarbons, Brominated - administration & dosage; Hydrocarbons, Brominated - chemistry; Hydrocarbons, Brominated - pharmacology; Indole Alkaloids - administration & dosage; Indole Alkaloids - chemistry; Indole Alkaloids - pharmacology; Ion channels; Male; Mice; Molecular Structure; Narcotics; Neuromodulation; Nicotine; nicotinic acetylcholine receptors (nAChRs); Pain; Pain - chemically induced; Pain - drug therapy; Pain perception; positive allosteric modulators (PAMs); Receptors, Nicotinic - metabolism; Spinal cord
• ISSN: 1420-3049; 1420-3049
• DOI: 10.3390/molecules24050944

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.