Publication:

Screening of novel 2-4 methylphenylimino-3-carboxamide substituted thiophene compound for central analgesic activity

Background Pain is an unpleasant sensation that can range from mild, localized discomfort to agony. The mechanism of pain perception involves dedicated subsets of peripheral and central neurons. For management of pain, currently, available treatment regimens are opioid analgesics and NSAIDs which are easily available over the counter drugs. Long term use of analgesics can lead to significant impact on human renal system, cardiovascular system and analgesic abuse etc. So, there is a need for novel, safe and cost-effective analgesic compound. Hence a study on 2-4 methylphenylimino-3-carboxamide substituted thiophene compound, a novel thiophene compound has been carried out in different experimental animal models.

Methods Two methods were used to evaluate the central analgesic activity of 2-4 methylphenylimino-3-carboxamide substituted thiophene compound. First method was Eddy’s hot plate method and compared to standard central analgesic, morphine. Second method was early phase of formalin induced paw licking in mice and compared to a standard drug, aspirin.

Results With eddy’s hot plate method, 40mg/kg dose of 2-4 methylphenylimino-3-carboxamide substituted thiophene compound has shown maximum pain inhibition percentage (PIP) of 45% at 60 min compared to 125% by morphine. Whereas with early phase of formalin test, 40 mg/kg dose of 2-4 methylphenylimino-3-carboxamide substituted thiophene compound has shown maximum PIP of 44% in early phase compared to 60% by aspirin. The results were statistically significant with p<0.05.

Conclusions It can be concluded that 2-4 methylphenylimino-3-carboxamide substituted thiophene compound found to have minimal central analgesic activity as evident in eddy’s hot plate and early phase of formalin tests.