Scientists have created a TAS2R14 receptor agonist that has the potential to help asthma when stimulated. Reported by the American Chemical Society.
Bitter taste buds are found not only in the mouth, but also in other parts of the body, including the respiratory tract. Among 25 different types of bitter taste receptors, the TAS2R14 subtype is one of the most widely distributed in tissues outside the mouth. Activation of these receptors opens passageways in the lungs, thus making it a potential target in the treatment of asthma. However, scientists do not know about its natural agonists – substances that, when interacting with the receptor, cause a biological response by changing its state. Flufenamic acid, a synthetic NSAID, is known to have a similar effect, but its effect is not clear enough.
Now Lucas Waterloo and his colleagues synthesized more effective analogue of this substance. Flufenamic acid was taken as the starting material, then the phenyl ring was replaced by 2-aminopyrimidine and the carboxyl group was replaced by tetrazole during a series of chemical reactions.
As a result, an agonist of this receptor six times more potent than flufenamic acid was synthesized. This means less compound is required to produce a response similar to that of an NSAID. This agonist was also highly selective for TAS2R14 and did not affect other receptors, potentially minimizing side effects.
The new compound will help shed light on the structure, mechanism and physiological function of bitter taste receptors. Additionally, it would potentially allow asthma treatment by acting on these receptors.
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