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Local anesthetics are widely utilized in dentistry, cosmetology, and medicine. Local anesthesia is essential to providing a pain-free experience during dental and local surgeries as well as cosmetic procedures. However, the injection itself may produce discomfort and be a source of aversion. A novel approach toward the taste modulation of local anesthetics is proposed, in which the anesthetics of the "-caine" family serve as cations and are coupled with anionic sweeteners such as saccharinate and acesulfamate. Ionic conjugates of vasoconstrictor epinephrine such as epinephrine saccharinate and epinephrine acesulfamate have also been synthesized. Novel ionic conjugates were developed using anion exchange techniques. Reported compounds are sweet-tasting and are safe to use both topically and as injections.


John K Neubert, Alexander A Oliferenko, Polina V Oliferenko, Sergey V Emets, David A Ostrov, Gary I Altschuler, Joe Calkins, Jay Wickersham, Robert Hromas, Iryna O Lebedyeva. Sweet-Tasting Ionic Conjugates of Local Anesthetics and Vasoconstrictors. Molecules (Basel, Switzerland). 2021 Feb 12;26(4)

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PMID: 33673320

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