Antihistaminic activity of lidocaine derivatives in the isolated guinea pig ileum

Local anesthetics (LAs) are drugs that inhibit membrane depolarization by reducing sodium conductance. In addition to the most prominent and well-defined function of LAs described above, numerous studies have shown that LAs possess many other properties, such as anti-inflammatory, anti-arrhythmic or analgesic activities. Furthermore, LAs are structurally similar to histamine H-receptor antagonists. Thus, LAs can be considered antihistaminic drugs. The aim of the present study was to determine and compare the antihistaminic effects of lidocaine derivatives - JCB-1, JCB-2 and JCB-3 - on the isolated guinea pig ileum. Only JCB-1 and JCB-2 at the highest concentration (10 4M) showed the antihistaminic effect. The studied compounds showed a dose-dependent effect. Interestingly, lower concentrations of the studied compounds (10 8M and 10"I0M) caused the opposite effect - increased the contraction of the ileum induced by histamine. These effects necessitate further studies. Nevertheless, this is the first time that JCB compounds have been demonstrated to possess antihistaminic properties.

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