Anticonvulsant, sedative and muscle relaxant effects of carbenoxolone in mice

Background: Carbenoxolone, as an antiulcer medicine, has some pharmacological properties such as: the inhibition of gap junctional (GJ) intercellular communication. In vitro studies have shown, carbenoxolone to abolish the generation of full or partial ectopic spike generation, by 4-aminopyridine, as well as spontaneous epileptiform activity in CA3 or CA1 regions of the rat hippocampal slices via closing GJ channels. Thus, we considered the possible anticonvulsant effects of carbenoxolone in animal seizure models.

Results: ED50 values of diazepam and carbenoxolone in the pentylenetetrazole model were 1.13 mg/kg and 283.3 mg/kg, respectively. In this model, carbenoxolone in doses of 200 and 300 mg/kg prolonged the onset time of seizure and decreased the duration of seizures. In the maximal electroshock model, carbenoxolone in a dose of 400 mg/kg decreased the duration of seizure producing protection against seizure but failing to protect against mortality in comparison with diazepam. In the potentiation of pentobarbitone sleep test, carbenoxolone significantly increased sleeping time and decreased latency in doses of 100, 200 and 300 mg/kg in mice dose dependently. In the traction test, carbenoxolone (400 mg/kg) showed muscle relaxant activity and in the accelerated rotarod test, carbenoxolone in doses of 200 and 300 mg/kg showed a decline in motor coordination.

Conclusion: It can be concluded that carbenoxolone possesses anticonvulsant, muscle relaxant and hypnotic effects, which could contribute to the control of petit mal and grand mal seizures.