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Published on: May 16, 2019
Anticonvulsant effects of carbenoxolone in genetically epilepsy prone rats (GEPRs)
Pietro Gareri1, Daniele Condorelli, Natale Belluardo
1Section of Pharmacology, Department of Experimental and Clinical Medicine, Faculty of Medicine and Surgery, University of Catanzaro, 88100 Catanzaro, Italy.
Abstract:
Carbenoxolone (CBX), the succinyl ester of glycyrrhetinic acid, is an inhibitor of gap junctional intercellular communication. Systemic administration of CBX was able to decrease the seizure severity score and to increase the latency time of seizure onset in genetically epilepsy prone rats (GEPRs). In particular, intravenous or intraperitoneal administration of carbenoxolone (5-30 mg/kg) produced a dose-dependent and significant reduction in the clonic and tonic phases of the audiogenic seizures in GEPRs. The anticonvulsant doses were not associated with an impairment of motor coordination. The bilateral microinjection of CBX (0.001-0.50 microg/0.5 microl) into the inferior colliculi, the substantia nigra (pars reticulata or compacta) and the inferior olivary complex was able to reduce the seizure severity score in a dose-dependent manner. The anticonvulsant effects were longer lasting after focal microinjection than after systemic administration. No anticonvulsant effects were observed following focal bilateral microinjections of glycyrrhizin into the same brain areas where CBX was shown to be effective.
Insights
Carbenoxolone (CBX) reduces seizure severity and increases seizure onset latency in epilepsy-prone rats. This gap junction inhibitor shows anticonvulsant effects without impairing motor coordination.
Area of Science:
- Neuroscience
- Pharmacology
- Epilepsy Research
Background:
- Carbenoxolone (CBX) is a glycyrrhetinic acid derivative that inhibits gap junctional intercellular communication.
- Epilepsy is a neurological disorder characterized by recurrent seizures.
Purpose of the Study:
- To investigate the anticonvulsant effects of carbenoxolone in a rat model of epilepsy.
- To determine the efficacy of systemic and focal administration of CBX on audiogenic seizures.
Main Methods:
- Systemic administration (intravenous, intraperitoneal) and bilateral microinjections of CBX into specific brain regions (inferior colliculi, substantia nigra, inferior olivary complex) in genetically epilepsy-prone rats (GEPRs).
- Assessment of seizure severity score, seizure onset latency, and motor coordination.
- Comparison with glycyrrhizin administration.
Main Results:
- Systemic CBX administration dose-dependently reduced seizure severity and prolonged seizure onset latency in GEPRs.
- Focal microinjections of CBX into the inferior colliculi, substantia nigra, and inferior olivary complex also reduced seizure severity in a dose-dependent manner.
- Anticonvulsant effects were longer-lasting with focal administration; no motor coordination impairment was observed at effective doses. Glycyrrhizin showed no anticonvulsant effects.
Conclusions:
- Carbenoxolone exhibits significant anticonvulsant properties in a genetic epilepsy rat model.
- Both systemic and focal administration of CBX are effective in reducing seizure severity, with focal delivery offering prolonged effects.
- CBX represents a potential therapeutic agent for epilepsy, targeting gap junction communication.
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