Effects of 4-amino-2-methyl-cantharidinimide on GABAC receptors

doi:10.5246/jcps.2012.03.032

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Effects of 4-amino-2-methyl-cantharidinimide on GABAC receptors

Yan-Xin Zhang, Yu-Fang Liao, Ming-Zheng Wang^*, Yan-Ting Gu, Yi Xiao, Xin-Feng Wang

Department of Pharmacology, Shanxi Medical University, Taiyuan 030001, China

Received:2011-12-27 Revised:2012-03-10 Online:2012-05-15 Published:2012-05-15
Contact: Ming-Zheng Wang*

Abstract

Abstract:

The antiepileptic effect of 4-amino-2-methyl-cantharidinimide (AMC) was reported, but its mechanism remains unknown. In this study, we investigated the effects of AMC on a rat model of penicillin-induced epilepsy. The doses of 88 and 22 mg/kg AMC and the dose of 154 mg/kg sodium valproate (VPA) were administered intragastrically (i.g.) 30 min before penicillin injection, respectively. The epileptiform activity was verified by electrocorticographic (ECoG) recordings. The levels of GABA and GABAC receptors in hippocampus were determined by immunohistochemistry, and real-time polymerase chain reaction (RT-PCR) technique was used to detect the mRNA expression of GABAC receptor ρ2. The mean frequency and amplification of spike epileptiform activity were significantly decreased in AMC and VPA-pretreated rats compared with those of non-pretreated penicillin-induced epilepsy (PIE) group. The levels of GABA, GABAC receptors and the mRNA expression of GABAC receptors ρ2 in AMC and VPA-pretreated rats were significantly increased as compared with PIE group. These findings indicate that AMC and VPA have an antiepileptic effect on PIE in rats, and the antiepileptic effect of AMC may be mediated by the GABAC receptors and GABA.

Key words: 4-Amino-2-methyl-cantharidinimide, Antiepileptic effect, GABAC receptors, Immunohistochemistry, RT-PCR

CLC Number:

R962.2

Supporting:

Yan-Xin Zhang, Yu-Fang Liao, Ming-Zheng Wang^*, Yan-Ting Gu, Yi Xiao, Xin-Feng Wang . Effects of 4-amino-2-methyl-cantharidinimide on GABAC receptors [J]. , DOI: 10.5246/jcps.2012.03.032.

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Effects of 4-amino-2-methyl-cantharidinimide on GABAC receptors

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