Neurotoxicity of dipiperidinoethane due to in vivo conversion to a selective cholinesterase inhibitor |
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Authors: | Bruce M. Baron Yoel Kashman Mordechai Sokolovsky |
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Abstract: | Dipiperidinoethane (DPE) administration produces seizures and CNS lesions. Here we elucidate the cholinergic origin of DPE toxicity. DPE is both an acetylcholinesterase (AChE) inhibitor and a muscarinic antagonist. This dual action negates most of the toxic effects of the compound in vivo. The neurotoxicity is believed to arise from oxidative conversion to DPE-N-oxide, which selectively inhibits AChE. Cytotoxicity does not involve muscarinic neurons, since binding parameters were unchanged following in vivo exposure. |
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Keywords: | dipiperidinoethane dipiperidinoethane-N-oxide cholinergic neurotoxin epileptogenic agent pharmacological action |
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