| Title : Protective effects of m-(tert-butyl) trifluoroacetophenone, a transition state analogue of acetylcholine, against paraoxon toxicity and memory impairments - Zueva_2021_Chem.Biol.Interact_345_109558 |
| Author(s) : Zueva IV , Lenina OA , Kayumova RM , Petrov KA , Masson P |
| Ref : Chemico-Biological Interactions , 345 :109558 , 2021 |
| Abstract : m-(Tert-butyl) trifluoroacetophenone (TFK), a slow-binding inhibitor of acetylcholinesterase (AChE), a transition state analog of acetylcholine, was investigated as a potential neuroprotectant of central and peripheral AChE against organophosphate paraoxon (POX) toxicity. Acute toxicity and pharmacological effects of TFK were investigated on mice and rats. Intraperitoneal administered TFK has low acute toxicity in mice (LD(50) = 19 mg/kg). Effects on motor function as investigated by rotarod and open field tests showed that TFK up to 5 mg/kg did not alter motor coordination and stereotypical exploration behavior of mice. Passive avoidance test showed that 1 or 5 mg/kg TFK restored memory impairment in scopolamine-induced Alzheimer's disease-like dementia in rats. Pretreatment of mice with 5 mg/kg TFK, 2-3 hrs before challenge by 2xLD(50) POX provided a modest and short protection against POX toxicity. Futhermore, analysis of POX-induced neuronal degeneration by using fluoro-jade B staining showed that TFK pretreatment, at the dose 5mg/kg before POX challenge, significantly reduced the density of apoptotic cells in hippocampus and entorhinal cortex of mice. Thus, TFK is capable of reducing POX-induced neurotoxicity. |
| ESTHER : Zueva_2021_Chem.Biol.Interact_345_109558 |
| PubMedSearch : Zueva_2021_Chem.Biol.Interact_345_109558 |
| PubMedID: 34147486 |
Zueva IV, Lenina OA, Kayumova RM, Petrov KA, Masson P (2021)
Protective effects of m-(tert-butyl) trifluoroacetophenone, a transition state analogue of acetylcholine, against paraoxon toxicity and memory impairments
Chemico-Biological Interactions
345 :109558
Zueva IV, Lenina OA, Kayumova RM, Petrov KA, Masson P (2021)
Chemico-Biological Interactions
345 :109558