In vitro Inactivation of Rat Brain Acetylcholinesterase by DSP-4 and Its Derivatives OS-21 and OS-23 and Protective Activity of Tacrine (9-Amino-1,2,3,4-tetrahydroacridine)
| Autor: | Jiří Patočka, Daniel Jun, Kamil Kuča |
|---|---|
| Jazyk: | angličtina |
| Rok vydání: | 2005 |
| Předmět: | |
| Zdroj: | Acta Medica, Vol 48, Iss 3, Pp 145-148 (2005) |
| Druh dokumentu: | article |
| ISSN: | 18059694 1211-4286 1805-9694 |
| DOI: | 10.14712/18059694.2018.42 |
| Popis: | Tertiary N-haloethylamines are able to cyclize to the corresponding aziridinium ions. The inhibitory activity of the DSP-4 (N-(o-brombenzyl)-N-ethyl-2-chlorethylamine) and its two derivatives OS-21 (N-benzyl-N-ethyl-2-chloroethylamine) and OS-23 (N-fenylethyl-N-ethyl-2-chloroethylamine) was studied toward rat brain acetylcholinesterase (AChE) in vitro. The influence of the THA (tacrine; 9–amino-1,2,3,4–tetrahydroacridine) on AChE inhibition by these substances was also evaluated. The results demonstrated that all of three aziridinium compounds formed in solution caused a timeand concentration-dependent irreversible enzyme inhibition. The association of aziridinium compounds with the AChE was a relatively slow second-order reaction. DSP-4 showed the fastest rate of AChE alkylation, OS-21 had a lowered rate and OS-23 displayed the lowest rate. Pretreatment of the enzyme by THA decreased the rate of alkylation by all three aziridinium compounds by allosteric mechanism. |
| Databáze: | Directory of Open Access Journals |
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