| Title : 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) - Patocka_2005_Acta.Medica.(Hradec.Kralove)_48_145 |
| Author(s) : Patocka J , Jun D , Kuca K |
| Ref : Acta Medica (Hradec Kralove) , 48 :145 , 2005 |
| Abstract : 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 time- and 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. |
| ESTHER : Patocka_2005_Acta.Medica.(Hradec.Kralove)_48_145 |
| PubMedSearch : Patocka_2005_Acta.Medica.(Hradec.Kralove)_48_145 |
| PubMedID: 16640027 |
Patocka J, Jun D, Kuca K (2005)
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)
Acta Medica (Hradec Kralove)
48 :145
Patocka J, Jun D, Kuca K (2005)
Acta Medica (Hradec Kralove)
48 :145