hrcak mascot   Srce   HID

Izvorni znanstveni članak

Inhibition of Human Blood Acetylcholinesterase and Butyrylcholinesterase by Ethopropazine

Vera Simeon-Rudolf ; Institute for Medical Research and Occupational Health, Ksaverska cesta 2, 10000 Zagreb, Croatia
Goran Šinko ; Institute for Medical Research and Occupational Health, Ksaverska cesta 2, 10000 Zagreb, Croatia
Anita Štuglin ; Institute for Medical Research and Occupational Health, Ksaverska cesta 2, 10000 Zagreb, Croatia
Elsa Reiner ; Institute for Medical Research and Occupational Health, Ksaverska cesta 2, 10000 Zagreb, Croatia

Puni tekst: engleski, pdf (81 KB) str. 173-182 preuzimanja: 214* citiraj
APA 6th Edition
Simeon-Rudolf, V., Šinko, G., Štuglin, A. i Reiner, E. (2001). Inhibition of Human Blood Acetylcholinesterase and Butyrylcholinesterase by Ethopropazine. Croatica Chemica Acta, 74 (1), 173-182. Preuzeto s https://hrcak.srce.hr/131786
MLA 8th Edition
Simeon-Rudolf, Vera, et al. "Inhibition of Human Blood Acetylcholinesterase and Butyrylcholinesterase by Ethopropazine." Croatica Chemica Acta, vol. 74, br. 1, 2001, str. 173-182. https://hrcak.srce.hr/131786. Citirano 06.03.2021.
Chicago 17th Edition
Simeon-Rudolf, Vera, Goran Šinko, Anita Štuglin i Elsa Reiner. "Inhibition of Human Blood Acetylcholinesterase and Butyrylcholinesterase by Ethopropazine." Croatica Chemica Acta 74, br. 1 (2001): 173-182. https://hrcak.srce.hr/131786
Harvard
Simeon-Rudolf, V., et al. (2001). 'Inhibition of Human Blood Acetylcholinesterase and Butyrylcholinesterase by Ethopropazine', Croatica Chemica Acta, 74(1), str. 173-182. Preuzeto s: https://hrcak.srce.hr/131786 (Datum pristupa: 06.03.2021.)
Vancouver
Simeon-Rudolf V, Šinko G, Štuglin A, Reiner E. Inhibition of Human Blood Acetylcholinesterase and Butyrylcholinesterase by Ethopropazine. Croatica Chemica Acta [Internet]. 2001 [pristupljeno 06.03.2021.];74(1):173-182. Dostupno na: https://hrcak.srce.hr/131786
IEEE
V. Simeon-Rudolf, G. Šinko, A. Štuglin i E. Reiner, "Inhibition of Human Blood Acetylcholinesterase and Butyrylcholinesterase by Ethopropazine", Croatica Chemica Acta, vol.74, br. 1, str. 173-182, 2001. [Online]. Dostupno na: https://hrcak.srce.hr/131786. [Citirano: 06.03.2021.]

Sažetak
Inhibition of human erythrocyte acetylcholinesterase (AChE; EC 3.1.1.7) and serum butyrylcholinesterase (BChE; EC 3.1.1.8) by ethopropazine, 10-(2-diethylaminopropyl)phenothiazine hydrochloride, was measured with acetylthiocholine (ATCh) as substrate. Dissociation constants for the enzyme-inhibitor complexes were calculated from the effect of ATCh concentration on the apparent dissociation constants by applying non-linear regression to fit the model to experimental data. Inhibition of AChE revealed a competitive inhibition for two binding sites (Ka = 161 and Ki = 393 μmol dm-3), inhibition of the atypical BChE was non-competitive (Ki = 7.5 μmol dm-3) while that of the usual BChE was competitive (K(I) = 0.16 μmol dm-3). At the ethopropazine concentration of 20 μmol dm-3 and the acetyl-thiocholine concentration of 1.0 mmol dm-3 (conditions used for differentiation between AChE and BChE activities), the erythrocyte AChE was 8% inhibited and the BChE phenotypes UU, UA, FF/FS, AF, AJ/AK and AA/AS between 98% and 74%.

Ključne riječi
acetylcholinesterase; butyrylcholinesterase; ethopropazine; selective inhibition; inhibition mechanism; enzyme-inhibitor; enzyme-substrate dissociation constants

Hrčak ID: 131786

URI
https://hrcak.srce.hr/131786

Posjeta: 383 *