Naslov
Inhibition of human serum butyrylcholinesterase phenotypes by ethopropazine

Autori
Simeon-Rudolf, Vera ; Šinko, Goran ; Reiner, Elsa

Vrsta, podvrsta i kategorija rada
Sažeci sa skupova, sažetak, znanstveni

Izvornik
Life Sciences Conference 1999, Gozd Martuljek, Slovenija / - Ljubljana : Slovensko farmacevtsko društvo, 1999

Skup
Life Sciences Conference 1999

Mjesto i datum
Gozd Martuljek, Slovenija, 18.09.1999. - 22.09.1999

Vrsta sudjelovanja
Poster

Vrsta recenzije
Međunarodna recenzija

Ključne riječi
ethopropazin; acethylcholinesterase; butyrylcholinesterase; phenotypes

Sažetak
Ethopropazine is a selective inhibitor (to a high degree a specific inhibitor) of butyrylcholinesterase (BChE ; EC 3.1.1.8) and is used to differentiate BChE from acetylcholinesterase (AChE ; EC 3.1.1.7) in whole blood or other tissues where both AChE and BChE are present. Ethopropazine, having a quaternary nitrogen, is expected to be a better inhibitor of the usual human serum BChE than the atypical enzyme or its heterozygotes. We have measured the activity of human sera with 0.5 and 1.0 mM acetylthiocholine as substrate in the presence and in the absence of 20 uM ethopropazine in 0.1 M phosphate buffer, pH=7.4 at 37 oC with the DTNB reagent (Ellman et al. 1961). The sera were from individuals who had different BChE homozygous and heterozygous phenotypes of usual (U), atypical (A), fluoride-resistant (F), Kalow (K), J, or silent (S) variants. Three to five sera of each BChE phenotype were tested. In our experimental conditions, the activities of UU, UA, FF/FS, AF, AJ/AK, AA/AS sera were inhibited 98, 94, 92, 87, 85 and 74%, respectively. The contribution of partially uninhibited BChE activity might affect the estimate of AChE activity in whole blood or other tissues. Furthermore, the AChE activity of human erythrocytes is 8% inhibited by 20 uM ethopropazine which should also be taken into account when applying ethopropazine for the differentiation of AChE and BChE activities in whole blood.

Izvorni jezik
Engleski

Znanstvena područja
Kliničke medicinske znanosti

POVEZANOST RADA