The inhibition, reactivation and mechanism of VX-, sarin-, fluoro-VX and fluoro-sarin surrogates following their interaction with HuAChE and HuBuChE.

ABSTRACT: In this study, the mechanisms of HuAChE and HuBChE inhibition by Me-P(O) (OPNP) (OR) [PNP = p-nitrophenyl; R = CH₂CH₃, CH₂CH₂F, OCH(CH₃)₂, OCH(CH₃) (CH₂F)] representing surrogates and fluoro-surrogates of VX and sarin were studied by in vitro kinetics and mass spectrometry. The in vitro measures showed that the VX- and fluoro-VX surrogates were relatively strong inhibitors of HuAChE and HuBChE (k_i ∼ 10⁵-10⁶ M^-1min^-1) and underwent spontaneous and 2-PAM-mediated reactivation within 30 min. The sarin surrogates were weaker inhibitors of HuAChE and HuBChE (k_i ∼ 10⁴-10⁵ M^-1min^-1), and in general did

SUBMITTER: Chao CK 

PROVIDER: S-EPMC6061941 | biostudies-literature | 2018 Aug

REPOSITORIES: biostudies-literature