生化/生理作用
已被有机磷杀虫剂或神经毒剂灭活的乙酰胆碱酯酶的原型激活剂。现已知没有活化剂可对广谱的有机磷试剂有效。
警示用语:
Warning
危险分类
Acute Tox. 4 Dermal - Acute Tox. 4 Inhalation - Acute Tox. 4 Oral
储存分类代码
11 - Combustible Solids
WGK
WGK 1
个人防护装备
dust mask type N95 (US), Eyeshields, Gloves
F Worek et al.
Archives of toxicology, 72(4), 237-243 (1998-05-20)
The treatment of poisoning by highly toxic organophosphorus compounds (nerve agents) is unsatisfactory. Until now, the efficacy of new potential antidotes has primarily been evaluated in animals. However, the extrapolation of these results to humans is hampered by species differences.
Kamil Musilek et al.
Bioorganic & medicinal chemistry letters, 17(11), 3172-3176 (2007-03-27)
Six novel AChE reactivators with a (Z)-but-2-ene linker were synthesized using the known synthetic pathways. Their ability to reactivate AChE, which had been previously inhibited by nerve agent tabun or pesticide paraoxon, was tested in vitro and compared to pralidoxime
Jyotiranjan Acharya et al.
European journal of medicinal chemistry, 44(3), 1335-1340 (2008-04-09)
A series of novel bis-pyridinium oximes connected by bis-methoxymethyl benzene, 1,4-bis-methoxymethyl (cis)-but-2-ene and 1,4-bis-methoxymethyl but-2-yne linkers were synthesized and their in vitro reactivation efficacy was evaluated against diisopropyl phosphorofluoridate (DFP) inhibited acetylcholinesterase (AChE) and compared with the established antidote 2-PAM
Jarosław Kalisiak et al.
Journal of medicinal chemistry, 55(1), 465-474 (2011-12-31)
A new class of amidine-oxime reactivators of organophosphate (OP)-inhibited cholinesterases (ChE) was synthesized and tested in vitro and in vivo. Compared with 2-PAM, the most promising cyclic amidine-oxime (i.e., 12e) showed comparable or greater reactivation of OP-inactivated AChE and OP-inactivated
Kamil Musilek et al.
Bioorganic & medicinal chemistry, 16(17), 8218-8223 (2008-08-05)
Acetylcholinesterase reactivators are crucial antidotes for the treatment of organophosphate intoxication. Eighteen monoquaternary reactivators of acetylcholinesterase with modified side chain were developed in an effort to extend the properties of pralidoxime. The known reactivators (pralidoxime, HI-6, obidoxime, trimedoxime, methoxime) and
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