Organophosphorus poisoning caused by some pesticides and nerve agents is a life-threating condition that must be swiftly addressed to avoid casualties. Despite the availability of medical countermeasures, clinically available compounds lack broad spectrum, are not effective towards all organophosphorus toxins, have poor pharmacokinetics properties allow them crossing blood-brain barrier, hamper...

organophosphate (op) poisoning is one of the most common causes of poisoning in developing countries especially in southeastern asia. poisoning with phosphorus-containing organic chemicals or op compounds can be managed with antidotes like oximes which are potential reactivators of acetylcholinesterase (ache). the efficacy of oxime therapy in op poisoned patients mainly depends upon various fac...

Introduction. Despite large experience in the use of basic therapies for acute poisoning by organophosphorus compounds (OPs)of anticholinesterase action and results research conducted world, current methods treatment such poisonings are insufficient do not meet requirements effective health. Purpose. Based on analysis scientific publications to outline main directions modern developments drugs ...

The potency of the Czech original pharmacological pretreatment consisting of pyridostigmine, benactyzine and trihexyphenidyle, designated PANPAL, to increase the resistance of rats and mice against tabun or soman and to increase the therapeutic efficacy of standard antidotal treatment of tabun or soman-poisoned experimental animals was studied and compared with commonly used pyridostigmine alon...

Four nonvolatile nerve agent surrogates, 4-nitrophenyl ethyl dimethylphosphoramidate (NEDPA, a tabun surrogate), 4-nitrophenyl ethyl methylphosphonate (NEMP, a VX surrogate), and two sarin surrogates, phthalimidyl isopropyl methylphosphonate (PIMP) and 4-nitrophenyl isopropyl methylphosphonate (NIMP), were synthesized and tested as acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) i...

A highly toxic nerve agent, tabun, can inhibit acetylcholinesterase (AChE) at cholinergic sites, which leads to serious cardiovascular complications, respiratory compromise and death. We have examined the structural features of the tabun-conjugated AChE complex with an oxime reactivator, Ortho-7, to provide a strategy for designing new and efficient reactivators. Mutation of mAChE within the ch...

Acetylcholinesterase (AChE) is an essential enzyme that terminates cholinergic transmission by rapid hydrolysis of the neurotransmitter acetylcholine. Compounds inhibiting this enzyme can be used (inter alia) to treat cholinergic deficiencies (e.g. in Alzheimer's disease), but may also act as dangerous toxins (e.g. nerve agents such as sarin). Treatment of nerve agent poisoning involves use of ...

BACKGROUND Pharmaceuticals with targets in the cholinergic transmission have been used for decades and are still fundamental treatments in many diseases and conditions today. Both the transmission and the effects of the somatomotoric and the parasympathetic nervous systems may be targeted by such treatments. Irrespective of the knowledge that the effects of neuronal signalling in the nervous sy...

Reactivation of organophosphate (OP)-inhibited acetylcholinesterase (AChE) by oximes is the primary reason for their effectiveness in the treatment of OP poisoning. Reactivation is reported to accelerate by quaternary ligands such as decamethonium, which is devoid of nucleophilicity. The mechanism of this enhancement is not known. To better understand the acceleration phenomenon, we examined li...