Nejvíce citovaný článek - PubMed ID 15204744
Protective effect of equine butyrylcholinesterase in inhalation intoxication of rats with sarin: determination of blood and brain cholinesterase activities
- Klíčová slova
- acetylcholinesterase, antidote, nerve agent, organophosphates, prophylaxis, therapy,
- Publikační typ
- časopisecké články MeSH
INTRODUCTION: Organophosphorus nerve agents inhibit the enzyme, acetylcholinesterase (AChE; EC 3.1.1.7). AChE reactivators (also known as oximes) are generally used for the reactivation of an inhibited enzyme. METHODS: Two new AChE reactivators--K033 and K027--were tested for their in vitro reactivation of sarin-inhibited pig-brain AChE. Their reactivation potencies were compared with the commercially available AChE reactivators, pralidoxime, obidoxime, and HI-6. RESULTS: Of the oximes tested, the newly developed oxime K027 achieved the highest reactivation potency (100%; concentration of the oxime -10(-2) M). However, oxime HI-6 (33%) and obidoxime (23%) seem to be the best AChE reactivators for human relevant doses (10(-4) M and lower). CONCLUSION: For human relevant doses, newly developed oximes (K027 and K033) do not surpass the reactivation potency of the most promising oxime, HI-6.
- MeSH
- acetylcholinesterasa metabolismus MeSH
- antidota farmakologie MeSH
- cholinesterasové inhibitory toxicita MeSH
- mozek účinky léků enzymologie MeSH
- obidoxim chlorid farmakologie MeSH
- oximy farmakologie MeSH
- pralidoximové sloučeniny farmakologie MeSH
- prasata MeSH
- pyridinové sloučeniny farmakologie MeSH
- reaktivátory cholinesterasy farmakologie MeSH
- sarin toxicita MeSH
- techniky in vitro MeSH
- výzkumný projekt MeSH
- vztah mezi dávkou a účinkem léčiva MeSH
- zvířata MeSH
- Check Tag
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
- srovnávací studie MeSH
- Názvy látek
- 1-(4-hydroxyiminomethylpyridinium)-3-(carbamoylpyridinium) propane dibromide MeSH Prohlížeč
- 1,4-bis(2-hydroxyiminomethylpyridinium)butane MeSH Prohlížeč
- acetylcholinesterasa MeSH
- antidota MeSH
- asoxime chloride MeSH Prohlížeč
- cholinesterasové inhibitory MeSH
- obidoxim chlorid MeSH
- oximy MeSH
- pralidoxime MeSH Prohlížeč
- pralidoximové sloučeniny MeSH
- pyridinové sloučeniny MeSH
- reaktivátory cholinesterasy MeSH
- sarin MeSH
