Pub. Date : 2013 Mar 25
PMID : 23123249
6 Functional Relationships(s)Download |
Sentence | Compound Name | Protein Name | Organism |
1 | Testing of novel brain-penetrating oxime reactivators of acetylcholinesterase inhibited by nerve agent surrogates. | Oximes | acetylcholinesterase | Rattus norvegicus |
2 | A critical need for combating the effects of organophosphate (OP) anticholinesterases, such as nerve agents, is the current lack of an effective oxime reactivator which can penetrate the blood-brain barrier (BBB), and therefore reactivate inhibited acetylcholinesterase (AChE) in the brain. | Oximes | acetylcholinesterase | Rattus norvegicus |
3 | A critical need for combating the effects of organophosphate (OP) anticholinesterases, such as nerve agents, is the current lack of an effective oxime reactivator which can penetrate the blood-brain barrier (BBB), and therefore reactivate inhibited acetylcholinesterase (AChE) in the brain. | Oximes | acetylcholinesterase | Rattus norvegicus |
4 | The oximes demonstrated a range of 14-76% reactivation of rat brain AChE in vitro. | Oximes | acetylcholinesterase | Rattus norvegicus |
5 | An in vivo testing paradigm was developed in which the novel oxime was administered at the time of maximal brain AChE inhibition (about 80%) (1h) elicited by nitrophenyl isopropyl methylphosphonate (NIMP; sarin surrogate). | Oximes | acetylcholinesterase | Rattus norvegicus |
6 | This paradigm, with delayed administration of oxime to a time when brain AChE was starting to recover, was designed to minimize reactivation/reinhibition of peripheral AChE during the reactivation period which would decrease the availability of the surrogate for entry into the brain; this paradigm will allow proof of concept of BBB penetrability. | Oximes | acetylcholinesterase | Rattus norvegicus |