Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: EC:3.1.1.8 (cholinesterase)
 12,691 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Various doses of several bispyridinium compounds (HS-6, HI-6, HGG-12, HGG-42, and SAD-128) known to protect animals against the irreversible cholinesterase inhibitor soman were examined to determine their effects on the cardiovascular and respiratory system of cats. Although the potency varied considerably all of the compounds tested lowered the blood pressure, which appeared to be the result of ganglion blocking properties as determined by their reduction of the pressor response to dimethylphenylpiperazinium and the blockage of the contraction of the preganglionically stimulated cat nictitating membrane. Some of the compounds caused cessation of respiration at much lower doses than others but did so at doses greater than those causing ganglion blockage.
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PMID:Ganglion blocking properties of some bispyridinium soman antagonists. 4 47

Carbamate inhibitors (e.g., pyridostimine bromide) are used as a pre-exposure treatment for the prevention of organophosphorus poisoning. They work by blocking acetylcholinesterase's (AChE) native function and thus protect AChE against irreversible inhibition by organophosphorus compounds. However, carbamate inhibitors are known for many undesirable side-effects related to the carbamylation of AChE. In this Letter, 19 analogues of SAD-128 were prepared and evaluated as cholinesterase inhibitors. The screening results showed promising inhibitory ability of four compounds better to used standards (pralidoxime, obidoxime, BW284c51, ethopropazine, SAD-128). Four most promising compounds were selected for further molecular docking studies. The SAR was stated from obtained data. The former receptor studies were reported and discussed. The further in vivo studies were recommended in the view of OP pre-exposure treatment.
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PMID:Preparation, in vitro screening and molecular modelling of symmetrical 4-tert-butylpyridinium cholinesterase inhibitors--analogues of SAD-128. 2114 49