Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Pivot Concepts:
Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Target Concepts:
Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Query: EC:3.1.1.8 (
cholinesterase
)
12,691
document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)
These results for the first time document that the brief duration of action of the ganglionic blocker,
Arfonad
(trimethaphan camsylate), is not due to inactivation by plasma
cholinesterase
. Inhibition of the enzyme in vitro by
Arfonad
was not altered by prior incubation of the drug in plasma at 37 degrees C for up to 16 hours nor by treatment with NaOH at 100 degrees C for 10 minutes. Both procedures inactivated succinylcholine. These results in vitro were confirmed in vivo by finding that the toxicity of
Arfonad
in mice was not significantly altered by these procedures whereas they rendered succinylcholine inocuous.
Arfonad
is a noncompetitive whereas succinylcholine is a competitive inhibitor of plasma
cholinesterase
using benzoylcholine as the substrate. The camphorsulfonate moiety of
Arfonad
was inactive in vitro but caused mild tremors in mice at relatively high doses.
...
PMID:Trimethaphan camsylate (Arfonad) and human plasma cholinesterase. 73 20
