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- W2083705370 abstract "Abstract Acryloylcholine, an unsaturated choline ester was found to be a strong inhibitor of rat and pigeon brain choline acetyltransferase. Substitution of the hydrogen atoms of the C-2 and C-3 carbon atoms in the acylgroup by methylgroups resulted in less potent inhibitors Propionylcholine, the saturated choline ester analogue, was 1000-fold less potent. The rat brain enzyme was not protected against the inhibition by acryloylcholine by high concentration of acetyl-CoA or choline and the inhibition was neither affected by variation in the concentration of sodium chloride nor by variation in pH. The inhibition of rat brain choline acetyltransferase was uncompetitive with respect to choline and acetyl-CoA. The inhibition of pigeon choline acetyltransferase was completely reversible whereas the inhibition of rat choline acetyltransferase could only be reversed with difficulty. Acryloylcholine inhibited acetylcholinesterase reversibly and to the same extent as propionyllcholine. Acryloylcholine was a better substrate for buturylcholinesterase that for acethylcholinesterase. Acryloylcholine caused a neuromuscular block in the rat diaphragm, but this block was probably not due to inhibition of choline acetyltransferase. The ester contracted the esterinized frog rectus abdominus muscle to the same extent as propionylcholine." @default.
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- W2083705370 date "1974-02-01" @default.
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- W2083705370 title "Biochemical and pharmacological properties of acryloylcholine, an inhibitor of choline acetyltransferase" @default.
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- W2083705370 doi "https://doi.org/10.1016/0006-2952(74)90622-4" @default.
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