“…Structurally it is a substituted benzamide, and a derivative of procainamide. Some benzamides, including procainamide, and local anaesthetic agents, have been shown to inhibit plasma cholinesterase in vitro [1][2][3][4][5]. The nature of such inhibition has been reported to be non-competitive in nature [5].…”
The inhibition of serum cholinesterase by metoclopramide has been previously characterised in vitro at high dilution of the enzyme. We examined the effect of varying enzyme dilution over a range of 1000 fold dilution, and assay temperature at 25 degrees C and 37 degrees C on the fractional inhibition of enzyme activity by metoclopramide. Neither enzyme concentration nor reaction temperature affected this fractional inhibition. Concentrations of metoclopramide producing 50% inhibition of enzyme activity were in the range 1.0-1.9 x 10(-6) M. Lineweaver-Burk analysis of the enzyme reaction suggests that the pattern of this inhibition is competitive.
“…Structurally it is a substituted benzamide, and a derivative of procainamide. Some benzamides, including procainamide, and local anaesthetic agents, have been shown to inhibit plasma cholinesterase in vitro [1][2][3][4][5]. The nature of such inhibition has been reported to be non-competitive in nature [5].…”
The inhibition of serum cholinesterase by metoclopramide has been previously characterised in vitro at high dilution of the enzyme. We examined the effect of varying enzyme dilution over a range of 1000 fold dilution, and assay temperature at 25 degrees C and 37 degrees C on the fractional inhibition of enzyme activity by metoclopramide. Neither enzyme concentration nor reaction temperature affected this fractional inhibition. Concentrations of metoclopramide producing 50% inhibition of enzyme activity were in the range 1.0-1.9 x 10(-6) M. Lineweaver-Burk analysis of the enzyme reaction suggests that the pattern of this inhibition is competitive.
“…Data produced by several investigators show that plasma cholinesterase activity declines during normal pregnancy (15)(16)(17), while others have reported that there is no change in plasma cholinesterase activity between preeclamptic and normal pregnancy (13,(18)(19)(20).…”
Background: Human placenta, a non-neural tissue, contains cholinergic system and high-affinity muscarinic receptors. The role of cholinesterases (CE) in trophoblast function and pregnancy is not clear.
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