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. 2011 May 14;2011:918283. doi: 10.4061/2011/918283

Table 2.

Inhibition of PchP by AACs. Percentage inhibition was measured with 1 mM inhibitor, 10 mM p-NPP, and 2 mM Mg2+ at pH 5.0. Inhibition constants were calculated with the application of the program DYNAFIT from activity curves performed in the presence of 0.5, 1, 2, 4, and 10 mM p-NPP with 2 mM Mg2+ in 100 mM sodium acetate buffer, pH 5.0. The AAC concentrations were 0.01, 0.05, 0.25, and 1 mM. Values shown are averaged from three independent experiments ± SD. PU: partial uncompetitive and C: competitive inhibition.

Inhibitor Number of N-alkyl groups % Inhibition Inhibition constants Type of inhibition
KI1, mM ± SD KI2, mM ± SD
Trimethylamine N,N,N-trimethyl 81 0.21 ± 0.03 0.06 ± 0.01 PU + C
Tetramethylammonium N,N,N,N-tetramethyl 91 0.17 ± 0.04 0.04 ± 0.01 PU + C
Choline 1 N,N,N-trimethyl 85 0.89 ± 0.08 0.10 ± 0.01 PU + C
Chlorocholine 1 N,N,N-trimethyl 82 0.44 ± 0.04 0.12 ± 0.01 PU + C
Betaine 1 N,N,N-trimethyl 26 1.44 ± 0.09 7.75 ± 0.91 PU + C
Hexamethonium 2 N,N,N-trimethyl 85 0.37 ± 0.05 0.08 ± 0.01 PU + C
Decamethonium 2 N,N,N-trimethyl 83 0.21 ± 0.04 0.08 ± 0.01 PU + C
Tubocurarine 1 N-methyl + 1 N,N-dimethyl 22 2.51 ± 0.21 4.10 ± 1.20 PU + C
Neostigmine 1 N,N-dimethyl + 1 N,N,N-trimethyl 55 6.25 ± 0.34 0.57 ± 0.05 PU + C
2-amino-2-methyl-1-propanol 1 N 74 3.94 ± 0.16 0.21 ± 0.01 PU + C
L-histidinol 1 N 56 2.11 ± 0.05 0.31 ± 0.08 PU + C