pEC0.5,diss | pKA (pα) | |||||||
---|---|---|---|---|---|---|---|---|
M5 | M5477W→A | M5482W→A | M5477W→A + 482W→A | M5 | M5477W→A | M5482W→A | M5477W→A + 482W→A | |
W84 | 5.41 ± 0.04 | 3.24 ± 0.54 | 5.51 ± 0.04 | 2.75 ± 0.86 | 5.47 ± 0.05a (-0.05 ± 0.05) | 4.72 ± 0.09 (-1.56 ± 0.15) | 5.49 ± 0.03a (0.02 ± 0.04) | 4.50 ± 0.07 (-1.23 ± 0.21) |
Dimethyl-W84 | 5.40 ± 0.04 | 4.08 ± 0.29 | 5.52 ± 0.07 | 4.41 ± 0.24 | N.D. | N.D. | N.D. | N.D. |
Naphmethonium | 6.22 ± 0.03 | 4.94 ± 0.17 | 6.20 ± 0.04 | 4.19 ± 0.29 | N.D. | N.D. | N.D. | N.D. |
Gallamine | 5.41 ± 0.11 | —b | 3.49 ± 0.05 | — | 6.12 ± 0.03 (-1.45 ± 0.11) | 5.05 ± 0.03 (-1.19 ± 0.03) | 5.91 ± 0.15 (-1.35 ± 0.16) | 4.90 ± 0.14 (-1.08 ± 0.10) |
Diallylcaracurine V | 5.57 ± 0.09 | 5.61 ± 0.05 | 5.43 ± 0.09 | 5.87 ± 0.08 | 6.18 ± 0.06 (-0.82 ± 0.08) | 6.41 ± 0.11 (-0.46 ± 0.02) | 6.13 ± 0.04 (-1.05 ± 0.01) | 6.26 ± 0.15 (-0.40 ± 0.03) |
pEC0.5,diss, minus log concentration reducing [3H]NMS dissociation to half of the control rate; pKA, minus log value of the equilibrium dissociation constant for allosteric agent binding to free receptors; N.D., not determined.
↵ a EC0.5,diss was used for curve fitting because of nearly neutral cooperativity as described under Materials and Methods.
↵ b —, no effect up to minus log concentration = 2.5.