TABLE 2

Affinities of ligands for the allosteric site, estimated in terms of Scheme 1

The data represented in Fig. 5 were analyzed simultaneously in terms of Scheme 1 to obtain the parametric values listed in the table. Values of KL and mL (L ≡ A, B, or C in eq. 10) were assigned to each ligand as follows: in the case of NMS, oxotremorine-M, and gallamine, single values of each parameter were common to all of the relevant data; in the case of obidoxime, a single value of mL was common to all of the data, and separate values of KL were assigned to data acquired with obidoxime taken alone and in the presence of 10 mM NMS, 32 mM oxotremorine-M, or 1 mM gallamine. The latter values are listed in the table under KObi, where the value of KL for obidoxime alone is reprinted in brackets for the purpose of comparison. A separate value of kP/ko was assigned to the data from each experiment, and the mean is 1.01 ± 0.01 (n = 36). The value of mL for gallamine was fixed at 1 during the fitting process, as described in the text. The weighted sum of squares was not increased appreciably when the affinity of obidoxime was estimated as 1 parameter rather than 4 (p = 0.089), and the resulting value of KL is −1.73 ± 0.08.

Ligand log KL log KObimL
N-Methyl scopolamine −2.55 ± 0.13 −2.13 ± 0.18 0.89 ± 0.06
Oxotremorine-M −2.29 ± 0.14 −1.58 ± 0.17 0.78 ± 0.04
Gallamine −4.12 ± 0.04 −1.68 ± 0.10 1.0
Obidoxime −1.73 ± 0.91 [−1.73 ± 0.91] 0.11 ± 0.05