Table 1

Estimates of cooperativity of brucine analogues with [3H]NMS and ACh at muscarinic receptors

m1m2m3m4m5
Cooperativity with [3H]NMS
 Brucine0+−−
 CMB+0
 BNO+++00+
N-Benzyl brucine++00
 Strychnine0+++−−
Cooperativity with ACh
 Brucine+−−
 CMB−−++0−−
 BNO0+++
N-Benzyl brucine+
 Strychnine−−−−−−

Values of cooperativity (shown as symbols) for brucine, CMB, BNO, and strychnine are from the results of detailed experiments summarized in Tables 3-6.

Values for N-benzyl brucine were derived from results with the semiquantitative equilibrium assay together with the results of the off-rate assay, each with at least two experiments. The logic for analyzing these results is described in the .

    • −−, <0.2; −, 0.2–0.8; 0, 0.81–1.19; +, 1.2–2; ++, >2.