Estimates of cooperativity of brucine analogues with [3H]NMS and ACh at muscarinic receptors
m1 | m2 | m3 | m4 | m5 | |
---|---|---|---|---|---|
Cooperativity with [3H]NMS | |||||
Brucine | 0 | + | − | − | −− |
CMB | − | + | − | 0 | − |
BNO | + | ++ | 0 | 0 | + |
N-Benzyl brucine | − | ++ | − | 0 | 0 |
Strychnine | 0 | ++ | − | + | −− |
Cooperativity with ACh | |||||
Brucine | + | − | − | − | −− |
CMB | − | −− | ++ | 0 | −− |
BNO | 0 | − | ++ | + | − |
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.