Parameter | LY2033298 (A) vs Clozapine (B) M_{4} WT | LY2033298 (A) vs CNO (B) M_{4} WT | ACh (A) vs LY2033298 (B) M_{4} DREADD |
---|---|---|---|
pK_{A} | 5.43^{a} | 5.43^{a} | 3.53 ± 0.19 |
pK_{B} | 7.87 ± 0.17 | 6.07 ± 0.09 | 5.39 ± 0.73 |
Log α | 0.65^{a} | 0.55^{a} | 0^{a} |
Log β | −2.61 ± 0.83 | N.F. | 2.19 ± 0.81 |
(β = 0.002) | (β → 0) | (β = 155) | |
Log τ_{A} | 1.66 ± 0.13 | 1.56 ± 0.07 | 0.38 ± 0.12 |
E_{m} | 47.1 ± 4.7 | 69.0 ± 3.8 | 53.7 ± 2.9 |
n
| 1.52 ± 0.46 | 1.36 ± 0.49 | 1.63 ± 0.36 |
pK_{A}, negative logarithm of the dissociation constant of ligand A (agonist); pK_{B}, negative logarithm of the dissociation constant of ligand B (modulator); Log α, logarithm of the binding cooperativity factor; Log β, logarithm of the activation cooperativity factor; Log τ_{A}, logarithm of the agonist operational efficacy parameter; E_{m}, maximum system response level; n, transducer slope factor; N.F., not fitted; parameter estimate was ambiguous and approached a lower boundary (less than −90), indicating that the value of β was practically indistinguishable from zero.
↵ a Fixed as a constant based on the value determined in the radioligand binding assay.