Parameters | WT | N410K+T423K | na |
---|---|---|---|
[3H]NMS binding | |||
pKib | |||
ACh | 6.06 ± 0.05 | 7.71 ± 0.07* | 5 |
Atropine | 8.71 ± 0.04 | 8.96 ± 0.07 | 5 |
[35S]GTPγS | |||
pEC50c | |||
ACh | 6.28 ± 0.06 | 6.70 ± 0.07* | 3 |
pKBd | |||
Atropine | 8.88 ± 0.09 | 9.00 ± 0.09 | 3 |
pERK1/2 | |||
pEC50c | |||
ACh | 7.99 ± 0.09 | 8.76 ± 0.09* | 3 |
pKBd | |||
Atropine | 9.10 ± 0.17 | 9.38 ± 0.17 | 3 |
pERK1/2, phosphorylated ERK1/2.
↵a Number of experiments performed.
↵b Negative logarithm of the orthosteric ligand equilibrium dissociation constant.
↵c Negative logarithm of agonist potency.
↵d Negative logarithm of the orthosteric antagonist equilibrium dissociation constant derived from functional interactions with ACh.
↵* Significantly different from the corresponding value at the wild type (P < 0.05), Student’s t test.