Table 1.
Side chain* | EC50,† μM
|
||
---|---|---|---|
α86 | α184 | γ55/δ57‡ | |
Trp | 50 | 50 | 50 |
5-Br-Trp | 53 | 48 | 23 |
5-CN-Trp | 61 | 46 | 25 |
4,5,6,7-F4-Trp | 45 | 62 | 92 |
See Fig. 2 for side-chain structures.
Hill coefficients are all in the range 1.5–2.0.
For all studies of this Trp, mutations were introduced into both the γ55 and δ57 sites, and both mutant subunits were expressed, so both agonist binding sites have the mutant Trp.