The KA(app.) and q values for UK-14,304 as calculated from Furchgott analysis of dose-response curves of UK-14,304 in α2A-H (+ PTX ) and α2A-L (− PTX ) before and after partial receptor alkylation by the irreversible inhibitor benextramine
| Condition | Gs Pathway: α2A-H (+PTX) | Gi Pathway: α2A-L (−PTX) | ||||||
|---|---|---|---|---|---|---|---|---|
| pKA(app.) | KA(app.)/Ki | q | Smax/Emax | pKA(app.) | KA(app.)/Ki | q | Smax/Emax | |
| [Benextramine] = 1 μM | 6.39 | 0.85 | 0.28 | 2.4 | 6.23 | 1.22 | 0.36 | 2.4 |
| [Benextramine] = 10 μM | 6.31 | 1.02 | 0.11 | 4.0 | 6.33 | 0.99 | 0.25 | 2.9 |
| [Benextramine] = 100 μM | 5.83 | 3.08 | 0.02 | 13.8 | 5.62 | 5.0 | 0.01 | 32.5 |
| [UK] = 1×K i | 1.7 | 1.9 | ||||||
Smax/Emax ratios were calculated from the q values and Emax values after partial receptor alkylation and from the submaximal response of UK-14,304 at a 1× Ki concentration, as described in the text (Data Analysis).