Table 1

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

ConditionGs Pathway: α2A-H (+PTX)Gi Pathway: α2A-L (−PTX)
[Benextramine] = 1 μM6.390.850.
[Benextramine] = 10 μM6.311.
[Benextramine] = 100 μM5.833.080.0213.85.625.00.0132.5
[UK] = 1×K i 1.71.9

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).