Table 2

Affinity for the α1b-adrenoceptor-GFP constructs and potency of phenylephrine to stimulate inositol phosphate generation

α1b-Adrenoceptor-GFP ConstructKiEC50
μM nM
Wild Type30  ± 11438  ± 9
3CAM0.4  ± 0.052-a 2.0  ± 0.42-a
A293E46  ± 1280  ± 182-a
D142A61  ± 24180  ± 602-a
M834  ± 14356  ± 54

The affinity of phenylephrine to bind to the various forms of the α1b-adrenoceptor-GFP was estimated from competition binding experiments with [3H]prazosin and corrected for receptor occupancy by [3H]prazosin. EC50values derive from stimulation of [3H]inositol phosphate production above basal levels. Data are presented as mean ± S.E. from three independent experiments.

    • 2-a Significantly different from wild type,P < .01.