Table 1

3 [H]Yohimbine binding to WT, R3, B2, B3, and R3B3 membranes

[3H]Yohimbine Binding
Saturation BindingUK 14,304 Competition
BmaxKdKi
pmol/mg protein nM nM
WT19  ± 27.5  ± 2.283  ± 28
R310  ± 1* 4.9  ± 1.826  ± 4*
B236  ± 3* 8.3  ± 1.995  ± 18
B334  ± 4* 9.5  ± 3.278  ± 15
R3B334  ± 2* 6.3  ± 1.4ND

[3H]Yohimbine binding to WT and mutant α2a-AR in membranes was performed in 96-well plates for 30 min at room temperature. For saturation-binding experiments, 1 to 40 nM [3H]yohimbine was used. Competition assays were done using 10 nM [3H]yohimbine. Data represent the mean ± S.E. of three to five separate experiments performed in duplicate.

    • ∗ , results significantly different from WT, p< .05.

    • ND, not determined.