Table 2

pKB values for α1A or α1Lantagonists against PE-induced contractions of DMA

Antagonist0.3 nM3.0 nM10 nM30 nM100 nM300 nM1000 nM
RS-17053∗9.29  ± 0.088.57  ± 0.148.04  ± 0.227.57  ± 0.26
Rec15/27399.63  ± 0.129.63  ± 0.109.66  ± 0.17
MDL 728328.49  ± 0.148.26  ± 0.088.15  ± 0.17
5-MU∗2-151 9.12  ± 0.098.64  ± 0.098.64  ± 0.18
5-MU∗2-152 9.06  ± 0.068.60  ± 0.098.32  ± 0.15
  • ∗ 5-MU, 5-methylurapidil; pKB values significantly different from one another at increasing antagonist concentrations.

  • 2-151  pKB value for 5-MU at 3000 nM was 8.35 (n = 2); otherwise, n = 4 except for RS-17053 at 3 nM, n = 6; at 30nM, n = 5. In no case was Bmax shown to be reduced significantly.

  • 2-152  pKB values from studies carried out 3 years after first study of 5-MU and used in Fig. 2.