Table 1

Drug affinities at MDCK cell alpha-1 adrenoceptors

CompetitorHill slope−log Ki
5-Methylurapidil1.04  ± 0.027.37  ± 0.14
Epinephrine0.83  ± 0.036.38  ± 0.07
Methoxamine0.99  ± 0.044.34  ± 0.21
Norepinephrine0.91  ± 0.096.79  ± 0.28
Oxymetazoline1.06  ± 0.036.77  ± 0.04
Phentolamine1.35  ± 0.278.27  ± 0.04
SDZ NVI-0851.16  ± 0.065.16  ± 0.03
(−)-Tamsulosin0.98  ± 0.099.78  ± 0.03
(+)-Tamsulosin1.04  ± 0.067.82  ± 0.06

None of the drugs had competition curves that were significantly better explained by a two- than a one-site model; agonist competition curves (epinephrine, methoxamine, norepinephrine, oxymetazoline, SDZ NVI-085) were performed in the presence of 100 μM GTP.

  • Data are mean ± SEM of 3 or 4 experiments.