TABLE 1

Potency (pEC50), maximum response (Emax), and α value (Emax relative to norepinephrine) of agonists at the human α1A-AR

Ca2+ ReleasecAMPECAR
Norepinephrine
    pEC508.58 ± 0.075.55 ± 0.057.36 ± 0.04
    Emax92.8 ± 1.727.3 ± 0.5152.2 ± 1.1
    α1.00 (6)1.00 (5)1.00 (4)
Methoxamine
    pEC507.44 ± 0.054.39 ± 0.066.95 ± 0.04
    Emax87.7 ± 1.625.7 ± 0.8146.5 ± 0.9
    α0.95 (6)0.94 (5)0.96 (4)
Phenylephrine
    pEC508.10 ± 0.064.93 ± 0.068.29 ± 0.07
    Emax91.7 ± 1.623.4 ± 0.6148.3 ± 1.6
    α0.99 (6)0.86 (5)0.97 (4)
Oxymetazoline
    pEC508.86 ± 0.10N.D.8.55 ± 0.05
    Emax78.4 ± 2.4N.D.146.6 ± 1.0
    α0.84 (6)N.D.0.96 (4)
Cirazoline
    pEC508.54 ± 0.126.89 ± 0.088.13 ± 0.03
    Emax97.0 ± 3.514.8 ± 0.5148.5 ± 0.6
    α1.05 (6)0.54 (5)0.98 (4)
A61603
    pEC509.63 ± 0.067.59 ± 0.059.09 ± 0.05
    Emax97.4 ± 2.028.6 ± 0.5147.6 ± 1.1
    α1.05 (6)1.05 (5)0.97 (4)
  • N.D., not determined.