Table 2.
Vessel | hU-II | GSK248451 | Urantide | SB-710411 |
---|---|---|---|---|
Rat aorta |
Agonist (full) |
Antagonist |
Antagonist |
Antagonist |
Cat femoral artery |
Agonist (full) |
Antagonist |
Agonist (weak partial) |
Antagonist |
Cat aorta |
Agonist (full) |
Antagonist |
Agonist (weak partial) |
Inactive |
Monkey renal artery |
Agonist (full) |
Antagonist |
Agonist (moderate partial) |
Agonist (moderate partial) |
Monkey mesenteric artery | Agonist (full) | Antagonist | Agonist (moderate partial) | Agonist (full) |
Weak partial agonists were defined as those exhibiting a relative efficacy [α] <0.5. Moderate partial agonists exhibited relative efficacies [α]⩾0.5 to ⩽0.9. Full agonists possessed relative efficacies [α] >0.9 (intrinsic activities are expressed relative to hU-II, considered a full agonist where relative efficacy [α] is 1.0). ‘Inactive' entities (10 μM) exhibited neither agonist nor antagonist properties in the vessels studied (see Tables 3 and 4).