ICI 118,551 hydrochloride is a highly selective β2-adrenoceptor antagonist, with Ki values of 0.7, 49.5 and 611 nM for β2, β1 and β3 receptors, respectively. ICI 118551 (0.2 mg/kg) injected into the jugular vein of the mice, reduces systolic pressure in the pulmonary circuit but not systemic arterial pressure.
| Molecular Weight | 313.86 |
| Formula | C17H27NO2.HCl |
| CAS Number | 72795-01-8 |
| Solubility (25°C) | Water 8 mg/mL DMSO 30 mg/mL |
| Storage | 4°C, dry, sealed |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[5] O E Brodde. The functional importance of beta 1 and beta 2 adrenoceptors in the human heart
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