Naftopidil (Flivas) is a selective α1-adrenergic receptor antagonist or alpha blocker with a Ki of 58.3 nM. Naftopidil (Flivas) is an antihypertensive agent. Naftopidil (Flivas) binds specifically to alpha 1-adrenoceptors. The Ki values are 58.3 nM for naftopidil, 0.43 nM for prazosin, and 197 nM for urapidil. The affinities of naftopidil to alpha 2- and beta-adrenoceptor sites are very low (> 6,000 and > 2,500 nM). Naftopidil relaxes aortic strips precontracted with norepinephrine concentration-dependently, and naftopidil (Flivas) shifts the concentration-response curve of norepinephrine in a parallel manner to the right. The pA2 values are 7.10 for naftopidil, 8.85 for prazosin, and 6.25 for urapidil.
| Molecular Weight | 392.49 |
| Formula | C24H28N2O3 |
| CAS Number | 57149-07-2 |
| Solubility (25°C) | DMSO 70 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| 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.
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