Silodosin (Rapaflo) is an α1-adrenoceptor antagonist with high uroselectivity. It causes practically no orthostatic hypotension (in contrast to other α1 blockers). Since Silodosin is a highly selective inhibitor of the α1A adrenergic receptor, it causes practically no orthostatic hypotension (in contrast to other α1 blockers). On the other hand, the high selectivity seems to cause more problems with ejaculation.
Molecular Weight | 495.53 |
Formula | C25H32F3N3O4 |
CAS Number | 160970-54-7 |
Solubility (25°C) | DMSO 90 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.
[1] Gianluigi Califano, et al. Focus on Silodosin: Pros and Cons of Uroselectivity
[2] No authors listed. Silodosin
[3] Luca Villa, et al. Silodosin: An Update on Efficacy, Safety and Clinical Indications in Urology
[4] No authors listed. Aust Prescr. Silodosin for benign prostatic hypertrophy
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