Molecular Formula | C24H28N2O3 |
Molar Mass | 392.49 |
Density | 1.1592 (rough estimate) |
Melting Point | 127 °C |
Boling Point | 517.2°C (rough estimate) |
Flash Point | 318.3°C |
Water Solubility | methanol: >10 mg/mL |
Solubility | Soluble in Dichloromethane, DMSO and Methanol |
Vapor Presure | 2.22E-15mmHg at 25°C |
Appearance | White-like solid |
Color | white |
Merck | 14,6356 |
pKa | 14.01±0.20(Predicted) |
Storage Condition | Sealed in dry,Room Temperature |
Refractive Index | 1.6300 (estimate) |
MDL | MFCD00242741 |
Use | Vasodilator for the treatment of mild to moderate essential hypertension |
UN IDs | 3077 |
WGK Germany | 3 |
RTECS | TL9336500 |
HS Code | 29335990 |
Toxicity | LD50 in mice, rats (g/kg): 1.3, 6.4 orally (Himmel) |
an off-white crystal was obtained from isopropanol, melting point 125-126 °c. There are data for colorless crystals. mp125 ~ 129 deg C. Insoluble in water. Octanol, water partition coefficient of 75, with moderate lipophilicity.
naphthol and tetrabutylammonium bromide were added to epichlorohydrin, the reaction was stirred, and sodium hydroxide aqueous solution was added dropwise, the temperature was controlled not to exceed 110 ℃, and the reaction was completed, 3-(1-naphthyloxy)-1,2-propylene oxide was obtained by post-treatment. This product and 1-(2-methoxyphenyl) piperazine were added to ethanol, reacted under reflux, cooled, filtered, dried and recrystallized to give naftopidil.
developed by the German company Boehling Mannheim, which was first launched in Japan in March 1999. Naftopidil is a selective ai receptor antagonist, which can inhibit the increase of blood pressure caused by a1 receptor, and has calcium ion antagonism, receptor blocker, calcium antagonist and 5-HT antagonism, and has a long time to reduce blood pressure, no drug resistance. It is a safe and effective new antihypertensive drug for the long-term treatment of hypertension in patients with hypertension complicated with hyperlipidemia, diabetes mellitus and prostatic hyperplasia. It is also used to treat dysuria with prostatic hypertrophy.
mouse, rat oral LDso:1.3g]kg, 6.4g/kg.