Name | urapidil |
Synonyms | b-66256 ebrantil urapidil URAPIDIL 6-(3-(4-(o-methoxyphenyl)-1-piperazinyl)propylamino)-1,3-dimethyluracil 1,3-dimethyl-6-(3-(4-(o-methoxyphenyl)-1-piperazinyl)proppylamino)-uraci 6-[[3-[4-(2-methoxyphenyl)-1-piperazinyl]propyl]amino]-1,3-dimethyluracil 6-[[3-[4-(2-Methoxyphenyl)-1-Piperazinyl]Propyl]Amino]-1,3-Dimethyluracil 6-[3-[4-(2-methoxyphenyl)piperazin-1-yl]propylamino]-1,3-dimethylpyrimidine-2,4-dione 6-[3-[4-(2-methoxyphenyl)-1-piperazinyl]propylamino]-1,3-dimethylpyrimidine-2,4-dione 6-({3-[4-(2-methoxyphenyl)piperazin-1-yl]propyl}amino)-1,3-dimethylpyrimidine-2,4(1H,3H)-dione 6-[[3-[4-(2-methoxyphenyl)-1-piperazinyl]-propyl]amino]1,3-dimethyl-2,4(1H,3H)-pyrimidinedione |
CAS | 34661-75-1 |
EINECS | 252-130-4 |
InChI | InChI=1/C20H29N5O3/c1-22-18(15-19(26)23(2)20(22)27)21-9-6-10-24-11-13-25(14-12-24)16-7-4-5-8-17(16)28-3/h4-5,7-8,15,21H,6,9-14H2,1-3H3 |
Molecular Formula | C20H29N5O3 |
Molar Mass | 387.48 |
Density | 1.2058 (rough estimate) |
Melting Point | 156-158° |
Boling Point | 513.42°C (rough estimate) |
Flash Point | 285.8°C |
Solubility | DMSO: >10mg/mL |
Vapor Presure | 4.22E-12mmHg at 25°C |
Appearance | Needle crystal |
Color | White to Light yellow to Light orange |
Maximum wavelength(λmax) | ['268nm(MeOH)(lit.)'] |
Merck | 14,9865 |
pKa | 7.10(at 25℃) |
Storage Condition | Sealed in dry,Room Temperature |
Refractive Index | 1.7600 (estimate) |
MDL | MFCD00133908 |
In vitro study | Urapidil is an α1 adrenoreceptor antagonist and a 5-HT 1A receptor agonist. Urapidil does not affect vascular tone at concentrations up to 10 -5 M. Urapidil (10 -5 M) markedly inhibits the alpha 1-adrenergic agonist (phenylephrine)-induced concentration-dependent contractions in aortic rings without endothelium and also to some extent in those with endothelium. Moreover, the inhibitory effect of Urapidil is more pronounced in rings without endothelium than in those with endothelium. Urapidil (10 -5 M) affects neither the vascular tone nor the concentration-dependent contraction to serotonin. |
Hazard Symbols | Xn - Harmful |
Risk Codes | R22 - Harmful if swallowed R36/37/38 - Irritating to eyes, respiratory system and skin. |
Safety Description | 26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. |
RTECS | YQ9862000 |
Toxicity | LD50 in male mice, rats (mg/kg): 750, 550 orally; 260, 145 i.v. (Koenig) |
This product is 6-[[3-[4-(2-methoxyphenyl)-l-farnesyl] propyl] Endo]-1, 3-dimethyluracil. Calculated as the dried product, including not less than 99.0%.
take this product 0.5g, add 0.lmol/L hydrochloric acid solution 25ml, the solution should be clear and colorless.
take an appropriate amount of this product, add the mobile phase to dissolve and dilute to make a solution containing lmg per lml, as a test solution; Take a sample solution of lml with precision, in a 200ml measuring flask, dilute to the scale with mobile phase, and shake well as
Control solution. According to the chromatographic conditions under the content determination item, 20 u1 of the test solution and the control solution are respectively injected into the liquid chromatograph, and the chromatogram is recorded to 2 times of the retention time of the main component peak. If there are impurity peaks in the chromatogram of the test solution, the area of a single impurity peak shall not be greater than the area of the main peak of the control solution (0.5% ), the sum of each impurity peak area shall not be greater than 2 times (1.0%) of the main peak area of the control solution.
take this product about lg, precision weighing, top empty bottle, precision plus dilute sulfuric acid 10ml, sealed, as a test solution; Another precision weighing 1, 2-dichloroethane, the appropriate amount of ethanol, acetone and benzene was added to dilute sulfuric acid to make a solution containing 0.5ug of 1, 2-dichloroethane, 0.5mg of ethanol, mg of acetone and 0.2ug of benzene per 1 ml, 10ml was precisely weighed, placed in a top empty bottle, sealed, and used as a reference solution. According to the determination method of residual solvent (General Principle 0861 first method), the capillary column with polyethylene glycol as stationary liquid is used as the column; The column temperature is 80°C; The detector temperature is 200°C; the inlet temperature was 200°C; The headspace bottle equilibration temperature was 85°C and the equilibration time was 30 minutes. Take the reference solution into the headspace, and the separation degree between the chromatographic peaks of each component shall meet the requirements. The sample solution and the reference solution were sampled by Headspace injection, and the chromatogram was recorded. The peak area was calculated according to the external standard method, 1, 2-dichloroethane, ethanol, the residual amount of acetone and benzene shall be in accordance with the regulations.
take this product, dry to constant weight at 105°C, weight loss shall not exceed 0.5% (General rule 0831).
take l.Og of this product and check it according to law (General rule 0841). The residue left shall not exceed 0.1%.
The residue left under the item of taking the ignition residue shall not contain more than 20 parts per million of heavy metal when examined by law (General rule 0821, Law II).
measured by high performance liquid chromatography (General 0512).
silica gel bonded with eighteen alkyl silane was used as the filler; Sodium acetate solution (8.2g of anhydrous sodium acetate and 40ml of glacial acetic acid were taken, dissolved in water and diluted to 600ml)-methanol (70:30) was used as the mobile phase; the detection wavelength was 268nm. Urapidil and 1, 3-dimethyl-4-(y-chloropropyl amino) uracil (impurity I), the mobile phase was added and dissolved and diluted to prepare urapidil containing 0.lmg with impurities 10.20M1 of the mixed solution of Olmg is injected into the liquid chromatograph, and the chromatogram is recorded. The separation degree of urapidil peak and impurity I peak shall meet the requirements, and the number of theoretical plates shall not be less than 2000 based on urapidil.
take about 25mg of this product, precision weighing, put in 25ml measuring flask, add mobile phase to dissolve and dilute to the scale, shake, take 5ml precision, put in 50ml measuring flask, dilute to scale with mobile phase, shake well, take 20ul with precision, inject into liquid chromatograph, record chromatogram; Take appropriate amount of urapidil reference, the mobile phase was added for dissolution and quantitative dilution to make about 0.lmg solution, the same method for determination. According to the external standard method to calculate the peak area, that is.
antihypertensive drugs.
shade, seal, and store in a cool place.
This product is a sterile aqueous solution of urapidil. Containing urapidil (C20H9N602) shall be between 95.0% and 105.0% of the labeled amount.
This product is colorless or almost colorless clear liquid.
Same as urapidil.
5ml : 25mg
shade, close, and store in a cool place.