Molecular Formula | C18H22ClNO.ClH |
Molar Mass | 340.29 |
Melting Point | 137.5°C |
Boling Point | 381.5°C at 760 mmHg |
Flash Point | 184.5°C |
Water Solubility | <0.01 g/100 mL at 18.5 ºC |
Solubility | soluble in organic solvents such as ethanol, DMSO, and dimethyl formamide (DMF). |
Vapor Presure | 5.07E-06mmHg at 25°C |
Appearance | powder |
Color | white |
Merck | 14,7256 |
pKa | pKa 4.4 (Uncertain) |
Storage Condition | 15-25°C |
Stability | Stable for 2 years as supplied. Solutions in DMSO or distilled water may be stored at -20°C for up to 3 months. |
MDL | MFCD00055152 |
Physical and Chemical Properties | Properties: white or white crystalline powder; Odorless, almost tasteless Melting Point: 137.5-140 ° C |
Use | For the treatment of pheochromocytoma, Raynaud's syndrome, hand and foot cyanosis and chilblain sequelae |
In vitro study | The IC 50 (100 nM) derived from the blockade of [ 3 H]yohimbine binding by Phenoxybenzamine hydrochloride is significantly less than the IC 50 (550 nM) for the corresponding reversal by Phenoxybenzamine hydrochloride of the effects of norepinephrine on cyclic AMP accumulation. Phenoxybenzamine hydrochloride (50 nM) in conbination with Phenoxybenzamine hydrochloridetolamine (1000 nM) enhances Phenoxybenzamine hydrochlorideylephrine-induced contraction compared with pretreatment with Phenoxybenzamine hydrochloride (50 nM) alone in endothelium-intact aortae. Combined treatment with either dexmedetomidine (300 or 1000 nM) and Phenoxybenzamine hydrochloride (50 nM) or Phenoxybenzamine hydrochloridetolamine (1000 nM) and Phenoxybenzamine hydrochloride (50 nM) enhance Phenoxybenzamine hydrochlorideylephrine-induced contraction compared with Phenoxybenzamine hydrochloride alone (50 nM). In addition, combined treatment with Phenoxybenzamine hydrochloridetolamine and Phenoxybenzamine hydrochloride enhances Phenoxybenzamine hydrochlorideylephrine-induced contraction compared with dexmedetomidine (1000 nM) and Phenoxybenzamine hydrochloride combined treatment. Combined treatment with high concentrations of dexmedetomidine (1000 nM) and Phenoxybenzamine hydrochloride enhances Phenoxybenzamine hydrochlorideylephrine-induced contraction compared with combined treatment with low concentrations of dexmedetomidine (300 nM) and Phenoxybenzamine hydrochloride. Phenoxybenzamine hydrochloride (0.1-100 μM) inhibits glioma proliferation, migration, and invasion and suppresses the tumorigenesis capacity. Phenoxybenzamine hydrochloride also inhibits self-renewal of glioma stem-like cells. Phenoxybenzamine hydrochloride activates LINGO-1 and inhibits the TrkB-Akt pathway. Phenoxybenzamine hydrochloride (0.1 μM-1 mM) preserves primary neurons within the CA1, CA3 and dentate gyrus and produces a robust neuroprotective effect, and prevents neuronal death from OGD in all regions of the hippocampus when delivered at 2, 4, and 8 h post-OGD at 100 μM. |
In vivo study | Phenoxybenzamine hydrochloride (20 nM, s.c.) effectively suppresses the tumorigenesis of glioma cells in mice and the cell density in Phenoxybenzamine hydrochloride-U87MG xenografts decreases significantly. Phenoxybenzamine hydrochloride (1 mg/kg, i.v.) treated rats shows significant improvements in NSS and foot fault scoring. |
Hazard Symbols | Xn - Harmful |
Risk Codes | R22 - Harmful if swallowed R40 - Limited evidence of a carcinogenic effect |
Safety Description | S22 - Do not breathe dust. S36/37/39 - Wear suitable protective clothing, gloves and eye/face protection. S45 - In case of accident or if you feel unwell, seek medical advice immediately (show the label whenever possible.) |
WGK Germany | 3 |
RTECS | DP3750000 |
HS Code | 2922299000 |
This product is N-(l-methyl-2-phenoxyethyl)-N-(2-chloroethyl) benzylamine hydrochloride. Based on the dry product, the content of C18H22C1NO • HCl should be 98.0% to 102.0%.
The melting point of this product (General 0612) is 137~140°C.
take 0.2g of this product, put it in a 10ml measuring flask, add methanol to dissolve and dilute to the scale, shake well, as a test solution; Take 1ml for precision measurement, put it in a ml measuring flask, as a control solution, it was diluted to the scale with methanol and shaken. 1ml of the control solution was accurately measured, placed in a 5ml measuring flask, diluted to the scale with methanol, and shaken to obtain a sensitivity solution. According to the thin layer chromatography (General 0502) test, draw 10ul of each of the above three solutions, respectively, on the same silica gel G thin layer plate, with acetone-chloroform (8:2) as the developing solvent, dry, spray with dilute bismuth potassium iodide solution, immediately check, the sensitivity of the solution of the main spots should be clearly visible. If the test solution shows impurity spots, the color should not be deeper (0.5%) than the main spot of the control solution.
take this product, put the phosphorus pentoxide dryer under reduced pressure to dry to constant weight, loss of weight should 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 octa-alkyl silane was used as filler, and methanol-ammonium acetate buffer (10g of ammonium acetate was dissolved in 3.0 ml of water, pH was adjusted to with phosphoric acid)(80:20) was used as mobile phase; the detection wavelength was 267nm. The number of theoretical plates shall not be less than 2000 based on the calculation of phenol benzhydrin peak, and the separation degree between phenol benzhydrin peak and adjacent impurity peak shall meet the requirements.
take the right amount of this product, precision weighing, plus O. 1 mol / L hydrochloric acid solution is dissolved and quantitatively diluted to make a solution containing 0.5mg per 1 ml, which is used as a test solution, and 10u1 is accurately measured and injected into the human liquid chromatograph, and the chromatogram is recorded; an appropriate amount of phenoxybenzamine hydrochloride reference substance was measured with the same method. According to the external standard method to calculate the peak area, that is.
a adrenergic receptor blockers.
light shielding, sealed storage.
This product contains phenoxybenzamine hydrochloride (C18H22ClNO • HCl) should be 90.0% ~ 110.0% of the label amount.
This product is a white tablet or film-coated tablet, White after removing the coating.
Take 20 tablets of this product, precision weighing, fine grinding, precision weighing an appropriate amount (about equivalent to phenoxybenzamine hydrochloride 10mg ), put it in a 100ml measuring flask, add 0.1 mol/L hydrochloric acid solution to dissolve phenoxybenzamine hydrochloride and dilute to the scale, shake, filter, take the continued filtrate as a test solution; in addition, take 10mg of phenoxybenzamine hydrochloride reference product, put it in a 100ml measuring flask, add 0.1 mol/L hydrochloric acid solution was dissolved and diluted to the scale, and shaken to serve as a control solution. The above two kinds of solutions were taken, and the absorbance was measured at the wavelength of 0401 Mn by ultraviolet-visible spectrophotometry (general rule), and calculated.
with phenoxybenzamine hydrochloride.
(l ) 5mg (2)10mg
light shielding, sealed storage.
This product is a sterile aqueous solution of phenoxybenzamine hydrochloride. Phenoxybenzamine hydrochloride (C18H22ClNO • HC1) shall be present in an amount of 90.0% to 110.0% of the label amount.
This product is a clear colorless liquid.
take 1ml of this product, add 0.Olmol / L hydrochloric acid solution 20ml, with chloroform shaking extraction, extract plus acid treatment of three methane (chloroform, with O. Olmol / L hydrochloric acid solution shaking washing, after separation, add anhydrous sodium sulfate dehydration, take the supernatant distillation) diluted to each 1ml containing about 0. A solution of 1 mg has an absorption maximum at wavelengths of 272nm and 279nm as determined by UV-Vis spectrophotometry (General rule 0401).
take 10ml of this product accurately, put it on a water bath to dry, dry at 105°C for 30 minutes, let it cool, add 10ml of glacial acetic acid and 5ml of Mercury test solution for acid fermented grains to dissolve, add 1 drop of crystal violet indicator solution, titrate the solution with high gas acid titration solution (0.05mol/L) to blue-green, and correct the titration result with blank test. Each 1 ml of perchloric acid titration solution (0.05mol/L) corresponds to 17.02mg of C18H22ClNO. Hc1.
with phenoxybenzamine hydrochloride.
lml : 1Omg
light shielding, closed storage.