apresine
Hydralazine hydrochloride
CAS: 304-20-1
Molecular Formula: C8H9ClN4
apresine - Names and Identifiers
| Name | Hydralazine hydrochloride |
| Synonyms | Asozart apresine Hydrapress aiselazine Hydralazine hcl apresoline-esidrix 1-hydrazinylphthalazine Hydralazine hydrochloride 1(2H)-Phthalazinone hydrazone 1-Hydrazinophthalazine hydrochloride 1-hydrazinophthalazinemonohydrochloride 1-hydrazino-phthalazinmonohydrochloride 1(2h)-phthalazinone,hydrazone,monohydrochloride |
| CAS | 304-20-1 |
| EINECS | 206-151-0 |
| InChI | InChI=1/C8H8N4.ClH/c9-11-8-7-4-2-1-3-6(7)5-10-12-8;/h1-5H,9H2,(H,11,12);1H/p-1 |
| InChIKey | ZUXNZUWOTSUBMN-UHFFFAOYSA-N |
apresine - Physico-chemical Properties
| Molecular Formula | C8H9ClN4 |
| Molar Mass | 196.64 |
| Density | 1.2961 (rough estimate) |
| Melting Point | 273°C |
| Boling Point | 322.13°C (rough estimate) |
| Water Solubility | Soluble in water. Slightly soluble in diethyl ether and alcohol. |
| Solubility | Soluble in water, slightly soluble in ethanol (96 per cent), very slightly soluble in methylene chloride |
| Appearance | White crystalline solid |
| Color | White to Almost white |
| Merck | 14,4763 |
| BRN | 3568329 |
| PH | pH (20g/l, 25℃) : 3.5～4.5 |
| Storage Condition | 2-8°C |
| Stability | Stable. Incompatible with strong oxidizing agents. |
| Refractive Index | 1.6110 (estimate) |
| MDL | MFCD00135998 |
| Use | Used as an antihypertensive agent |
| In vitro study | Hydralazine impairs up-regulation of RAG-2 gene expression and reduces secondary immunoglobulin gene rearrangements. Hydralazine subverts B- lymphocyte self-tolerance and leads to the generation of pathogenic autoreactivity by disrupting Receptor editing. Hydralazine removes acrolein directly and reduces the activity of acrolein in cells, thereby inhibiting macromolecular adduction. Hydralazine inhibited crosslinking after 30 minutes after the start of acrolein treatment, but was ineffective after 90 minutes. Hydralazine(0.1-10 mM) inhibits extracellular and intracellular ROS production in inflammatory macrophages, likely affecting xanthine oxidase (XO) through ROS clearance mechanisms and the superoxide radical (O(2)(*-))-Production of nicotinamide adenine dinucleotide/nicotinamide adenine dinucleotide phosphate (NADH/ NADPH) oxidase. Hydralazine(0.1-10 mM) significantly reduced NO(*) production, and this effect resulted in NOS-2 gene expression and protein synthesis. Hydralazine also effectively blocked COX-2 gene expression, which was associated with decreased protein levels and PGE(2) synthesis. In the guinea pig spinal cord in vitro, Hydralazine not only protects against acrolein-mediated injury, but also compresses. Hydralazine can significantly reduce acrolein-induced superoxide production, glutathione depletion, mitochondrial dysfunction, loss of membrane integrity, and decrease compound action potential conduction. |
| In vivo study | In mice, Hydralazine dose-dependently protects against increased plasma marker enzymes, but not liver glutathione depletion of allyl alcohol production. |
apresine - Risk and Safety
| Hazard Symbols | Xn - Harmful |
| Risk Codes | R22 - Harmful if swallowed R36/37/38 - Irritating to eyes, respiratory system and skin. |
| Safety Description | S26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. 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.) |
| UN IDs | UN 2811 6.1/PG 3 |
| WGK Germany | 3 |
| RTECS | TH9000000 |
| TSCA | Yes |
| HS Code | 29339900 |
| Hazard Class | 6.1 |
| Packing Group | III |
| Toxicity | LD50 oral in rat: 280mg/kg |
apresine - Standard
Authoritative Data Verified Data
This product is the hydrochloride of 1-hydrazinyl-2, 3-naphthyridine. The content of C8H8N4 • HC1 shall be between 98.0% and 102.0% based on the dry product.
Last Update：2024-01-02 23:10:35
apresine - Trait
Authoritative Data Verified Data
- This product is white to light yellow crystalline powder; Odorless.
- This product is soluble in water, slightly soluble in ethanol, and slightly soluble in ethanol.
Last Update：2022-01-01 15:06:45
apresine - Differential diagnosis
Authoritative Data Verified Data
- take about 10mg of this product, put it in a test tube, add 2ml of water to dissolve it, and add 1ml of ammonia silver nitrate test solution to generate bubbles and black turbidity, and generate a silver mirror on the wall of the test tube.
- take about 10 mg of this product, add about 5ml of water, 2 drops of dilute hydrochloric acid and several drops of ferric chloride test solution, neutralize with sodium hydroxide test solution, the solution is initially red, then turn blue.
- take this product, add water to dissolve and dilute to make a solution containing about 10ug per lml, and measure by UV-visible spectrophotometry (General rule 0401), at 260nm, there is a maximum absorption at the wavelength of 303nm and 315nm.
- The infrared absorption spectrum of this product should be consistent with that of the control (Spectrum set 374).
- the aqueous solution of this product was chloride identification (1) of the reaction (General 0301).
Last Update：2022-01-01 15:06:46
apresine - Exam
Authoritative Data Verified Data
acidity
take 0.50g of this product, add 25ml of water to dissolve it, and determine it according to law (General rule 0631). The pH value should be 3.5-4.5.
clarity and color of solution
take 0.20g of this product, Add 10ml of water to dissolve, the solution should be clarified; If the color is colored, check according to law (General rule 0901 The first law), and yellow 4 standard colorimetric liquid comparison, not deeper.
sulfate
take 0.50g of this product and check it according to law (General rule 0802). If there is a mudpool, it should not be more concentrated (0.04%) compared with the control solution made of 2.0 ml of standard potassium sulfate solution.
Free hydrazine
take 0.10g of this product, add 5ml of water and salicylaldehyde ethanol solution (1-20 )0. Lml, 1 min should not occur turbidity.
insoluble in water
take 2.og of this product, add 100ml of water, shake for 30 minutes to dissolve, filter with constant weight No. 5 vertical melting glass crucible, and wash the filter residue with water for 3 times, 10ml each time, after drying at 105 ° C. To constant weight, the residue should not exceed 10mg (0.5%).
Related substances
take this product, add mobile phase to dissolve and dilute to make a solution containing 0.5mg per 1ml as a test solution; Take 1ml for precision measurement and put it in a 100ml measuring flask, dilute to the scale with the mobile phase, shake, and serve as a control solution. According to the high performance liquid chromatography (General 0512) test, using cyanosilane bonded silica gel as filler; Buffer solution (weigh sodium dodecyl sulfate 1.44g and tetrabutylammonium bromide 0.75g), water was added to dissolve and diluted to 0.05 mL, and the pH value was adjusted to 3.0 with mol/L sulfuric acid solution. The mobile phase was acetonitrile (78:22); The detection wavelength was 230nm. Take appropriate amount of Hydralazine Hydrochloride and 2, 3-naphthyridine respectively, add mobile phase to dissolve and dilute to prepare solution containing 20ug and 2ug respectively per lml, and inject 20u1 into human liquid chromatograph, the degree of separation of 2, 3-naphthyridine peak and hydrazinium peak should be greater than 2.5. 20ul of the test solution and the control solution were respectively injected into the human liquid chromatograph, and the chromatogram was recorded to 3 times of the retention time of the main component peak. If there are impurity peaks in the chromatogram of the test solution, the sum of each impurity peak area shall not be greater than the main peak area of the control solution (1.0%).
loss on drying
take this product, dry to constant weight at 105°C, weight loss shall not exceed 0.5% (General rule 0831).
ignition residue
take l.Og of this product and check it according to law (General rule 0841). The residue left shall not exceed 0.1%.
precious metals
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).
Last Update：2022-01-01 15:06:47
apresine - Content determination
Authoritative Data Verified Data
take about 0.2g of this product, weigh it accurately, put it in a 100ml measuring flask, add water to dissolve it and dilute it to the scale, shake it well, take 25ml accurately, put it in an iodine bottle, add 25ml of bromine titration solution (0.05mol/L) and 5ml of hydrochloric acid, immediately pack, shake well, place in the dark for 15 minutes, open the stopper carefully, add 7ml of potassium iodide test solution, immediately plug, shake, with sodium thiosulfate titration solution (0.1 mol/L) titration, to the near end point, add 2ml of starch indicator solution, continue titration to blue disappeared, and the titration result is corrected by blank test. Each 1 ml of bromine titration solution (0.05 mol/L) corresponds to mg of C8H8N4. Hc1.
Last Update：2022-01-01 15:06:47
apresine - Category
Authoritative Data Verified Data
anti-hypertension drugs.
Last Update：2022-01-01 15:06:48
apresine - Storage
Authoritative Data Verified Data
light-shielded, sealed, and stored in a dry place.
Last Update：2022-01-01 15:06:48
apresine - Hydralazine Hydrochloride Tablets
Authoritative Data Verified Data
This product contains Hydralazine Hydrochloride (C8H8N4 • HCI) should be 90.0% ~ 110.0% of the label amount.
trait
This product is white or white-like tablets or sugar-coated tablets, after removing the coating, white or white.
identification
take an appropriate amount of fine powder of this product (about 30mg equivalent to Hydralazine Hydrochloride), add 10ml of water, shake to dissolve Hydralazine Hydrochloride, filter, the filtrate showed the same reaction according to the tests of identification (1) and (2) in the case of Hydralazine Hydrochloride.
examination
- dissolution: according to the dissolution and release determination method (General rule 0931 method 1), 100 hydrochloric acid solution (9-l000) was used as dissolution medium at RPM, operate according to law, after 30 minutes (sugar-coated tablets for 60 minutes), take 10ml of solution, filter, take appropriate amount of filtrate with precision, dilute with dissolution medium to make a solution containing Hydralazine Hydrochloride 10 ~ 20ug per lml; Take an appropriate amount of Hydralazine Hydrochloride reference substance, the dissolution medium was added and dissolved and diluted to prepare a solution containing 10-20ug per 1 ml. The absorbance of each of the above two Solutions was measured at a wavelength of 0401 nm by ultraviolet-visible spectrophotometry (general), and the elution amount of each tablet was calculated. The limit is 70% of the labeled amount and shall be in accordance with the provisions.
- others shall be in accordance with the relevant provisions under the item of tablets (General rule 0101).
Content determination
take 25 tablets (lOmg specifications) or 20 tablets (25mg, 50mg specifications) of this product, if it is sugar-coated tablets, remove the coating, precision weighing, grinding, accurately weigh an appropriate amount (about 0.1g of Hydralazine Hydrochloride), put it in a mortar, add a small amount of water, grind it into a paste, then move it into a 50ml measuring flask, wash the mortar with water, wash the lotion and put it in a measuring flask, dilute to scale with water, shake well, filter with dry filter paper, take 25ml of filtrate accurately, and set it in iodine bottle according to the method of Hydralazine Hydrochloride, precision Plus bromine titration solution (0.05mol/L)25ml, according to the law. Each 1 ml of bromine titrant (0.05mol/L) corresponds to 4.916mg of C8H8N4. HCl.
category storage
with Hydralazine Hydrochloride.
specification
(l)10mg (2)25mg (3)50mg
Last Update：2022-01-01 15:06:49
apresine - Reference Information
| EPA chemical information | Information provided by: ofmpub.epa.gov (external link) |
| Introduction | Hydrazine hydrochloride, also known as hydrazine hydrochloride, is a known compound. Its chemical name is 1(2H)-2, 3 diazaphthalene ketone hydrazone, and its English name is Hydralazine. It has the effect of relaxing blood vessels and is often used in the treatment of moderate hypertension. In clinical application, it is usually combined with β-blockers and diuretics. Hydralazine is an antihypertensive drug that directly acts on the smooth muscle of arteries and arterioles. It reduces peripheral resistance by relaxing vascular smooth muscle, thereby achieving the purpose of lowering blood pressure. Hydralazine has a moderate blood pressure lowering effect, which is characterized by a significant drop in diastolic blood pressure and an increase in renal blood flow. |
| pharmacological action | 1) antihypertensive: the exact mechanism of antihypertensive action is unknown. The main expansion of small arteries, small effect on the vein, so that the peripheral vascular resistance is reduced, heart rate increases, heart stroke volume and cardiac output increase. Long-term application can increase the secretion of renin, increase aldosterone, and reduce the effect of water and sodium retention. 2) Heart failure: Hydralazine hydrochloride increases cardiac output and reduces vascular resistance and afterload. |
| drug interaction | 1. hydralazine hydrochloride and non-steroidal anti-inflammatory analgesics can weaken the antihypertensive effect. 2. The use of sympathomimetic amines and hydralazine hydrochloride can reduce the antihypertensive effect of this product. 3. Hydralazine hydrochloride and diazoxide or other antihypertensive drugs can strengthen the antihypertensive effect. |
| Preparation | A process method for industrial production of hydralazine hydrochloride, using o-cyanobenzaldehyde as raw material, cyclization and condensation of hydrazine hydrochloride, and then salt with hydrochloric acid to prepare hydralazine hydrochloride, the process steps are: 1) Production of hydrazine hydrochloride: add a 50% mixture of hydrazine hydrate and ethanol dropwise into ethanol chloride, the temperature is controlled at -10 ℃ ~-15 ℃ to generate hydrazine hydrochloride ethanol solution, and the final pH2 ~ 4. 2) Production of hydralazine hydrochloride: o-cyanobenzaldehyde is added in batches in hydrazine hydrochloride ethanol solution, the temperature is slowly increased and the reaction temperature is controlled at 45 ℃ ~ 50 ℃, the reaction is 24~48 hours, after the reaction is over, CP-grade hydrochloric acid is added to adjust the PH value to pH1 ~ 2, then cool down, crystallide, filter, wash and dry. 3) Refining: The crude product is put into ethanol solution according to the ratio of 1: 1(M: V), heated and dissolved, then added with appropriate amount of activated carbon for decolorization, pressure filtration, cooling and crystallization, filtering and drying. The production route is as follows: |
| Biological activity | Hydralazine HCl is the hydrochloride form of Hydralazine (Apresoline) and is a direct and effective smooth muscle relaxant with IC50 of 1.9 mM. |
| Target | Value |
| Use | Used as an antihypertensive drug |
| toxic substance data | information provided by: pubchem.ncbi.nlm.nih.gov (external link) |
Last Update：2024-04-09 02:00:08
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Product Name: Hydralazine hydrochloride Request for quotation
CAS: 304-20-1
Tel: 0086-551-65418684
Email: sales@tnjchem.com
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Mobile: 0086 189 4982 3763
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CAS: 304-20-1
Tel: 0086-551-65418684
Email: sales@tnjchem.com
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Mobile: 0086 189 4982 3763
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Product Name: 1-hydrazinyl-Phthalazine hydrochloride Visit Supplier Webpage Request for quotationCAS: 304-20-1
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