Buspar hydrochloride
buspirone hydrochloride
CAS: 33386-08-2
Molecular Formula: C21H32ClN5O2
Buspar hydrochloride - Names and Identifiers
| Name | buspirone hydrochloride |
| Synonyms | axoren bespar buspinol BUSPIRONE HCL Buspirone HCl Buspar hydrochloride Buspiron hydrochloride buspirone hydrochloride 1-cyclopentanediacetimide,n-(4-(4-(2-pyrimidinyl)-1-piperazinyl)butyl)-h 8-(4-(4-(2-pyrimidinyl)-1-piperazinyl)butyl)-8-azaspiro(4.5)decane-9-dione 1-[4-(7,9-dioxo-8-azaspiro[4.5]dec-8-yl)butyl]-4-(pyrimidin-2-yl)piperazin-1-ium 8-[4-[4-(2-pyrimidinyl)-1-piperazin-1-iumyl]butyl]-8-azaspiro[4.5]decane-7,9-dione 8-[4-[4-(2-PYRIMIDINYL)-1-PIPERAZINYL]BUTYL]-8-AZASPIRO[4,5]DECANE-7,9-DIONE HYDROCHLORIDE |
| CAS | 33386-08-2 |
| EINECS | 251-489-4 |
| InChI | InChI=1/C21H31N5O2/c27-18-16-21(6-1-2-7-21)17-19(28)26(18)11-4-3-10-24-12-14-25(15-13-24)20-22-8-5-9-23-20/h5,8-9H,1-4,6-7,10-17H2/p+1 |
Buspar hydrochloride - Physico-chemical Properties
| Molecular Formula | C21H32ClN5O2 |
| Molar Mass | 421.96 |
| Melting Point | 201.5-202.50C |
| Boling Point | 613.9°C at 760 mmHg |
| Flash Point | 9℃ |
| Water Solubility | Soluble in methanol (50 mg/ml), water (partly), DMSO (100 mM). |
| Solubility | Freely soluble in water and in methanol, practically insoluble in acetone. |
| Vapor Presure | 5.24E-15mmHg at 25°C |
| Appearance | neat |
| Storage Condition | 2-8°C |
| Physical and Chemical Properties | White crystalline powder. |
| In vitro study | Buspirone is a clinically effective non-benzodiazepine anxiolytic drug that causes inhibition of the activation of these neurons when administered intravenously (ED50=0.011 mg/kg), intraperitoneal injection (ED50=0.088 mg/kg, I. P.), and intragastric injection (effective dose = 1.0-20.0 mg/kg). Buspirone also inhibited these cells when administered to recording neurons by microelectrophoresis. Buspirone is eliminated primarily by oxidative metabolism, yielding several hydroxylated metabolites, including 5-hydroxy-buspirone and 1-pyrimidinylpiperazine. |
| In vivo study | Busspirone (3 mg/only, I. P.) completely inhibited vibration-induced ultrasonic vocalization in a dose-dependent manner, busspirone was injected systemically and microinjected into the dorsal raphe nucleus, this brain area is rich in somato-dendritic 5-HT1A receptors. Busspirone (20 mg/kg) reduced the time of immobility in the forced swim test in rats. Buspirone is a serotonin (5HT(1A) receptor agonist) anxiolytic with D(2) dopaminergic effects in the anxious zebrafish model. By acting on 5-HT(1A) receptors in L-dopa-primed rats, buspione dose-dependently reduces LID and improves I-DOPA-related mobility. In L-DOPA-wild type rats, busspirone delays the development of LID and simultaneously enhances the antiparkinsonian efficacy of I-DOPA, suggesting that 5-HT(1A) receptor agonists reduce the potential long-term benefits of L-dopa. |
Buspar hydrochloride - Risk and Safety
| Risk Codes | R25 - Toxic if swallowed R36/37/38 - Irritating to eyes, respiratory system and skin. R20/21/22 - Harmful by inhalation, in contact with skin and if swallowed. R39/23/24/25 - R23/24/25 - Toxic by inhalation, in contact with skin and if swallowed. R11 - Highly Flammable |
| Safety Description | S45 - In case of accident or if you feel unwell, seek medical advice immediately (show the label whenever possible.) S36 - Wear suitable protective clothing. S26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. S36/37 - Wear suitable protective clothing and gloves. S16 - Keep away from sources of ignition. |
| UN IDs | UN 2811 6.1/PG 3 |
| WGK Germany | 3 |
| RTECS | CL9915000 |
| HS Code | 29335995 |
| Hazard Class | 6.1 |
| Toxicity | LD50 i.p. in rats: 136 mg/kg (Allen) |
Buspar hydrochloride - Standard
Authoritative Data Verified Data
This product is N-[4-[4-(2-pyrimidinyl)-l-piperazinyl] butyl]-8-azaspiro [4,5] decane-7, 9-dione hydrochloride. Calculated as dry product, containing not less than 98.5% from C21H31N5O2 • hc1.
Last Update：2024-01-02 23:10:35
Buspar hydrochloride - Trait
Authoritative Data Verified Data
- This product is white or off-white crystalline powder; Odorless.
- This product is soluble in water, methanol or chloroform, dissolved in ethanol; Almost insoluble in ether.
melting point
The melting point of this product (General 0612) is 202~206°C.
Last Update：2022-01-01 14:20:04
Buspar hydrochloride - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.37 ml | 11.849 ml | 23.699 ml |
| 5 mM | 0.474 ml | 2.37 ml | 4.74 ml |
| 10 mM | 0.237 ml | 1.185 ml | 2.37 ml |
| 5 mM | 0.047 ml | 0.237 ml | 0.474 ml |
Last Update：2024-01-02 23:10:35
Buspar hydrochloride - Differential diagnosis
Authoritative Data Verified Data
- take about 10 mg of this product, add 2ml of water to dissolve, and add 3 drops of ammonium molybdate test solution to generate white flocculent precipitate.
- take this product, add 0.1mol/L hydrochloric acid solution to dissolve and dilute to make a solution containing 10ug per lml, and measure it by UV-Vis spectrophotometry (General 0401), there is a maximum absorption at wavelengths of 214nm and 233nm.
- The infrared absorption spectrum of this product should be consistent with that of the reference product (General rule 0402).
- the aqueous solution of this product was chloride identification (1) of the reaction (General 0301).
Last Update：2022-01-01 14:20:05
Buspar hydrochloride - Exam
Authoritative Data Verified Data
Related substances
take this product, add water to dissolve and dilute to make each lml containing 0.1 mg of the solution was used as a test solution; An appropriate amount was taken in a precise amount and diluted quantitatively with water to prepare a solution containing 1 μg per 1 ml as a control solution. According to the test of high performance liquid chromatography (General rule 0512), silica gel bonded with eighteen alkyl silane was used as filler; Acetonitrile-phosphate buffer solution (1.36g of potassium dihydrogen phosphate, dissolved in water and diluted to 1000ml, the mobile phase was adjusted to pH 3.5 with phosphoric acid (30:70); The detection wavelength was 238nm. The theoretical plate number is not less than 3000 based on the buspirone peak. 20 u1 of the test solution and the control solution were respectively injected into the liquid chromatograph, and the chromatogram was 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 sum of each impurity peak area shall not be greater than or equal to
According to the main peak area of the solution (1.0%).
chlorine content
take about 0.4g of this product, weigh it accurately, add 50ml of water to dissolve, add 5ml of dextrin solution (1-50), calcium carbonate 0.lg and fluorescent yellow indicator solution 5~8 drops, with silver nitrate titration solution (0.lmol/L) titration to turbid liquid from yellow-green to reddish. Each 1 ml of silver nitrate titration solution (O. 1 mol/L) should be equivalent to 3.54mg of Cl. The chlorine content should be 8.0% to 8.8%.
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%.
Heavy metals
The residue left under the item of taking the ignition residue shall not contain more than 10 parts per million of heavy metal when examined by law (General Principles 0821, Law II).
Last Update：2022-01-01 14:20:06
Buspar hydrochloride - Content determination
Authoritative Data Verified Data
take about 0.15g of this product, precision weighing, add 20ml of glacial acetic acid and 5ml of Mercury acetate test solution, add 1 drop of crystal violet indicator solution, and use high gas acid titration solution (O. 1 mol/L) titration to the solution is green, and the titration result is corrected with blank test. Each 1 ml of perchloric acid titrant (0.1 mol/L) corresponds to 21.10 mg of C21H31N502. HCI.
Last Update：2022-01-01 14:20:06
Buspar hydrochloride - Category
Authoritative Data Verified Data
Anti-Anxiety drug.
Last Update：2022-01-01 14:20:06
Buspar hydrochloride - Storage
Authoritative Data Verified Data
light shielding, sealed storage.
Last Update：2022-01-01 14:20:06
Buspar hydrochloride - Buspirone Hydrochloride Tablets
Authoritative Data Verified Data
This product contains buspirone hydrochloride (C21H31N502 • HCI) should be 90.0% ~ 110.0% of the label amount.
trait
This product is white tablet.
identification
- take an appropriate amount of fine powder of this product (equivalent to 20mg of buspirone hydrochloride), put it in a test tube, add 5ml of water, shake to dissolve, filter, and take 2ml of filtrate, add 3 drops of ammonium molybdate solution, namely the formation of white flocculent precipitation.
- the sample solution under the content measurement item was taken and measured by ultraviolet-visible spectrophotometry (General 0401), and the maximum absorption was found at wavelengths of NM and Nm.
- The filtrate under identification (1) was taken to identify the reaction of (1) with chloride (General 0301).
examination
- Content uniformity take 1 tablet of this product, put it in a 50ml measuring flask, and add O. 1 mol/L hydrochloric acid solution appropriate amount, shake to dissolve buspirone hydrochloride and dilute to the scale, shake, filter. According to the method under the content determination item, the determination shall be carried out according to law from the "precise amount of filtrate 5ml, put in 50ml measuring flask", and shall comply with the regulations (General rule 0941)o
- dissolution of this product, according to the dissolution and release determination method (General 0931 second method), with 0.lmol/L hydrochloric acid solution 600ml as dissolution medium, rotating speed of 50 rpm, operated according to law, after 20 minutes, take 10ml of solution to filter, take the filtrate according to the method under the content determination item, from the "UV-visible spectrophotometry", the dissolution amount of each tablet was calculated according to the law. The limit is 75% 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 20 tablets of this product, precision weighing, fine grinding, precision weighing an appropriate amount (equivalent to buspirone hydrochloride 10 mg ), put it in a 100ml measuring flask, add 0.1 mol/L hydrochloric acid solution dissolved and diluted to the scale, shake, filter, precision take the remaining filtrate 5ml, 50ml flask, with 0. Dilute 1 mol/L hydrochloric acid solution to the scale, shake well, as the test solution, according to UV-visible spectrophotometry (General 0401), at the wavelength of 233nm absorbance; take an appropriate amount of buspirone hydrochloride reference, precision weighing, add 0.lmol/L hydrochloric acid solution dissolved and quantitatively diluted into 10% solution per lml, the same method of determination, calculation, that is.
category
with buspirone hydrochloride.
specification
5mg
storage
light shielding, sealed storage.
Last Update：2022-01-01 14:20:07
Buspar hydrochloride - Reference Information
| biological activity | Buspirone is a serotonin (5HT(1A) receptor agonist) anxiolytic drug with D(2) dopaminergic effect. |
| Target | Value |
Last Update：2024-04-09 20:49:11
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View History
Buspar hydrochloride
2-氨基-6-甲基-4,5,6,7-四氢-苯并噻吩-3-甲酸乙酯
SODIUM ANILINESULFONATE
ALPHA-BROMO-2-ACETYL NAPHTHALENE
2-氨基-6-甲基-4,5,6,7-四氢-苯并噻吩-3-甲酸乙酯
SODIUM ANILINESULFONATE
ALPHA-BROMO-2-ACETYL NAPHTHALENE