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 |
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. |
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) |
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.
The melting point of this product (General 0612) is 202~206°C.
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 |
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%).
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%.
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 10 parts per million of heavy metal when examined by law (General Principles 0821, Law II).
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.
Anti-Anxiety drug.
light shielding, sealed storage.
This product contains buspirone hydrochloride (C21H31N502 • HCI) should be 90.0% ~ 110.0% of the label amount.
This product is white tablet.
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.
with buspirone hydrochloride.
5mg
light shielding, sealed storage.
biological activity | Buspirone is a serotonin (5HT(1A) receptor agonist) anxiolytic drug with D(2) dopaminergic effect. |
Target | Value |