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Buspirone hydrochloride

Product Name
Buspirone hydrochloride
CAS No.
33386-08-2
Chemical Name
Buspirone hydrochloride
Synonyms
BUSPIRONE HCL;Narol;bespar;axoren;travin;Ansial;censpar;lucelan;Ansiced;buspinol
CBNumber
CB8367136
Molecular Formula
C21H32ClN5O2
Formula Weight
421.96
MOL File
33386-08-2.mol
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Buspirone hydrochloride Property

Melting point:
201.5-202.50C
Flash point:
9℃
storage temp. 
2-8°C
solubility 
Freely soluble in water and in methanol, practically insoluble in acetone.
form 
Solid
color 
White to off-white
Water Solubility 
Soluble in methanol (50 mg/ml), water (partly), DMSO (100 mM).
CAS DataBase Reference
33386-08-2(CAS DataBase Reference)
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Safety

Hazard Codes 
T,Xn,F
Risk Statements 
25-36/37/38-20/21/22-39/23/24/25-23/24/25-11
Safety Statements 
45-36-26-36/37-16
RIDADR 
UN 2811 6.1/PG 3
WGK Germany 
3
RTECS 
CL9915000
HazardClass 
6.1
HS Code 
29335995
Toxicity
LD50 i.p. in rats: 136 mg/kg (Allen)
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Danger
Hazard statements

H301Toxic if swalloed

Precautionary statements

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P301+P310IF SWALLOWED: Immediately call a POISON CENTER or doctor/physician.

P405Store locked up.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
B-054
Product name
Buspirone hydrochloride solution
Purity
1.0?mg/mL in methanol (as free base), ampule of 1?mL, certified reference material, Cerilliant?
Packaging
1mL
Price
$79.4
Updated
2024/03/01
Sigma-Aldrich
Product number
1078802
Product name
Buspirone hydrochloride
Purity
United States Pharmacopeia (USP) Reference Standard
Packaging
200mg
Price
$400
Updated
2024/03/01
Alfa Aesar
Product number
J60476
Product name
Buspirone hydrochloride
Packaging
1g
Price
$52.65
Updated
2024/03/01
Alfa Aesar
Product number
J60476
Product name
Buspirone hydrochloride
Packaging
5g
Price
$191.65
Updated
2024/03/01
Cayman Chemical
Product number
22028
Product name
Buspirone (hydrochloride)
Purity
≥98%
Packaging
1mg
Price
$57
Updated
2024/03/01
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Buspirone hydrochloride Chemical Properties,Usage,Production

Description

Buspirone hydrochloride is an anxiolytic agent indicated for the management of anxiety disorders with or without accompanying depression. In contrast to the benzodiazepines, buspirone does not interact with alcohol, and lacks sedative, anticonvulsant, and muscle relaxant effects, and abuse potential.

Chemical Properties

White Solid

Originator

Mead Johnson (USA)

Uses

Non-benzodiazepine anxiolitic; 5-hydroxytryptamine (5-HT1) receptor agonist.

Uses

anxiolitic;serotonin receptor agonist

Uses

Non-benzodiazepine anxiolytic; 5-hydroxytryptamine (5-HT1) receptor agonist.

Definition

ChEBI: A hydrochloride salt resulting from the reaction of equimolar amounts of buspirone and hydrogen chloride.

Manufacturing Process

There is the 3 methods for preparing of 8-azaspiro(4.5)decane-7,9-dione, 8- (4-(4-(2-pyrimidinyl)-1-piperazinyl)butyl) monohydrochloride (U.S. Patent 3,717,634). One of them is follows: a mixture of 0.1 mole of the substituted glutaric anhydride, 0.1 mole of l-(4-aminobutyl)-4-(2-pyrimidinyl)piperazine (U.S. Pat. 3,398151), and 300 ml of pyridine was refluxed until imide formation was completed. The degree of reaction was readily followed by taking an aliquot portion of the reaction mixture, removing the solvent, and obtaining the infrared absorption spectrum of the residue. When reaction is complete, the spectrum exhibited typical infrared imide bands at 1701 and 1710 cm-1 whereas if incomplete, the infrared spectrum contains amide and carboxyl absorption bands at 1680, 1760 and 3300 cm-1.
1-(3-Cyanopropyl)-4-(2-pyrimidinyl)-piperazine. A mixture of 1-(2- pyrimidinyl)piperazine (6.0 g, 0.04 mole), 4.6 g (0.044 mole) of 3- chloropropionitrile and sodium carbonate (4.24 g, 0.04 mole) in 50 ml of nbutanol was gently refluxed for 16 hours. The reaction mixture was concentrated in vacuo and the residual oil dissolved in about 100 ml of cyclohexane. On standing a white crystalline material separated which was crystallized from cyclohexane to provide 6.5 g (yield 70%) of the cyano intermediate, m.p. 56.6-58°C. A solution of 11.5 g (0.05 mole) of 1-(3- cyanopropyl)-4-(2-pyrimidinyl)piperazine in 150 ml of absolute ethanol was saturated with ammonia. W-6 Raney nickel catalyst was added and the mixture hydrogenated under 1200 p.s.i. When the hydrogenation was completed the mixture was filtered and the residual oil distilled under reduced pressure to provide 8.2 g (70% ) of 1-(4-aminobutyl)-4-(2- pyrimidinyl)piperazine, b.p. 143-146°C at 0.1 mm. (nD 26 = 1.5582).
The azospiroalkenedione 8-[4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl]-8- azaspiro[4.5]decane-7,9-dione was purified as free base by stripping off the pyridine solvent and crystallizing the residue from a suitable solvent or by vacuum distillation thereof hydrochloric salt of it was prepared by treating of an ethanol solution of free base with equimolar amount of HCl.

brand name

Buspar (Bristol-Myers Squibb);BESPAR.

Therapeutic Function

Anxiolytic

General Description

Pharmaceutical secondary standards for application in quality control provide pharma laboratories and manufacturers with a convenient and cost-effective alternative to the preparation of in-house working standards

Biological Activity

Classic 5-HT 1A partial agonist with relatively high affinity (K i = 9.3 - 29.5 nM). A clinically effective anxiolytic.

Biochem/physiol Actions

5-HT1A serotonin receptor agonist; anxiolytic.

Clinical Use

Anxiolytic

Veterinary Drugs and Treatments

Buspirone may be effective in treating certain behavior disorders in dogs and cats, principally those that are fear/phobia related and especially those associated with social interactions. Buspirone may also be useful for urine spraying or treatment of motion sickness in cats.

Drug interactions

Potentially hazardous interactions with other drugs
Antibacterials: concentration increased by erythromycin - reduce dose; concentration reduced by rifampicin.
Antidepressants: avoid with tranylcypromine; risk of severe hypertension with MAOIs - avoid.
Antifungals: concentration increased by itraconazole - reduce dose.
Antipsychotics: enhanced sedative effects; haloperidol concentration increased.
Antivirals: concentration increased by ritonavir, increased risk of toxicity.
Calcium-channel blockers: concentration increased by diltiazem and verapamil - reduce dose.
Grapefruit juice: concentration increased by grapefruit juice - reduce dose.
Methylthioninium: possible risk of CNS toxicity - avoid if possible.

Metabolism

Systemic bioavailability of buspirone is low because of extensive first-pass metabolism. Metabolism in the liver is extensive via the cytochrome P450 isoenzyme CYP3A4; hydroxylation yields several inactive metabolites and oxidative dealkylation produces 1-(2-pyrimidinyl)- piperazine, which is reported to be about 25% as potent as the parent drug in one model of anxiolytic activity. Buspirone is excreted mainly as metabolites in the urine, and also the faeces.

storage

+4°C (desiccate)

Buspirone hydrochloride Preparation Products And Raw materials

Raw materials

3,3-Tetramethyleneglutarimide N,N-Dimethylformamide Piperazine 2-Chloropyrimidine Hydrochloric acid 1,4-Dibromobutane Dichloromethane Methanol Sodium hydroxide Isopropyl alcohol Sodium carbonate

Preparation Products

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Buspirone hydrochloride Suppliers

Belgium 2 Brazil 2 Canada 2 China 185 Czech Republic 1 Egypt 1 Europe 2 Finland 1 France 3 Germany 5 Hungary 1 India 23 Italy 1 South Korea 1 Switzerland 2 United Kingdom 12 United States 33 Global 277
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View Lastest Price from Buspirone hydrochloride manufacturers

WUHAN FORTUNA CHEMICAL CO., LTD
Product
Buspirone hydrochloride 33386-08-2
Price
US $0.00-0.00/Kg/Drum
Min. Order
1KG
Purity
98.5%min
Supply Ability
100KGS
Release date
2021-07-09
Hebei Yanxi Chemical Co., Ltd.
Product
Buspirone hydrochloride 33386-08-2
Price
US $40.00/kg
Min. Order
1kg
Purity
0.99
Supply Ability
10 tons
Release date
2023-09-06
Wuhan Senwayer Century Chemical Co.,Ltd
Product
Buspirone hydrochloride 33386-08-2
Price
US $780.00/KG
Min. Order
1KG
Purity
99% HPLC
Supply Ability
20 TONS
Release date
2022-10-13

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