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Buspirone hydrochloride

Buspirone hydrochloride Structure
Buspirone hydrochloride
  • CAS No.33386-08-2
  • Chemical Name:Buspirone hydrochloride
  • CBNumber:CB8367136
  • Molecular Formula:C21H32ClN5O2
  • Formula Weight:421.96
  • MOL File:33386-08-2.mol
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)
  • FDA UNII 207LT9J9OC
  • NCI Drug Dictionary buspirone hydrochloride
  • UNSPSC Code 41116107
  • NACRES NA.77
Safety
Hazard and Precautionary Statements (GHS)
  • Symbol(GHS)
  • Signal wordDanger
  • Hazard statements H301
  • Precautionary statements P264-P270-P301+P310-P405-P501
Buspirone hydrochloride Price More Price(4)
  • Brand: Sigma-Aldrich(India)
  • Product number: B7148
  • Product name : Buspirone hydrochloride
  • Purity: 
  • Packaging: 1G
  • Price: ₹8356.9
  • Updated: 2022/06/14
  • Buy: Buy
  • Brand: Sigma-Aldrich(India)
  • Product number: PHR1917
  • Product name : Buspirone hydrochloride
  • Purity: Pharmaceutical Secondary Standard; Certified Reference Material
  • Packaging: 500MG
  • Price: ₹31652.3
  • Updated: 2022/06/14
  • Buy: Buy
  • Brand: Sigma-Aldrich(India)
  • Product number: B7148
  • Product name : Buspirone hydrochloride
  • Purity: 
  • Packaging: 5G
  • Price: ₹27495.5
  • Updated: 2022/06/14
  • Buy: Buy
  • Brand: Sigma-Aldrich(India)
  • 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: ₹9323.3
  • Updated: 2022/06/14
  • Buy: Buy

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 anxiolitic;serotonin receptor agonist
  • Uses Non-benzodiazepine anxiolitic; 5-hydroxytryptamine (5-HT1) 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
Preparation Products
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Buspirone hydrochloride Spectrum
33386-08-2, Buspirone hydrochlorideRelated Search:
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  • Buspirone HydrochlorideQ: What is Buspirone Hydrochloride Q: What is the CAS Number of Buspirone Hydrochloride Q: What is the storage condition of Buspirone Hydrochloride Q: What are the applications of Buspirone Hydrochloride
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