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Buspirone

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CAS:36505-84-7
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CAS:36505-84-7
Package:1 mg;10 mg;100 mg;200 mg;25 mg;5 mg;50 mg Remarks:REAGENT;FOR LABORATORY USE ONLY

Buspirone manufacturers

  • Buspirone USP/EP/BP
  • $1.10 / 1g
  • 2021-07-23
  • CAS:36505-84-7
  • Min. Order: 1g
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  • Buspirone
  • $7.00 / 1KG
  • 2019-09-02
  • CAS:36505-84-7
  • Min. Order: 1KG
  • Purity: 99%
  • Supply Ability: JD 646
  • Buspirone
  • $7.00 / 1KG
  • 2019-09-02
  • CAS:36505-84-7
  • Min. Order: 1KG
  • Purity: 99%
  • Supply Ability: JD 580

Related articles

Buspirone Basic information
Product Name:Buspirone
Synonyms:8-[4-[4-(2-PYRIMIDINYL)-1-PIPERAZINYL]BUTYL]-8-AZASPIRO[4,5]DECANE-7,9-DIONE HYDROCHLORIDE;5)decane-7,9-dione,8-(4-(4-(2-pyrimidinyl)piperizinyl)butyl)-8-azaspiro(;8-(4-(4-(2-pyrimidinyl)-1-piperizinyl)butyl)-8-azaspiro(4,5)decane-7,9-dione;BUSPIRONE,USP;Buspirone (base and/or unspecified salts);BUPROPIONHCL;Ansiced:Axoren;Buspimen
CAS:36505-84-7
MF:C21H31N5O2
MW:385.5
EINECS:253-072-2
Product Categories:
Mol File:36505-84-7.mol
Buspirone Structure
Buspirone Chemical Properties
Melting point 105-107 °C(Solv: ethyl acetate (141-78-6))
Boiling point 511.93°C (rough estimate)
density 1.1527 (rough estimate)
refractive index 1.7600 (estimate)
storage temp. Sealed in dry,2-8°C
pkapKa 7.60±0.01(H2O t=25.0 I=0.1(NaCl)) (Uncertain)
CAS DataBase Reference36505-84-7(CAS DataBase Reference)
NIST Chemistry Reference8-Azaspiro[4.5]decane-7,9-dione, 8-[4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl]-(36505-84-7)
EPA Substance Registry System8-Azaspiro[4.5]decane-7,9-dione, 8-[4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl]- (36505-84-7)
Safety Information
Hazard Codes T
Risk Statements 25
Safety Statements 45
RIDADR UN 2811 6.1/PG 3
WGK Germany 3
RTECS CL9915000
MSDS Information
ProviderLanguage
SigmaAldrich English
Buspirone Usage And Synthesis
UsesTranquilizer (minor).
Uses5-Chloro Buspirone is an impurity of Buspirone Hydrochloride (B689850), a non-benzodiazepine anxiolytic and a 5-hydroxytryptamine (5-HT1) receptor agonist.
UsesBuspirone is an extremely specific drug that could possibly represent a new chemical class of anxiolytics—azaspirones. As an anxiolytic, its activity is equal to that of benzodiazepines; however, it is devoid of anticonvulsant and muscle relaxant properties, which are characteristic of benzodiazepines.
DefinitionChEBI: An azaspiro compound that is 8-azaspiro[4.5]decane-7,9-dione substituted at the nitrogen atom by a 4-(piperazin-1-yl)butyl group which in turn is substituted by a pyrimidin-2-yl group at the N4 position.
Brand nameBuspar (Bristol-Myers Squibb).
Biological FunctionsBuspirone (BuSpar) is the first example of a class of anxiolytic agents that can relieve some symptoms of anxiety in doses that do not cause sedation. Buspirone is structurally unrelated to existing psychotropic drugs.
General DescriptionThe initial compound in this series, buspirone (BuSpar), hasanxiolytic and antidepressant activities and is a partial5-HT1A agonist. Its anxiolytic activity is reportedly causedby its ability to diminish 5-HT release (via 5-HT1A agonism).High short-term synaptic levels of 5-HT are characteristic ofanxiety. Also, because it is a partial agonist, it can stimulatepostsynaptic receptors when 5-HT levels are low in thesynapse, as is the case in depression. Several other spironesare in development as anxiolytics and antidepressants.
Mechanism of actionAlthough buspirone has been shown to interact with a number of neurotransmitter systems in the brain, it appears that its clinically relevant effects are mediated through interactions at the serotonin (5-hydroxytryptamine, 5-HT) 5-HT1A receptor, where it acts as a partial agonist.
PharmacologyBuspirone is as effective as the benzodiazepines in the treatment of general anxiety. However, the full anxiolytic effect of buspirone takes several weeks to develop, whereas the anxiolytic effect of the benzodiazepines is maximal after a few days of therapy. In therapeutic doses, buspirone has little or no sedative effect and lacks the muscle relaxant and anticonvulsant properties of the benzodiazepines. In addition, buspirone does not potentiate the central nervous system depression caused by sedative–hypnotic drugs or by alcohol, and it does not prevent the symptoms associated with benzodiazepine withdrawal.
Clinical UseBuspirone is effective in general anxiety and in anxiety with depression.
Side effectsLike the benzodiazepines, buspirone appears to be safe even when given in very high doses. The most common side effects are dizziness, light-headedness, and headache. Abuse, dependence, and withdrawal have not been reported, and buspirone administration does not produce any cross-tolerance to the benzodiazepines. Buspirone has been reported to increase blood pressure in patients taking monoamine oxidase inhibitors, and it may increase plasma levels of haloperidol if coadministered with that agent.
SynthesisBuspirone, 8-[4-[4-(2-pyrimidyl)-1-piperazinyl]butyl]-8-azaspiro [4,5] decan-7,9-dione (5.2.6), is synthesized by the reaction of 1-(2-pyrimidyl)-4- (4-aminobutyl)piperazine (5.2.4) with 8-oxaspiro[4,5]decan-7,9-dione (5.2.5). In turn, 1- (2-pyrimidyl)-4-(4-aminobutyl)piperazine (5.2.4) is synthesized by the reaction of 1-(2-pyrimidyl)piperazine with 4-chlorobutyronitrile, giving 4-(2-pyrimidyl)-1-(3- cyanopropyl)piperazine (5.2.3), which is hydrogenated with Raney nickel into buspirone (5.2.4) [51–55].

MetabolismBuspirone is well absorbed from the gastrointestinal tract, and peak blood levels are achieved in 1 to 1.5 hours; the drug is more than 95% bound to plasma proteins. Buspirone is extensively metabolized, with less than 1% of the parent drug excreted into the urine unchanged. At least one of the metabolic products of buspirone is biologically active. The parent drug has an elimination half-life of 4 to 6 hours.
Tag:Buspirone(36505-84-7) Related Product Information
Piperazine Butyl acetate Decane tert-Butanol 2-Butoxyethanol Bromophenol Red Buspirone 1-Methylpiperazine Homopiperazine Buspirone Hydrochlorid,BUSPIRONE HCL,BUSPIRONE HYDROCHLORIDE Piperacillin 2-Ethylhexyl ferulate N-Aminoethylpiperazine Buprofezin BUSPIRONE FOR SYSTEM SUITABILITY 6-Hydroxy Buspirone-d8 BUSPIRONE HYDROCHLORIDE IMP. K (EP): 8-AZASPIRO[4,5]-DECANE-7,9-DIONE BUSPIRONE (D8),BUSPIRONE-D8 HCL (BUTYL-D8),Buspirone-d8 Hydrochloride,Buspirone-d8 HCl