Buspirone
- CAS No.
- 36505-84-7
- Chemical Name:
- Buspirone
- Synonyms
- BUSPIRONE HCL;buspar;8-[4-[4-(2-PYRIMIDINYL)-1-PIPERAZINYL]BUTYL]-8-AZASPIRO[4,5]DECANE-7,9-DIONE;Buspisal;Buspimen;BUSPIRONE;Nard：Tmvin;BUPROPIONHCL;BUSPIRONE,USP;Ansiced：Axoren
- CBNumber:
- CB1367137
- Molecular Formula:
- C21H31N5O2
- Molecular Weight:
- 385.5
- MDL Number:
- MFCD00243004
- MOL File:
- 36505-84-7.mol
- MSDS File:
- SDS
| 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 |
| pka | pKa 7.60±0.01(H2O t=25.0 I=0.1(NaCl)) (Uncertain) |
| form | Solid |
| color | White to off-white |
| BCS Class | 1 |
| CAS DataBase Reference | 36505-84-7(CAS DataBase Reference) |
| NCI Dictionary of Cancer Terms | buspirone |
| FDA UNII | TK65WKS8HL |
| NCI Drug Dictionary | Buspar |
| ATC code | N05BE01 |
| NIST Chemistry Reference | 8-Azaspiro[4.5]decane-7,9-dione, 8-[4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl]-(36505-84-7) |
| EPA Substance Registry System | 8-Azaspiro[4.5]decane-7,9-dione, 8-[4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl]- (36505-84-7) |
Buspirone price More Price(7)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| TRC | B689855 | Buspirone | 36505-84-7 | 100mg | $65 | 2021-12-16 | Buy |
| TRC | C371285 | 5-ChloroBuspirone | 36505-84-7 | 10mg | $255 | 2021-12-16 | Buy |
| American Custom Chemicals Corporation | INB0000487 | BUSPIRONE 95.00% | 36505-84-7 | 5MG | $504.94 | 2021-12-16 | Buy |
| American Custom Chemicals Corporation | INB0000487 | BUSPIRONE 95.00% | 36505-84-7 | 1G | $2344.65 | 2021-12-16 | Buy |
| AHH | MT-46118 | 8-[4-[4-(2-Pyrimidinyl)-1-piperazinyl]butyl]-8-azaspiro[4,5]decane-7,9-dione 98% | 36505-84-7 | 0.1g | $680 | 2021-12-16 | Buy |
Buspirone Chemical Properties,Uses,Production
Uses
Tranquilizer (minor).
Uses
5-Chloro Buspirone is an impurity of Buspirone Hydrochloride (B689850), a non-benzodiazepine anxiolytic and a 5-hydroxytryptamine (5-HT1) receptor agonist.
Uses
Buspirone 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.
Definition
ChEBI: 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 name
Buspar (Bristol-Myers Squibb).
Biological Functions
Buspirone (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 Description
The 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 action
Although 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.
Pharmacology
Buspirone 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 Use
Buspirone is effective in general anxiety and in anxiety with depression.
Side effects
Like 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.
Synthesis
Buspirone, 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¨C55].
Metabolism
Buspirone 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.
Buspirone Preparation Products And Raw materials
Raw materials
1of4
Preparation Products
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| Hebei Mojin Biotechnology Co., Ltd | +86 13288715578 +8613288715578 | sales@hbmojin.com | China | 12833 | 58 |
| Hangzhou Hyper Chemicals Limited | +86-0086-57187702781 +8613675893055 | info@hyper-chem.com | China | 295 | 58 |
| Henan Tianfu Chemical Co.,Ltd. | +86-0371-55170693 +86-19937530512 | info@tianfuchem.com | China | 21634 | 55 |
| career henan chemical co | +86-0371-86658258 +8613203830695 | sales@coreychem.com | China | 29880 | 58 |
| CONIER CHEM AND PHARMA LIMITED | +8618523575427 | sales@conier.com | China | 49374 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 32161 | 58 |
| Xi'an MC Biotech, Co., Ltd. | 029-89275612 +8618991951683 | mcbio_sales@163.com | China | 2251 | 58 |
| Dorne Chemical Technology co. LTD | +86-86-13583358881 +8618560316533 | Ethan@dornechem.com | China | 3095 | 58 |
| Dideu Industries Group Limited | +86-29-89586680 +86-15129568250 | 1026@dideu.com | China | 22787 | 58 |
| Finetech Industry Limited | +86-27-87465837 +8618971612321 | info@finetechnology-ind.com | China | 9639 | 58 |
Related articles
- Buspirone: Pharmacokinetics,side effects and mechanism of action
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- Oct 12，2019
View Lastest Price from Buspirone manufacturers
| Image | Update time | Product | Price | Min. Order | Purity | Supply Ability | Manufacturer | |
|---|---|---|---|---|---|---|---|---|
 |
2024-11-19 | Buspirone
36505-84-7
|
US $30.00-79.00 / mg | 99.95% | 10g | TargetMol Chemicals Inc. | ||
 |
2024-11-01 | Buspirone
36505-84-7
|
US $0.00-0.00 / KG | 1KG | 98% | 1000KG | Hangzhou Hyper Chemicals Limited | |
 |
2024-03-29 | Buspirone
36505-84-7
|
US $0.00 / KG | 1KG | 99% | 50000KG/month | Hebei Mojin Biotechnology Co., Ltd |