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Buspirone

Buspirone
Buspirone structure
CAS No.
36505-84-7
Chemical Name:
Buspirone
Synonyms
buspar;Buspisal;Buspimen;BUSPIRONE;Nard:Tmvin;BUPROPIONHCL;BUSPIRONE,USP;BUSPIRONE HCL;Ansiced:Axoren;Buspirone Impurity
CBNumber:
CB1367137
Molecular Formula:
C21H31N5O2
Formula Weight:
385.5
MOL File:
36505-84-7.mol

Buspirone 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. 
2-8°C
pka
pKa 7.60±0.01(H2O t=25.0 I=0.1(NaCl)) (Uncertain)
CAS DataBase Reference
36505-84-7(CAS DataBase Reference)
FDA UNII
TK65WKS8HL
NCI Dictionary of Cancer Terms
buspirone
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)
SAFETY
  • Risk and Safety Statements
Hazard Codes  T
Risk Statements  25
Safety Statements  45
RIDADR  UN 2811 6.1/PG 3
WGK Germany  3
RTECS  CL9915000

Buspirone Chemical Properties,Uses,Production

Uses

Tranquilizer (minor).

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.

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

Preparation Products


Buspirone Suppliers

Global( 85)Suppliers
Supplier Tel Fax Email Country ProdList Advantage
career henan chemical co
+86-371-86658258
sales@coreychem.com CHINA 30039 58
BOC Sciences
1-631-619-7922 1-631-619-7922
1-631-614-7828 inquiry@bocsci.com United States 20039 58
HENAN BON INDUSTRIAL CO.,LTD
0371-55170695
info@hnbon.com CHINA 20535 58
CONIER CHEM AND PHARMA LIMITED
86-18523575427
sales@conier.com CHINA 47486 58
Amadis Chemical Company Limited
0086-571-89925085
0086-571-89925065 sales@amadischem.com China 132149 58
Mainchem Co., Ltd. +86-0592-6210733
+86-0592-6210733 sale@mainchem.com CHINA 32444 55
Chemwill Asia Co.,Ltd. 86-21-51086038
86-21-51861608 chemwill_asia@126.com;sales@chemwill.com;chemwill@hotmail.com;chemwill@gmail.com CHINA 23977 58
J & K SCIENTIFIC LTD. 400-666-7788 010-82848833-
86-10-82849933 jkinfo@jkchemical.com;market6@jkchemical.com China 96815 76
3B Pharmachem (Wuhan) International Co.,Ltd. 18930552037 821-50328103-801
86-21-50328109 3bsc@sina.com China 15880 69
LGM Pharma 1-(800)-881-8210
615-250-9817 inquiries@lgmpharma.com United States 1938 70

Related articles


View Lastest Price from Buspirone manufacturers

Image Release date Product Price Min. Order Purity Supply Ability Manufacturer
2019-09-01 Buspirone
36505-84-7
US $7.00 / KG 1KG 99% JD 646 career henan chemical co
2019-09-01 Buspirone
36505-84-7
US $7.00 / KG 1KG 99% JD 580 career henan chemical co

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