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Buspirone

Buspirone Structure
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
MOL File:
36505-84-7.mol
MSDS File:
SDS
Modify Date:
2024/11/15 19:19:13

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. 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)
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

Symbol(GHS) 
GHS06
Signal word  Danger
Hazard statements  H301
Precautionary statements  P264-P270-P301+P310-P321-P330-P405-P501
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

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.

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.

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Buspirone Spectrum

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 Buspisal Nard:Tmvin BUSPIRONE Buspirone Impurity 5-Chloro Buspirone Buspirone EP Impurity D Hydrochloride 8-[4-(4-pyrimidin-2-ylpiperazin-1-yl)butyl]-8-azaspiro[4.5]decane-7,9-dione 8-[4-(4-pyrimidin-2-ylpiperazin-1-yl)butyl]-8-azaspiro[4.5]decane-7,9-quinone 8-Azaspiro[4.5]decane-7,9-dione,8-[4-[4-(2-pyriMidinyl)-1-piperazinyl]butyl]- Buspirone for system suitability CRS Buspirone USP/EP/BP 36505-84-7 Buspirone Buspirone free base 8-[4-[4-(2-PYRIMIDINYL)-1-PIPERAZINYL]BUTYL]-8-AZASPIRO[4,5]DECANE-7,9-DIONE buspar BUSPIRONE HCL 5-HT Receptor,inhibit,5-hydroxytryptamine Receptor,Serotonin Receptor,Reactive Oxygen Species,anxiety,Buspirone,Inhibitor,depression,5-HT1A receptor Refametinib Impurity 5 36505-84-7 C21H31N5O2