Buspirone Hydrochloride

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Cat Number

API33386082

CAS Number

33386-08-2

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CAS Number

33386-08-2

EINECS

251-489-4

Storage

2-8℃

Synonyms

8-[4-[4-(2-pyrimidinyl)-1-piperazin-1-iumyl]butyl]-8-azaspiro[4.5]decane-7,9-dione

Molecular Formula

C21H32ClN5O2

Molecular Weight

421.96

Smiles

C1CCC2(C1)CC(=O)N(C(=O)C2)CCCCN3CCN(CC3)C4=NC=CC=N4.Cl

Appearance

White to off-white solid

Melting Point

201.5-202.5℃

General Description

Buspirone Hydrochloride is a serotonin 5-HT1A receptor partial agonist anxiolytic used for the treatment of generalized anxiety disorder (GAD). Unlike benzodiazepines and barbiturates, it does not exert significant sedative, muscle relaxant, or anticonvulsant effects, and has negligible abuse potential. Its novel mechanism of action differentiates it from traditional anxiolytic drug classes and provides a favorable safety profile.

Mechanism of Action

Buspirone Hydrochloride acts as a partial agonist at presynaptic and postsynaptic serotonin 5-HT1A receptors. Presynaptic 5-HT1A autoreceptor activation leads to decreased serotonergic neuron firing and reduced serotonin release, while postsynaptic 5-HT1A agonism in limbic and cortical regions mediates anxiolytic effects. The delayed onset of action (typically 2-4 weeks) reflects the downstream modulation of second-messenger systems including adenylate cyclase inhibition and gene expression changes.

Application

Buspirone Hydrochloride is indicated for the treatment of generalized anxiety disorder (GAD) in adults. It is particularly valued for its non-sedating profile, making it suitable for patients who require anxiolytic therapy without cognitive or psychomotor impairment. Its absence of withdrawal potential and lack of cross-tolerance with benzodiazepines or alcohol make it a preferred choice in patients with substance use histories.

Buspirone hydrochloride (BUH), an anxiolytic agent for general anxiety disorder, suffers from extensive first-pass metabolism (only 5% oral bioavailability). To overcome this, thiolated chitosan nanoparticles (TCS-NPs) were developed for intranasal brain delivery. TCS-NPs were prepared by ionic gelation, showing particle size 226.7 nm, PDI 0.483, entrapment efficiency 81.13%, and loading capacity 49.67%. Ex vivo permeation through nasal mucosa reached 76.21%, significantly higher than BUH solution (20.97%). Porcine mucin binding efficiency was 90.22%, demonstrating strong bioadhesion.
Drug targeting efficiency (78.94%) and direct transport percentage (95.97%) confirmed direct nose-to-brain transport bypassing the blood-brain barrier. Pharmacodynamic studies using elevated plus maze showed increased open arm residence time, confirming anxiolytic effect. TCS-NPs provide a promising non-invasive strategy for brain delivery of BUH.

References

Bari N K, et al. Brain delivery of buspirone hydrochloride chitosan nanoparticles for the treatment of general anxiety disorder. International journal of biological macromolecules, 2015, 81: 49-59.

What is the recommended storage condition for Buspirone Hydrochloride?

It should be stored at 2-8°C in a well-sealed container, protected from moisture and direct light, to maintain its chemical integrity throughout the shelf life.

Can we obtain batch-specific analytical data for Buspirone Hydrochloride?

Batch-specific COA documents are standard with every shipment. Additional analytical reports, including HPLC chromatograms or spectral data, may be provided upon request.

What quantities of Buspirone Hydrochloride are available for order?

We accommodate orders of varying scale, from small research quantities through bulk commercial supply. Contact our sales team to discuss pack sizes and volume pricing.

What is the standard particle size of Buspirone Hydrochloride supplied?

Standard commercial grades are supplied; custom particle size specifications are available upon request for specific formulation needs.