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Buspirone HCl 5-HT Receptor agonist

Cat.No.S4256

Buspirone(Buspirone hydrochloride) is a serotonergic (5HT(1A) receptor agonist) anxiolytic drug with some D(2) dopaminergic effect, used for anxiety disorders.
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Quality Control

Batch: S425601 DMSO]84 mg/mL]false]Water]84 mg/mL]false]Ethanol]36 mg/mL]false Purity: 99.99%
99.99

Solubility

In vitro
Batch:

DMSO : 84 mg/mL (199.07 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 84 mg/mL

Ethanol : 36 mg/mL

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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Chemical Information, Storage & Stability

Molecular Weight 421.96 Formula

C21H31N5O2.HCl

Storage (From the date of receipt)
CAS No. 33386-08-2 Download SDF Storage of Stock Solutions

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

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Mechanism of Action

Targets/IC50/Ki
5-HT1A
In vitro

Buspirone, a clinically effective non-benzodiazepine anxiolytic drug, causes inhibition of firing of these neurons when given by intravenous (ED50 = 0.011 mg/kg, i.v.), intraperitoneal (ED50 = 0.088 mg/kg, i.p.), and intragastric (effective dose = 1.0-20.0 mg/kg, i.g.) injection. Buspirone also inhibits these cells when it is administered to the outside of recorded neurons by microiontophoresis. Buspirone is eliminated primarily by oxidative metabolism, which produces several hydroxylated metabolites, including 5-hydroxy-buspirone and 1-pyrimidinylpiperazine.

In vivo

Buspirone (3 mg/rat, i.p.) dose dependently and completely inhibits shock-induced ultrasonic vocalization after systemic injection and after microinjection into the dorsal raphe nucleus of rats, a brain region rich in somatodendritic 5-HT1A receptors. Buspirone (20 mg/kg) decreases immobility in the rat forced swim test. Buspirone is a serotonergic (5HT(1A) receptor agonist) anxiolytic drug with some D(2) dopaminergic effect in a zebrafish model of anxiety. Buspirone dose-dependently reduces LID and improved l-DOPA-related motor performance due to action at the 5-HT(1A) receptor in l-DOPA-primed rats. Buspirone delayes LID development while improving l-DOPA's anti-parkinsonian efficacy indicating the potential long-term benefits of 5-HT(1A) agonists for reduction of l-DOPA-related side effects in l-DOPA-naive rats.

References
  • [4] https://pubmed.ncbi.nlm.nih.gov/19643124/
  • [5] https://pubmed.ncbi.nlm.nih.gov/17553556/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2026-09-04)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT07439042 NOT_YET_RECRUITING
Anxiety; Autism Spectrum Disorder
Massachusetts General Hospital
2026-09 PHASE4
NCT04400266 RECRUITING
Depression; Brain Injuries, Traumatic
Massachusetts General Hospital
2020-08-01 PHASE4
NCT05511909 RECRUITING
Opioid Use Disorder; Opioid Withdrawal; Opioid Craving; Anxiety
University of Maryland, Baltimore
2022-12-15 PHASE2
NCT04118387 RECRUITING
Sleep Disordered Breathing; Able Bodied
VA Office of Research and Development
2021-01-07 PHASE4
NCT03954483 RECRUITING
Anxiety
University of Manitoba
2023-10-16
NCT04458324 ACTIVE_NOT_RECRUITING
Spinal Cord Injuries
Spaulding Rehabilitation Hospital
2020-12-22 PHASE2

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