Buspirone HCl

Catalog No.S4256

For research use only.

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

Buspirone HCl Chemical Structure

CAS No. 33386-08-2

Selleck's Buspirone HCl has been cited by 1 Publication

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Biological Activity

Description Buspirone is a serotonergic (5HT(1A) receptor agonist) anxiolytic drug with some D(2) dopaminergic effect, used for anxiety disorders.
Targets
5-HT1A [1]
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. [1] Buspirone is eliminated primarily by oxidative metabolism, which produces several hydroxylated metabolites, including 5-hydroxy-buspirone and 1-pyrimidinylpiperazine. [2]

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. [3] Buspirone (20 mg/kg) decreases immobility in the rat forced swim test. [4] Buspirone is a serotonergic (5HT(1A) receptor agonist) anxiolytic drug with some D(2) dopaminergic effect in a zebrafish model of anxiety. [5] 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. [6]

Protocol (from reference)

Solubility (25°C)

In vitro

DMSO 84 mg/mL
(199.07 mM)
Water 84 mg/mL
(199.07 mM)
Ethanol 36 mg/mL
(85.31 mM)

Chemical Information

Molecular Weight 421.96
Formula

C21H31N5O2.HCl

CAS No. 33386-08-2
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1CCC2(C1)CC(=O)N(C(=O)C2)CCCCN3CCN(CC3)C4=NC=CC=N4.Cl

In vivo Formulation Calculator (Clear solution)

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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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03444831 Completed Drug: Buspirone|Drug: Placebo Oral Tablet Dyspepsia Isfahan University of Medical Sciences March 1 2016 Phase 4
NCT02483598 Terminated Drug: Buspirone|Drug: Buspirone and Grapefruit Juice Gastric Bypass North Dakota State University|Neuropsychiatric Research Institute Fargo North Dakota June 2015 Phase 4
NCT01699828 Completed Drug: Buspirone|Drug: Placebo Smoking Cessation|Tobacco Use Cessation Centre for Addiction and Mental Health October 2012 Phase 1|Phase 2
NCT01496612 Terminated Drug: Buspirone|Drug: Placebo Anxiety Disorder|Seizures|Epilepsy|Partial Epilepsy|Depression National Institute of Neurological Disorders and Stroke (NINDS)|National Institutes of Health Clinical Center (CC) November 22 2011 Phase 2
NCT00873509 Completed Drug: Buspirone|Drug: Placebo Autistic Disorder Chugani Diane C.|National Institute of Neurological Disorders and Stroke (NINDS) May 2009 Phase 2|Phase 3
NCT00174226 Completed Drug: Atomoxetine|Drug: Buspirone Attention Deficit Disorder With Hyperactivity Pfizer November 2004 Phase 2

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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