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Buspirone HCl

Name: Buspirone HCl
Brand: Selleck Chemicals
SKU: S4256
Rating: 5 (1 reviews)

Synonyms: Buspirone hydrochloride

Catalog No.S4256 Purity: 99.99%

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

Buspirone HCl Chemical Structure

CAS: 33386-08-2

Selleck's Buspirone HCl has been cited by 1 publication

Purity & Quality Control

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

99.99

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Signaling Pathway

5-HT Receptor Signaling Pathway

Choose Selective 5-HT Receptor Inhibitors

Biological Activity

Description

Buspirone(Buspirone hydrochloride) 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
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
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]

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-01-11)
NCT05511909	Recruiting	Opioid Use Disorder\|Opioid Withdrawal\|Opioid Craving\|Anxiety	Johns Hopkins University	December 15 2022	Phase 2
NCT03444831	Completed	Dyspepsia	Isfahan University of Medical Sciences	March 1 2016	Phase 4
NCT02483598	Terminated	Gastric Bypass	North Dakota State University\|Neuropsychiatric Research Institute Fargo North Dakota	June 2015	Phase 4
NCT01699828	Completed	Smoking Cessation\|Tobacco Use Cessation	Centre for Addiction and Mental Health	October 2012	Phase 1\|Phase 2
NCT01496612	Terminated	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	Autistic Disorder	Chugani Diane C.\|National Institute of Neurological Disorders and Stroke (NINDS)	May 2009	Phase 2\|Phase 3

References

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Chemical Information & Solubility

Molecular Weight	421.96	Formula	C₂₁H₃₁N₅O₂.HCl
CAS No.	33386-08-2	SDF	Download Buspirone HCl SDF
Smiles	C1CCC2(C1)CC(=O)N(C(=O)C2)CCCCN3CCN(CC3)C4=NC=CC=N4.Cl
Storage (From the date of receipt)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

In vitro
Batch:

DMSO : 84 mg/mL ( (199.07 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 84 mg/mL

Ethanol : 36 mg/mL

Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.

In vivo Formulation Calculator

Preparing Stock Solutions

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In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

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Working concentration: mg/ml;

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.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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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