Home Neuronal Signaling 5-HT Receptor agonist Buspirone HCl

research use only

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.
Buspirone HCl 5-HT Receptor agonist Chemical Structure

Chemical Structure

Molecular Weight: 421.96

Jump to

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

Molarity Calculator

Mass Concentration Volume Molecular Weight
Dilution Calculator Molecular Weight Calculator

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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

mg/kg
g
μL

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
% DMSO
+
%

Calculation results:

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.

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

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 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
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

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

Signaling Pathway Map