Home Neuronal Signaling 5-HT Receptor agonist Buspirone HCl

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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.
Buspirone HCl 5-HT Receptor agonist Chemical Structure

Chemical Structure

Molecular Weight: 421.96

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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

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

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

In vivo
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Mechanism of Action

Targets/IC50/Ki
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]
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

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