Buspirone HCl

Catalog No.S4256

Buspirone HCl Chemical Structure

Molecular Weight(MW): 421.96

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

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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

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)

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 421.96
Formula

C21H31N5O2.HCl

CAS No. 33386-08-2
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03587142 Not yet recruiting Gastroparesis National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK) March 31 2019 Phase 2
NCT03587142 Not yet recruiting Gastroparesis National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK) March 31 2019 Phase 2
NCT03432065 Recruiting Autism Spectrum Disorder|Anxiety Massachusetts General Hospital October 2018 Phase 2
NCT03538431 Recruiting Autism Spectrum Disorder Massachusetts General Hospital|Massachusetts Institute of Technology October 31 2018 Phase 4
NCT03432065 Recruiting Autism Spectrum Disorder|Anxiety Massachusetts General Hospital October 2018 Phase 2
NCT03538431 Recruiting Autism Spectrum Disorder Massachusetts General Hospital|Massachusetts Institute of Technology October 31 2018 Phase 4

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID