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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|Description||Buspirone is a serotonergic (5HT(1A) receptor agonist) anxiolytic drug with some D(2) dopaminergic effect, used for anxiety disorders.|
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. |
-  VanderMaelen CP, et al. Eur J Pharmacol, 1986, 129(1-2), 123-130.
-  Gammans RE, et al. Am J Med, 1986, 80(3B), 41-51.
-  Schreiber R, et al. Eur J Pharmacol, 1993, 249(3), 341-351.
|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.
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Molecular Weight Calculator
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT03083405||Enrolling by invitation||Drug: Buspirone||Sleep Bruxism|Hypertension|Thyroid Dysfunction|Mental Status Change|Sleep Apnea|Sleep Disorders|Cardiovascular Risk Factor|Cardiovascular Diseases|Temporomandibular Disorder||Wroclaw Medical University||April 20 2017||--|
|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||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|
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.
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