product name Buspirone HCl
Description: Buspirone belongs to the azapirone chemical class and is a 5HT1A receptor agonist. Buspirone is used as an anxiolytic psychotropic drug. It is primarily used to treat generalized anxiety disorder (GAD). Unlike most drugs predominantly used to treat anxiety, buspirones pharmacology is not related to benzodiazepines or barbiturates, and so does not carry the risk of physical dependence and withdrawal symptoms.
References: Eur J Pharmacol. 1986 Sep 23;129(1-2):123-30; Am J Med. 1986 Mar 31;80(3B):41-51.
421.96
Formula
C21H31N5O2.HCl
CAS No.
33386-08-2
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 84 mg/mL (199.1 mM)
Water: 84 mg/mL (199.1 mM)
Ethanol: 36 mg/mL (85.3 mM)
Solubility (In vivo)
15% Captisol, pH 9: 10 mg/mL
Synonyms
other peoduct :
| In Vitro |
In vitro activity: 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. Kinase Assay: Cell Assay: |
|---|---|
| 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-DOPAs 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. |
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| Formulation & Dosage | |
| References | Eur J Pharmacol. 1986 Sep 23;129(1-2):123-30; Am J Med. 1986 Mar 31;80(3B):41-51; Eur J Pharmacol. 1993 Nov 16;249(3):341-51. |
3-O-(2-Aminoethyl)-25-hydroxyvitamin D4
