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Buspirone HCl(MJ90221)HCl
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Buspirone HCl(MJ90221)HCl图片
CAS NO:33386-08-2
规格:≥98%
包装与价格:
包装价格(元)
250mg电议
500mg电议
1g电议
2g电议
5g电议
10g电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)421.96
FormulaC21H31N5O2.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
SynonymsBuspirone, MJ 9022 1, Buspar, MJ-9022-1, MJ90221, MJ9022 1, MJ9022-1
SMILES CodeO=C(N(CCCCN1CCN(C2=NC=CC=N2)CC1)C(C3)=O)CC43CCCC4.Cl
实验参考方法
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.

In VivoBuspirone (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.
Animal modelRats
Formulation & Dosage3, 20 mg/rat, i.p.
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.