| CAS |
33386-08-2 |
| Chinese Name |
盐酸丁螺环酮 |
| English Name |
Buspirone Hydrochloride |
| Synonyms |
Buspirone HCl;Buspar;Narol |
| Molecular Formula |
C21H31N5O2·HCl |
| Molecular Weight |
421.96 |
| Solubility |
Soluble in DMSO ≥3mg/mL |
| Purity |
≥98% |
| Appearance |
White to off-white Solid |
| Storage |
Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| EC |
EINECS 251-489-4 |
| MDL |
MFCD00078569 |
| SMILES |
O=C(N(CCCCN1CCN(C2=NC=CC=N2)CC1)C(C3)=O)CC43CCCC4.[H]Cl |
| InChIKey |
RICLFGYGYQXUFH-UHFFFAOYSA-N |
| InChI |
InChI=1S/C21H31N5O2.ClH/c27-18-16-21(6-1-2-7-21)17-19(28)26(18)11-4-3-10-24-12-14-25(15-13-24)20-22-8-5-9-23-20;/h5,8-9H,1-4,6-7,10-17H2;1H |
| PubChem CID |
36431 |
| Target Point |
5-HT Receptor |
| Passage |
Neuronal Signaling;GPCR & G Protein |
| Background |
Buspirone Hydrochloride is a 5HT(1A) receptor agonist. |
| Biological Activity |
Buspirone, a serotonergic (5HT(1A) receptor agonist) anxiolytic drug with some D(2) dopaminergic effect.[2] Buspirone, a clinically effective non-benzodiazepine anxiolytic drug, caused 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.[3] |
| In Vitro |
Buspirone also inhibited these cells when it was administered to the outside of recorded neurons by microiontophoresis(effective currents = 2-15 nA).[3] |
| In Vivo |
In l-DOPA-primed rats，buspirone dose-dependently reduced LID and improved l-DOPA-related motor performance due to action at the 5-HT(1A)receptor. [1] Buspirone，a serotonergic(5HT(1A)receptor agonist)anxiolytic drug with some D(2)dopaminergic effect，had a pronounced anxiolytic-like effect in the zebrafish diving model at doses that did not have sedative effects.[2] |
| Animal Experiment |
To test this，male Sprague-Dawley rats received unilateral 6-hydroxydopamine(6-OHDA)lesions. In experiment 1，l-DOPA-primed rats were pre-treated with Vehicle(0.9% NaCl)，various doses of the partial 5-HT(1A)agonist，buspirone(0.25，1.0 or 2.5 mg/kg，ip)or buspirone(2.5 mg/kg，ip)+the 5-HT(1A)antagonist，WAY100635(0.5 mg/kg，ip)5 min prior to l-DOPA(12 mg/kg+15 mg/kg benserazide，ip). Rats were tested for LID using the abnormal involuntary movements(AIMs)scale and motor performance using the forepaw adjusting steps test(FAS). In experiment 2，l-DOPA-na ve rats received co-administration of l-DOPA+buspirone(1.0 or 2.5 mg/kg，ip)for 2 weeks. [1] |
| Data Literature Source |
[1]. Eskow KL，Gupta V，Alam S，Park JY，Bishop C. The partial 5-HT(1A) agonist buspirone reduces the expression and development of l-DOPA-induced dyskinesia in rats and improves l-DOPA efficacy. Pharmacol Biochem Behav. 2007 Aug-Sep;87(3):306-14.
[2]. Bencan Z，Sledge D，Levin ED. Buspirone，chlordiazepoxide and diazepam effects in a zebrafish model of anxiety. Pharmacol Biochem Behav. 2009 Nov;94(1):75-80.
[3]. VanderMaelen CP，Matheson GK，Wilderman RC，Patterson LA. Inhibition of serotonergic dorsal raphe neurons by systemic and iontophoretic administration of buspirone，a non-benzodiazepine anxiolytic drug. Eur J Pharmacol. 1986 Sep 23;129(1-2):123-30. |
| Unit |
Bottle |
| Specification |
25mg 50mg 100mg |
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