| CAS NO: | 33386-08-2 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 250mg | 电议 |
| 500mg | 电议 |
| 1g | 电议 |
| 2g | 电议 |
| 5g | 电议 |
| 10g | 电议 |
| Molecular Weight (MW) | 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 | Buspirone, MJ 9022 1, Buspar, MJ-9022-1, MJ90221, MJ9022 1, MJ9022-1 |
| SMILES Code | O=C(N(CCCCN1CCN(C2=NC=CC=N2)CC1)C(C3)=O)CC43CCCC4.Cl |
| 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 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. |
| Animal model | Rats |
| Formulation & Dosage | 3, 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. |
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