盐酸丁螺环酮
货号：
IB1910
品牌：
Jinpan
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产品简介
| 有效期 | 2年 |
| 描述 | 是一种5HT（1A）受体激动剂。 |
| MDL | MFCD00078569 |
| EC | EINECS 251-489-4 |
| 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 |
| 别名 | 丁螺环酮盐酸盐 |
| 英文名称 | Buspirone Hydrochloride |
| CAS | 33386-08-2 |
| 分子式 | C21H31N5O2·HCl |
| 分子量 | 421.96 |
| 储存条件 | 2-8℃ |
| 纯度 | ≥98% |
| 外观（性状） | White Solid |
| 单位 | 瓶 |
| 生物活性 | 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] |
| SMILES | O=C(N(CCCCN1CCN(C2=NC=CC=N2)CC1)C(C3)=O)CC43CCCC4.[H]Cl |
| 靶点 | 5-HT Receptor |
| 动物实验 | 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] |
| 数据来源文献 | [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. |
| 规格 | 25mg 50mg 100mg |