Fluvoxamine maleate/DU-23000 maleate；氟伏沙明马来酸盐
货号：
IF0550
品牌：
Jinpan
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产品简介
| MDL | MFCD00269809 |
| EC | EINECS 228-994-3 |
| 别名 | 马来酸氟;Fluvoxaminemaleate;DU-23000maleate |
| 英文名称 | Fluvoxamine maleate/DU-23000 maleate |
| CAS | 61718-82-9 |
| 分子式 | C14H18F3N2O2.C4H4O4 |
| 分子量 | 434.41 |
| 纯度 | ≥98% |
| 单位 | 瓶 |
| 生物活性 | Fluvoxamine maleate (DU-23000, MK-264)是一种选择性5-羟色胺再摄取抑制剂(SSRI)。[1] |
| In Vitro | Fluvoxamine增加大鼠前额皮质和丘脑中[5-HT]的水平，也增加纹状体中[DA]的水平。[1]??Fluvoxamine maleate可通过脊柱5-HT 2A/2C受体改善触觉异常性疼痛，通过作用于受体或5-HT的神经元起作用。[2] |
| In Vivo | 在非结扎小鼠的爪压力测试中，Fluvoxamine maleate也表现出剂量依赖方式的抗伤害感受。Fluvoxamine maleate也诱导急性爪压力测试的抗伤害作用，并且这种作用为5-HT3受体拮抗剂granisetron所拮抗。[2] 在大鼠海马内侧前额叶皮质（mPFC）中，Fluvoxamine（10和30 mg/kg，腹腔注射）以剂量依赖的方式增强了海马-mPFC通路突触效能。[3] 在麻醉大鼠的海马CA1区中，Fluvoxamine（10和30 毫克/千克，腹腔注射）抑制长时程增强（LTP）。Fluvoxamine（30 毫克/千克，腹腔注射）诱导的LTP为5-HT（1A）受体拮抗剂NAN-190（0.5 毫克/千克，腹腔注射）完全逆转，但不是受5-HT（4）受体拮抗剂GR113808（20 毫克/大鼠，脑室注射）以及5-HT的（7）受体拮抗剂DR4004（10 毫克/大鼠，脑室注射）所影响。[4] |
| SMILES | O=C(O)/C=CC(O)=O.FC(C1=CC=C(/C(CCCCOC)=N/OCCN)C=C1)(F)F |
| 靶点 | 5-HT Receptor;Serotonin Transporter (SERT) |
| 细胞实验 | Fluvoxamine maleate (10 and 30 mg/kg, i.p.) dose-dependently elevated the 50% threshold, as assessed by the von Frey test. At a dose of 30 mg/kg, the antiallodynic effects of fluvoxamine were significant and the 50% threshold was elevated to 0.19 _x005f 0.05 g at 15 min after its administration. On the other hand, the tricyclic antidepressant amitriptyline hydrochloride (3 and 10 mg/kg, s.c.) did not exert antiallodynic effects in Seltzer-model mice. Because amitriptyline showed the muscle relaxant effect via 5-HT2 receptors, effects of the higher dose of amitriptyline were not determined. Fluvoxamine was injected either i.c.v. or i.t. to determine the site of its antiallodynic effect. While i.c.v. injection of fluvoxamine maleate (10, 30, and 100 mg/animal) did not show any effects on the withdrawal threshold, i.t. injection (10, 30, and 100 mg/animal) induced the antiallodynic effect. These results indicate that the antiallodynic effect of i.p. fluvoxamine is produced at the spinal cord.[2] |
| 数据来源文献 | [1] Denys D, et al. Psychopharmacology (Berl),?004, 176(2), 195-203.? [2] Honda M, et al. Neuropharmacology,2006, 51(4), 866-872. [3] Ohashi S, et al. Brain Res,2002, 949(1-2), 131-138. [4] Kojima T, et al. Brain Res,2003, 959(1), 165-168. |
| 规格 | 10mg 50mg 100mg |
是5-羟色胺再吸收抑制剂。