GAB氧杂DOL盐酸盐
| 中文名称 | GAB氧杂DOL盐酸盐 |
|---|---|
| 中文同义词 | GAB氧杂DOL盐酸盐;加波沙朵 盐酸盐;4,5,6,7-四氢异唑[5,4-C]吡啶-3-醇 盐酸盐;THIP 盐酸盐;4,5,6,7-四氢异恶唑并[5,4-C]吡啶-3(2H)-酮盐酸盐;盐酸加波沙朵 |
| 英文名称 | GABOXADOL HYDROCHLORIDE |
| 英文同义词 | 4,5,6,7-tetrahydroisoxazolo[5,4-c]pyridin-3(2H)-one monohydrochloride;THIP HYDROCHLORIDE (GABOXADOL) POST-SYNA PTIC GABA RE;THIP hydrochloride, 4,5,6,7-Tetrahydroisoxazolo[5,4-c]pyridin-3-ol hydrochloride;Einecs 285-687-7;Isoxazolo[5,4-c]pyridin-3(2H)-one, 4,5,6,7-tetrahydro-, Monohydrochloride;Gaboxadol hydrochloride solid, >=98% (HPLC);4,5,6,7-Tetrahydroisoxazolo[5,4-c]pyridin-3-ol, (HCl salt);gaboxadol hydrochloride |
| CAS号 | 85118-33-8 |
| 分子式 | C6H9ClN2O2 |
| 分子量 | 176.6 |
| EINECS号 | 285-687-7 |
| 相关类别 | 合成;活性候选物 |
| Mol文件 | 85118-33-8.mol |
| 结构式 |  |
GAB氧杂DOL盐酸盐 性质
| 熔点 | 236 °C |
|---|---|
| 储存条件 | Keep in dark place,Inert atmosphere,Room temperature |
| 溶解度 | 在乙醇中的溶解度为0.91mg/mL |
| 形态 | 固体 |
| 颜色 | 白色 |
| Merck | 14,4321 |
Gaboxadol hydrochloride (Lu 02-030 hydrochloride; THIP hydrochloride) 是一种强效有力的 GABAA receptor 的激动剂和 GABAC receptors 受体拮抗剂 (IC50=25 μM)。Gaboxadol hydrochloride 在亚基 α1β2γ2 显示部分激动剂功效，ED50 值为 143 µM，在 α5 亚基显示出一个完整的受体激动剂功效 (ED50=28-129 µM) 以及在 α4β3δ 亚基也有激动作用 (ED50= 6 µM)。Gaboxadol hydrochloride 是一种非阿片类镇痛试剂，并且具有催眠作用。
GABA A receptor; GABA C receptor
Gaboxadol hydrochloride (0.34, 3.5 and 7.0 μM) decreses permeability across Caco-2 cell monolayers with a dose dependent manner, shows the mean P app values with 8.1 × 10 -6 cm·s -1 , 6.1 × 10 -1 cm·s -6 and 5.6 × 10 -6 cm·s -1 for 0.34, 3.5 and 7 μM gaboxadol, respectively.
Gaboxadol hydrochloride (intraperitoneal injection; 0.5, 1, 1.5, 2, 3, 4, or 5 mg/kg; once daily; three-day interval) normalizes the distance traveled by Fmr1 KO2 mice to WT activity levels at 0.5 mg/kg, additionally, this compound has no effect on locomotor activity in Fmr1 KO2 mice.
| Animal Model: | Fmr1 KO2 mice (deletion of the promoter and first exon of Fmr1 resulting in mRNA and protein null mice) |
| Dosage: | 0.5, 1, 1.5, 2, 3, 4, or 5 mg/kg |
| Administration: | Intraperitoneal injection |
| Result: | Normalized Hyperactivity Observed in Fmr1 KO2 mice. |
安全信息
| 安全说明 | 22-24/25 |
|---|---|
| WGK Germany | 3 |
| RTECS号 | NY3396800 |
| 海关编码 | 2934.99.9001 |
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/01/25 | HY-10233 | Gaboxadol hydrochloride | 5 mg | 312元 | |
| 2024/01/25 | HY-10233 | GAB氧杂DOL盐酸盐 Gaboxadol hydrochloride | 85118-33-8 | 10mg | 500元 |