GAB氧雜DOL鹽酸鹽
| 中文名稱 | GAB氧雜DOL鹽酸鹽 |
|---|---|
| 中文同義詞 | GAB氧雜DOL鹽酸鹽;加波沙朵 鹽酸鹽;4,5,6,7-四氫異唑[5,4-C]吡啶-3-醇 鹽酸鹽;THIP 鹽酸鹽;4,5,6,7-四氫異惡唑并[5,4-C]吡啶-3(2H)-酮鹽酸鹽;鹽酸加波沙朵;4,5,6,7-四氫異噁唑并[5,4-C]吡啶-3(2H)-酮 鹽酸鹽;GABOXADOL HYDROCHLORIDE (THIP HYDROCHLORIDE),GABAA RECEPTOR激動劑AND GABAC RECEPTOR拮抗劑 |
| 英文名稱 | GABOXADOL HYDROCHLORIDE |
| 英文同義詞 | 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號 | 85118-33-8 |
| 分子式 | C6H9ClN2O2 |
| 分子量 | 176.6 |
| EINECS號 | 285-687-7 |
| 相關類別 | 合成;活性候選物 |
| Mol文件 | 85118-33-8.mol |
| 結構式 |  |
GAB氧雜DOL鹽酸鹽 性質
| 熔點 | 236 °C |
|---|---|
| 儲存條件 | Keep in dark place,Inert atmosphere,Room temperature |
| 溶解度 | 在乙醇中的溶解度為0.91mg/mL |
| 形態(tài) | 固體 |
| 顏色 | 白色 |
| Merck | 14,4321 |
Gaboxadol hydrochloride (Lu 02-030 hydrochloride; THIP hydrochloride) 是一種強效有力的 GABAA receptor 的激動劑和 GABAC receptors 受體拮抗劑 (IC50=25 μM)。Gaboxadol hydrochloride 在亞基 α1β2γ2 顯示部分激動劑功效，ED50 值為 143 μM，在 α5 亞基顯示出一個完整的受體激動劑功效 (ED50=28-129 μM) 以及在 α4β3δ 亞基也有激動作用 (ED50= 6 μM)。Gaboxadol hydrochloride 是一種非阿片類鎮(zhèn)痛試劑，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
| 安全說明 | 22-24/25 |
|---|---|
| WGK Germany | 3 |
| RTECS號 | NY3396800 |
| 海關編碼 | 2934.99.9001 |
| 更新日期 | 產品編號 | 產品名稱 | CAS號 | 包裝 | 價格 |
|---|---|---|---|---|---|
| 2025/02/08 | HY-10233 | GAB氧雜DOL鹽酸鹽 Gaboxadol hydrochloride | 85118-33-8 | 5 mg | 312元 |
| 2025/02/08 | HY-10233 | GAB氧雜DOL鹽酸鹽 Gaboxadol hydrochloride | 85118-33-8 | 10 mM * 1 mLin DMSO | 343元 |