85118-33-8
中文名稱
GAB氧雜DOL鹽酸鹽
英文名稱
GABOXADOL HYDROCHLORIDE
CAS
85118-33-8
分子式
C6H9ClN2O2
分子量
176.601
MOL 文件
85118-33-8.mol
更新日期
2025/01/21 14:19:47
85118-33-8 結(jié)構(gòu)式
基本信息
中文別名
THIP 鹽酸鹽加波沙朵 鹽酸鹽
GAB氧雜DOL鹽酸鹽
4,5,6,7-四氫異唑[5,4-C]吡啶-3-醇 鹽酸鹽
4,5,6,7-四氫異惡唑并[5,4-C]吡啶-3(2H)-酮鹽酸鹽
英文別名
MK 0928)Einecs 285-687-7
gaboxadol hydrochloride
Gaboxadol HCl (Lu 02-030
GaboxadolHydrochloride>
Lu 02-030 (hydrochloride)
Gaboxadol hydrochloride solid, >=98% (HPLC)
THIP HYDROCHLORIDE (GABOXADOL) POST-SYNA PTIC GABA RE
4,5,6,7-Tetrahydroisoxazolo[5,4-c]pyridin-3-ol, (HCl salt)
4,5,6,7-tetrahydro-[1,2]oxazolo[5,4-c]pyridin-6-ium-3-olate
所屬類別
生物化工：激動劑抑制劑物理化學(xué)性質(zhì)
熔點(diǎn)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
Merck14,4321
安全數(shù)據(jù)
常見問題列表
生物活性
Gaboxadol hydrochloride (Lu 02-030 hydrochloride; THIP hydrochloride) 是一種強(qiáng)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。靶點(diǎn)
GABA A receptor; GABA C receptor
體外研究
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.
體內(nèi)研究
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. |