85118-33-8
中文名称
GAB氧杂DOL盐酸盐
英文名称
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
2024/08/14 15:30:11
![85118-33-8 结构式](/CAS/GIF/85118-33-8.gif)
基本信息
中文别名
THIP 盐酸盐加波沙朵 盐酸盐
GAB氧杂DOL盐酸盐
4,5,6,7-四氢异唑[5,4-C]吡啶-3-醇 盐酸盐
4,5,6,7-四氢异恶唑并[5,4-C]吡啶-3(2H)-酮盐酸盐
英文别名
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
所属类别
生物化工:激动剂抑制剂物理化学性质
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
Merck14,4321
常见问题列表
生物活性
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。靶点
GABA A receptor; GABA C receptor
体外研究
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.
体内研究
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. |