产品
编 号：F479809
分子式：C6H9ClN2O2
分子量：176.6
分子式：C6H9ClN2O2
分子量：176.6
产品类型
规格
价格
是否有货
5mg
250
In-stock
10mg
400
In-stock
25mg
720
In-stock
50mg
960
In-stock
100mg
1440
In-stock
结构图
CAS No: 85118-33-8
产品详情
生物活性：
Gaboxadol hydrochloride (Lu 02-030 hydrochloride) is a potent agonist of the GABAA receptor and an antagonist of GABAC receptors (IC50=25 μM). Gaboxadol hydrochloride displays a partial agonist efficacy on subunit α1β2γ2 with an ED50 value of 143 μM, a full agonist efficacy at α5 subunit (ED50=28-129 μM) and a superagonist efficacy at α4β3δ (ED50=6 μM). Gaboxadol hydrochloride is a non-opioid agent.
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.
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 Papp values with8.1 × 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 (Lu 02-030 hydrochloride) is a potent agonist of the GABAA receptor and an antagonist of GABAC receptors (IC50=25 μM). Gaboxadol hydrochloride displays a partial agonist efficacy on subunit α1β2γ2 with an ED50 value of 143 μM, a full agonist efficacy at α5 subunit (ED50=28-129 μM) and a superagonist efficacy at α4β3δ (ED50=6 μM). Gaboxadol hydrochloride is a non-opioid agent.
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.
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 Papp values with8.1 × 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.
产品资料
Copyright©2015-2024 沪ICP备2022026524号-1
沪公网安备