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CAS No.: 85118-33-8

Gaboxadol HCl/加波沙朵 Catalog No. CSN16036

Synonyms: Lu 02-030 hydrochloride;THIP hydrochloride;THIP HCl

Gaboxadol HCl is a systemically active GABAA receptor agonist and GABAA-ρ receptor antagonist. Displays antinociceptive, anticonvulsant and sedative effects. Hypnotic agent that enhances delta activity within non-REM sleep in rats.

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实验方案

技术信息

生物活性

描述Gaboxadol HCl is a potent agonist of the GABAA receptor and an antagonist of GABAC receptors (IC50=25 μM)^[3]. Gaboxadol HCl 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 analgesic and has hypnotic activities^[4]. Gaboxadol may be a substrate of the human proton-coupled amino acid transporter, hPAT1 and it inhibited the hPAT1-mediated L-[(3)H]proline uptake in Caco-2 cell monolayers with an inhibition constant K(i) of 6.6 mM. Gaboxadol HCl (0.34, 3.5 and 7.0 μM) decreases permeability across Caco-2 cell monolayers with a dose dependent manner, shows the mean Papp 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^[5]. Rat sleep EEG repeated dose studies of gaboxadol confirm a hypnotic-like profile and no withdrawal effects, whereas tolerance and withdrawal effects were shown with zolpidem^[6].
参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 5.6625 mL
- 28.3124 mL
- 56.6249 mL
- 5 mM
- 1.1325 mL
- 5.6625 mL
- 11.3250 mL
- 10 mM
- 0.5662 mL
- 2.8312 mL
- 5.6625 mL

技术信息

CAS号

85118-33-8

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C6H9ClN2O2

运输

蓝冰

分子量

176.60

别名

Lu 02-030 hydrochloride;THIP hydrochloride;THIP HCl;Gaboxadol (hydrochloride);THIP;Gaboxadol;OV-101;Lu-02-030;MK-0928;Lu02030. THIP;加波沙朵

溶解度

DMSO	73.0 mg/mL (413.4 mM) warming

动物实验配方

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