Gaboxadol hydrochloride 是GABAA受体激动剂和GABAC受体拮抗剂，是非阿片类试剂，可用于缓解疼痛和促进睡眠的研究。它在亚基 α1β2γ2 显示部分激动剂功效，在 α5 亚基显示出一个完整的受体激动剂功效以及在 α4β3δ 亚基也有激动作用。

Gaboxadol (hydrochloride) is a GABAA receptor agonist.

Gaboxadol produced ≥80 % gaboxadol-lever responding and did not alter rates. No other drug produced, on average, ≥80 % drug-lever responding up to doses that decreased rates, although 1.78 mg/kg midazolam produced 32 % gaboxadol-lever responding. Ethanol and pregnanolone did not enhance the effects of gaboxadol. Rats discriminating midazolam, pregnanolone, or ethanol from vehicle responded predominantly on the vehicle lever after receiving gaboxadol[1].

Eight rats discriminated 5.6 mg/kg gaboxadol from vehicle while responding under a fixed - ratio 10 schedule for food.?Modulators acting at GABAA receptors containing α4-δ subunits (pregnanolone, ethanol, and flumazenil) and receptors that do not contain those subunits (midazolam) were studied alone ;?pregnanolone and ethanol were also combined with gaboxadol.?In addition, gaboxadol was studied in separate groups discriminating 0.32 mg/kg midazolam, 3.2 mg/kg pregnanolone, or 0.75 g/kg ethanol from vehicle[1].

85118-33-8

C6H9ClN2O2

176.6

THIP (hydrochloride);GAB氧杂DOL盐酸盐;Gaboxadol (hydrochloride);加波沙朵;Lu 02-030 (hydrochloride);Gaboxadol hydrochloride

DMSO:75 mg/mL (424.69 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years