biological activity | Gaboxadol hydrochloride (Lu 02-030 hydrochloride; THIP hydrochloride) is a powerful agonist of GABAA receptor and GABAC receptors receptor antagonist (IC50=25 μM). The Gaboxadol hydrochloride shows partial agonist efficacy in the subunit α1β2γ2, with an ED50 value of 143 µM, a complete receptor agonist efficacy in the α5 subunit (ED50=28-129 µM) and in the α4β3δ subunit It also has an agonistic effect (ED50=6 µM). Gaboxadol hydrochloride is a non-opioid analgesic agent and has hypnotic effects. |
target | GABA A receptor; GABA C receptor |
in vitro study | Gaboxadol hydrochloride (0.34, 3.5 and 7.0 μ m) decreses permeability across Caco-2 cell monolayers with a dose dependent banner, shows the mean P app values with 8.1 × 10 -6cm s -1 , 6.1 × 10 -1cm s -6 and 5.6 × 10 -6cm s -1 for 0.34, 3.5 and 7 μ m gaboxadol, respectively. |
in vivo study | 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 byFmr1KO2 ice to WT activity levels at 0.5 mg/kg, additionally, this compound has no effect on locomotor activity inFmr1KO2 mice. Animal Model: Fmr1KO2 mice (deletion of the promoter and first exon ofFmr1resulting 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 inFmr1KO2 mice. |
Animal Model:
| Fmr1KO2 mice (deletion of the promoter and first exon ofFmr1resulting 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 inFmr1KO2 mice. |