Description
Gaboxadol HCl (64603-91-4) is a GABA-A receptor agonist. Hypnotic agent.
Uses
GABAa agonist, GABAc antagonist
Definition
ChEBI: 4,5,6,7-Tetrahydroisoxazolo(5,4-c)pyridin-3-ol is an oxazole.
Biological Activity
Systemically active GABA A receptor agonist and GABA C receptor antagonist. Displays antinociceptive, anticonvulsant and sedative effects. Hypnotic agent that enhances delta activity within non-REM sleep in rats.
in vivo
THIP (Gaboxadol) (0.5, 5.0 mg/kg; p.o.; single) shws a good oral utilization, with Fa values of 110% and 83% for dosage of 0.5 and 5.0 mg/kg, respectively[2].
| Animal Model: | Sprague-Dawley rats (255-276 g)[2]. |
| Dosage: | 2.5 mg/kg (for i.v.); 0.5 and 5.0 mg/kg (for p.o.). |
| Administration: | Oral gavage; intravenous injection; single. |
| Result: | 1.19Pharmacokinetic Parameters of THIP 4 in Sprague-Dawley rats[2].
| IV (2.5 mg/kg) | PO (0.5 mg/kg) | PO (5.0 mg/kg) | | AUC (ng/mLh) | 1193 | 263 | 1988 | | Tmax (h) | - | 0.22 | 0.33 | | Cmax (ng/mL) | 4350 | 291 | 2061 | | CL/Fa (mL/h/kg) | - | 1939 | 2558 | | CL (mL/h/kg) | 2043 | - | - | | Fa (%) | 100 | 110 | 83 |
|
IC 50
α4β3δ GABAAR: 13 μM (EC
50)
References
[1] PRATAP MEERA Thomas S O Martin Wallner. Molecular basis for the high THIP/gaboxadol sensitivity of extrasynaptic GABA(A) receptors.[J]. Journal of neurophysiology, 2011, 106 4: 2057-2064. DOI:
10.1152/jn.00450.2011
