Basic information Safety Supplier Related

THIP HYDROCHLORIDE

Basic information Safety Supplier Related

THIP HYDROCHLORIDE Basic information

Product Name:
THIP HYDROCHLORIDE
Synonyms:
  • THIP HYDROCHLORIDE
  • 4,5,6,7-tetrahydroisoxazolo(5,4-c)pyridin-3(2h)-onehydrate
  • 4-c)pyridin-3(2h)-one,4,5,6,7-tetrahydro-isoxazolo(hydrate
  • gaboxadol
  • 4,5,6,7-TETRAHYDROISOXAZOLO[5,4-C]PYRIDIN-3-OL
  • 4,5,6,7-TETRAHYDROISOXAZOLO[5,4-C]PYRIDIN-3-OL HYDROCHLORIDE
  • 4,5,6,7-Tetrahydroisoxazolo[5,4-c]pyridin-3(2H)-one
  • THIP
CAS:
64603-91-4
MF:
C6H8N2O2
MW:
140.14
EINECS:
264-963-0
Product Categories:
  • GABA/Glycine receptor
Mol File:
64603-91-4.mol
More
Less

THIP HYDROCHLORIDE Chemical Properties

Melting point:
242-244° (dec)
Density 
1.36±0.1 g/cm3(Predicted)
storage temp. 
Store at RT
solubility 
ethanol: 0.91 mg/mL
pka
pKa (water, 25°): 4.44 ±0.03; 8.48 ±0.04
form 
solid
color 
white
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO or distilled water may be stored at -20°C for up to 3 months.
More
Less

Safety Information

Safety Statements 
22-24/25
WGK Germany 
3
RTECS 
NY3396800

MSDS

More
Less

THIP HYDROCHLORIDE Usage And Synthesis

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/mL?h)11932631988
Tmax (h)-0.220.33
Cmax (ng/mL)43502912061
CL/Fa (mL/h/kg)-19392558
CL (mL/h/kg)2043--
Fa (%)10011083

IC 50

α4β3δ GABAAR: 13 μM (EC50)

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

THIP HYDROCHLORIDESupplier

3B Pharmachem (Wuhan) International Co.,Ltd.
Tel
821-50328103-801 18930552037
Email
3bsc@sina.com
LGM Pharma
Tel
1-(800)-881-8210
Email
inquiries@lgmpharma.com
Hangzhou Sage Chemical Co., Ltd.
Tel
+86057186818502 13588463833
Email
info@sagechem.com
Shanghai Jian Chao Chemical Technology Co., Ltd.
Tel
150-2103-5486 18017383231
Email
983544897@qq.com
Shanghai TaoSu Biochemical Technology Co., Ltd.
Tel
021-33632979
Email
info@tsbiochem.com
More
Less

THIP HYDROCHLORIDE(64603-91-4)Related Product Information