产品
编 号：F415758
分子式：C6H8N2O2
分子量：140.14
分子式：C6H8N2O2
分子量：140.14
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
5mg
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10mg
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25mg
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询价
50mg
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100mg
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询价
结构图
CAS No: 64603-91-4
产品详情
生物活性：
THIP (Gaboxadol) is a selective extrasynaptic GABAA receptors (eGABARs) agonist (with blood-brain barrier permeability), shows an EC50 value of 13 μM for δ-GABAAR. THIP induces strong tense GABAA-mediated currents in layer 2/3 neurons, but shows on effect on miniature IPSCs. THIP can be used in studies of sleep disorders.
体内研究：
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.Animal Model:Sprague-Dawley rats (255-276 g).
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.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
体外研究：
THIP (1 μM; 5 s) induces a robust tonic GABAA-mediated current in layer 2/3 neurons.THIP (1 μM; 1 s) shows no affect miniature IPSCs in layer 2/3 neurons.
THIP (Gaboxadol) is a selective extrasynaptic GABAA receptors (eGABARs) agonist (with blood-brain barrier permeability), shows an EC50 value of 13 μM for δ-GABAAR. THIP induces strong tense GABAA-mediated currents in layer 2/3 neurons, but shows on effect on miniature IPSCs. THIP can be used in studies of sleep disorders.
体内研究：
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.Animal Model:Sprague-Dawley rats (255-276 g).
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.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
体外研究：
THIP (1 μM; 5 s) induces a robust tonic GABAA-mediated current in layer 2/3 neurons.THIP (1 μM; 1 s) shows no affect miniature IPSCs in layer 2/3 neurons.
产品资料
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