ChemicalBook CAS DataBase List 520505-01-5

520505-01-5

Name	NCS-382
CAS	520505-01-5
Molecular Formula	C13H14O3
MDL Number	MFCD02114253
Molecular Weight	218.25
MOL File	520505-01-5.mol

Chemical Properties

Boiling point	460.8±30.0 °C(Predicted)
density	1.340±0.06 g/cm3(Predicted)
storage temp.	Store at -20°C
solubility	<21.83mg/ml in DMSO
pka	4.33±0.41(Predicted)

Hazard Information

Uses

NCS-382 is an antagonist of γ-hydroxybutyric acid (GHB).

in vivo

NCS-382 (100, 300, 500 mg/kg; i.p.) shows at a dose of 100 mg/kg has a maximum serum concentration that is 4 times that of the brain and 10 times that of the kidney, and a maximum liver concentration that is more than 700% higher than the serum in mouse model^[1].
At a dose of 500 mg/kg, it may preferentially reside in the liver after intraperitoneal administration in mouse model^[1].
At a dose of 500 mg/kg, brain permeability improves, as evidenced by an increase in brain serum ratio in mouse model^[1].
NCS-382 (0.83-2.08 mmol/kg; i.p.) reduces GHB-induced increases in the time mice spent immobile in the forced swim test, indicating anti-sedative activity, when administered at doses of 1.66 and 2.08 mmol/kg in mice model^[3].
NCS-382 (2.3 mmol/kg; i.p.) decreases spike and wave discharges in audiogenic seizure-susceptible Swiss Rb mice, as well as a rat model of petit mal epilepsy ^[4].
Pharmacokinetic analysis of mouse serum and tissue at a dose of 100 mg/kg ^[1]

Tissue	Dose (mg/kg)	AUC (μg h/L)	C_max (μmol/L)	T_1/2 (h)
Serum	100	119	241	0.243
Brain	100	139	60	0.967
Liver	100	1150	1695	/
Kidney	100	24.5	23.6	0.308

Pharmacokinetic analysis of mouse serum and tissue at a dose of 300mg/kg ^[1]

Pharmacokinetic Analysis^[1]

Tissue	Dose (mg/kg)	AUC (μg h/L)	C_max (μmol/L)	T_1/2 (h)
Serum	300	436	374	0.468
Brain	300	313	141	0.883
Liver	300	/	/	/
Kidney	300	/	/	/

Pharmacokinetic analysis of mouse serum and tissue at a dose of 500mg/kg ^[1]

Pharmacokinetic Analysis^[1]

Tissue	Dose (mg/kg)	AUC (μg h/L)	C_max (μmol/L)	T_1/2 (h)
Serum	500	717	451	0.683
Brain	500	1280	530	0.761
Liver	500	/	/	/
Kidney	500	/	/	/

Animal Model:	GBL induced mouse model^[1]
Dosage:	300 mg/kg(Combined with diclofenac (25 mg/kg))
Administration:	Intraperitoneal injection (i.p.), Thirty minutes later, mice were given an i.p. injection of GBL (100 mg/kg diluted in PBS)
Result:	In the presence of diclofenac, it was highly protective against GBL mediated responses.

Animal Model:	GBL induced mouse model^[3]
Dosage:	0.83, 1.25, 1.66, 2.08mmol/kg
Administration:	Intraperitoneal injection (i.p.), 30 min before the test
Result:	At a dosage of 2.08 mmol/kg, completely blocked the effect of GHB when administered at 3.18 mmol/kg

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