| Chemical Properties | Back Directory | [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 | Back Directory | [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) | Cmax (μmol/L) | T1/2 (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) | Cmax (μmol/L) | T1/2 (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) | Cmax (μmol/L) | T1/2 (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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