NCS-382
CAS No. : 520505-01-5
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| 500 mg | Get quote | |
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| Cat. No. : | HY-101207 |
| M.Wt: | 218.25 |
| Formula: | C13H14O3 |
| Purity: | >98 % |
| Solubility: | 10 mM in DMSO |
NCS-382 is a potent GABA receptor antagonist and also a GHBR receptor antagonist. NCS-382 has anticonvulsant and antisedative activity. NCS-382 is used in the related research of hereditary nervous system diseases[1][4].
In Vitro:NCS-382 (0.5 nM, 24 h) shows no capacity for inhibition of microsomal CYPs (CYP1A2, 2B6, 2C8, 2C9, 2C19, 2D6 and 3A4) and minimal potential for activation of xenobiotic nuclear receptors in HepG2 cells[2].
NCS-382 (0.01-1000 μM, 24 h) shows low probability of cellular toxicity in HepG2 cells[2].
NCS-382 is a GHBR antagonist with IC50s of 134.1 nM and 201.3 nM in isolated rat striatum and hippocampus membranes, respectively[4].
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 100mg/kg [1]
在剂量100mg/kg下小鼠血清和组织的药代动力学分析[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 |
在剂量300mg/kg下小鼠血清和组织的药代动力学分析[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 | / | / | / |
在剂量500mg/kg下小鼠血清和组织的药代动力学分析[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 | / | / | / |
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