2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. GABA Receptor
  4. NCS-382

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.

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NCS-382 Chemical Structure

NCS-382 Chemical Structure

CAS No. : 520505-01-5

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NCS-382 Related Antibodies

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Description

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

NCS-382 Related Antibodies

Cell Cytotoxicity Assay[2]

Cell Line: HepG2 cells
Concentration: 0.01-1000 μM
Incubation Time: 24 h
Result: Reduced HepG2 cell viability at a concentration of 1 mM, and this same concentration did not induce apoptosis or cytotoxicity in HepG2 cells.
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
Pharmacokinetic analysis of mouse serum and tissue at a dose of 300mg/kg [1]

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

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 / / /

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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
Molecular Weight

218.25

Formula

C13H14O3
CAS No.
SMILES

O=C(O)/C=C1CCCC2=CC=CC=C2C\1O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Solvent & Solubility

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In Vivo:

The following protocol is derived from the literature and is for reference only. It is recommended to first try a small sample.

  • Protocol 1

    NCS-382 dissolved in 0.1% sodium bicarbonate[1]

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Purity & Documentation
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NCS-382 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

NCS-382520505-01-5NCS382NCS 382GABA ReceptorGamma-aminobutyric acid Receptorγ-Aminobutyric acid ReceptorHepG2 cellsCytotoxicityNervous system diseasesanticonvulsantInhibitorinhibitorinhibit

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