| Bioactivity | 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]. |
| Invitro | NCS-382 (0.5 nM, 24 h) 在 HepG2 细胞中不显示抑制微粒体 CYPs (CYP1A2、2B6、2C8、2C9、2C19、2D6 和 3A4) 的能力[2]。NCS-382 (0.01-1000 μM, 24 h)对 HepG2 细胞具有较低的细胞毒性[2]。NCS-382是 GHBR 拮抗剂，在离体大鼠纹状体和海马膜中的 IC50 值分别为134.1 和 201.3 nM[4]。 Cell Cytotoxicity Assay[2] Cell Line: |
| In Vivo | NCS-382 (100, 300, 500 mg/kg; 腹腔注射) 在小鼠模型中，剂量为 100 mg/kg 时，最大血清浓度是脑组织的 4 倍，肾组织的 10 倍，最大肝浓度比血清浓度高 700% 以上[1]。在 100 mg/kg 剂量下，在小鼠模型中腹腔给药后可能优先停留在肝脏，但在大脑和肾脏停留时间较长。小鼠模型中在 500 mg/kg 剂量下，脑渗透性有所改善，表现为脑血清比增加。NCS-382 (0.83-2.08 mmol/kg/kg; 腹腔注射) 在小鼠模型中当以 1.66 mmol/kg 和 2.08 mmol/kg 的剂量给药时，它可减少 GHB 诱导的小鼠在强迫游泳试验中静止时间增加，表明有抗镇静活性[3]。NCS-382 (2.3 mmol/kg/kg; 腹腔注射) 可减少听源性癫痫易感的瑞士 RB 小鼠以及小型癫痫大鼠模型中的棘波和波形放电[4]。 Animal Model: |
| Name | NCS-382 |
| CAS | 520505-01-5 |
| Formula | C13H14O3 |
| Molar Mass | 218.25 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Ainslie GR, et al. A pharmacokinetic evaluation and metabolite identification of the GHB receptor antagonist NCS-382 in mouse informs novel therapeutic strategies for the treatment of GHB intoxication. Pharmacol Res Perspect. 2016 Oct 18;4(6):e00265. [2]. Vogel KR, et al. In vitro toxicological evaluation of NCS-382, a high-affinity antagonist of γ-hydroxybutyrate (GHB) binding. Toxicol In Vitro. 2017 Apr;40:196-202 [3]. Schmidt C, et al. Anti-sedative and anti-cataleptic properties of NCS-382, a gamma-hydroxybutyrate receptor antagonist. Eur J Pharmacol. 1991 Oct 22;203(3):393-7. [4]. Maitre M, Hechler V, Vayer P, Gobaille S, Cash CD, Schmitt M, Bourguignon JJ. A specific gamma-hydroxybutyrate receptor ligand possesses both antagonistic and anticonvulsant properties. J Pharmacol Exp Ther. 1990 Nov;255(2):657-63. |