2. GPCR/G Protein Neuronal Signaling Immunology/Inflammation
  3. Histamine Receptor
  4. H3R antagonist 8

H3R antagonist 8 是一种选择性非咪唑类组胺 H3 receptor 拮抗剂 (IC50 = 0.35 μM)。H3R antagonist 8 具有 hERG 通道阻断活性 (IC50 = 0.67 μM)。H3R antagonist 8 通过拮抗 H3 受体抑制癫痫发作。H3R antagonist 8 在最大电休克癫痫 (MES) 模型中减少小鼠的强直后肢伸展 (THLE) (ED50 = 20.21 mg/kg)，并缩短 AB 株斑马鱼幼虫中戊四唑 (PTZ) 诱导的总移动距离。H3R antagonist 8 可用于癫痫研究。

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H3R antagonist 8

H3R antagonist 8 Chemical Structure

CAS No. : 3097193-89-7

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H3R antagonist 8 相关抗体

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生物活性

H3R antagonist 8 is a selective nonimidazole histamine H3 receptor antagonist (IC50 = 0.35 μM). H3R antagonist 8 exhibits hERG channel blockade activity (IC50 = 0.67 μM). H3R antagonist 8 inhibits seizures by antagonizing H3 receptor. H3R antagonist 8 reduces tonic hind limb extension (THLE) in mice in the maximal electroshock seizure (MES) model (ED50 = 20.21 mg/kg) and and shortens pentylenetetrazol (PTZ)-induced total movement distance in AB strain zebrafish larvae. H3R antagonist 8 can be used for the study of epilepsy[1].

IC50 & Target[1]

H3 receptor

0.35 μM (IC50)

体外研究
(In Vitro)

H3R antagonist 8 (Compound 6n) 在表达人 H3R 的 HEK-293 细胞中通过 CRE 驱动的荧光素酶测定显示出强效的 H3 受体拮抗活性，其 IC50 值为 0.35 μM[1]。
H3R antagonist 8 (0.1-100 μM) 在稳定表达 hERG 钾通道的 HEK-293 细胞中使用膜片钳技术显示出 hERG 通道阻断活性，其 IC50 值为 0.67 μM[1]。

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

H3R antagonist 8 相关抗体:
体内研究
(In Vivo)

H3R antagonist 8 (Compound 6n) (30 mg/kg，腹腔注射，单次剂量) 在最大电休克癫痫 (MES) 诱导的癫痫模型中完全消除雄性昆明小鼠的强直后肢伸展 (THLE)[1]。
H3R antagonist 8 (Compound 6n) (1 μM，预处理 3 小时) 显著减少由戊四唑 (PTZ) 诱导的 AB 株斑马鱼幼虫的总移动距离[1]。

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

Animal Model: Male KunMing mice (6-8 weeks old, 18-22 g) were used for the maximal electroshock seizure (MES)-induced seizure model[1]
Dosage: 30 mg/kg
Administration: i.p., single dose
Result: Abolished tonic hind limb extension (THLE) of mice at 4 h post-administration, with a median effective dose of 20.21 mg/kg.
Animal Model: Pentylenetetrazol (PTZ)-induced AB strain zebrafish[1]
Dosage: 1 μM
Administration: Pretreatment for 3 h
Result: Reduced the total movement distance induced by PTZ.
分子量

398.93

Formula

C23H27ClN2O2
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

H3R antagonist 8 相关分类

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Keywords:

H3R antagonist 83097193-89-7Histamine ReceptorEpilepsyzebrafishH3 receptorhERG channelInhibitorinhibitorinhibit

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