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BMY 7378 dihydrochloride

CAS号

21102-95-4

分子式

C22H33Cl2N3O3

主要靶点

5-HT Receptor|Dopamine Receptor|Adrenergic Receptor

仅限科研使用

Cat No : CM10534

Print datasheet

Synonyms

α1D-adrenoceptor|α2C-adrenoceptor|spontaneously hypertensive rats|selective|Serotonin Receptor|Inhibitor|Beta Receptor|BMY 7378|BMY 7378 dihydrochloride|BMY 7378 Dihydrochloride|BMY7378|BMY-7378|BMY7378 Dihydrochloride|BMY-7378 Dihydrochloride|BMY7378 HCl|AdrenergicReceptor|Adrenergic Receptor|alpha 1-adrenoceptor|5-hydroxytryptamine Receptor|5HTReceptor|5HT Receptor|5-HT Receptor|5-HT1A receptor|5-HT1A|5-HT1C|Dopamine Receptor|DopamineReceptor|D2|inhibit

验证数据展示

  • CAS No.: 21102-95-4

    BMY 7378 dihydrochloride
    CAS#: 21102-95-4

产品信息

CAS号 21102-95-4
分子式 C22H33Cl2N3O3
主要靶点 5-HT Receptor|Dopamine Receptor|Adrenergic Receptor
主要通路 神经科学|G 蛋白偶联受体|G 蛋白偶联受体|神经科学|G 蛋白偶联受体|神经科学
分子量 458.42
纯度 99.08%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
别名 α1D-adrenoceptor|α2C-adrenoceptor|spontaneously hypertensive rats|selective|Serotonin Receptor|Inhibitor|Beta Receptor|BMY 7378|BMY 7378 dihydrochloride|BMY 7378 Dihydrochloride|BMY7378|BMY-7378|BMY7378 Dihydrochloride|BMY-7378 Dihydrochloride|BMY7378 HCl|AdrenergicReceptor|Adrenergic Receptor|alpha 1-adrenoceptor|5-hydroxytryptamine Receptor|5HTReceptor|5HT Receptor|5-HT Receptor|5-HT1A receptor|5-HT1A|5-HT1C|Dopamine Receptor|DopamineReceptor|D2|inhibit

靶点活性

α2C-adrenoceptor:6.54(pKi)|5-HT1A:8.3(pIC50)|α1D-adrenoceptor:8.2(pKi)|D2 receptor:7.4(pIC50)|5-HT1C:6.4(pIC50)

体内活性

BMY7378对α1D-肾上腺素受体亚型的作用有选择性{PKi: α1b-肾上腺素受体6.2（仓鼠）,7.2（人）；α1c-肾上腺素受体 6.1（牛）,6.6（人）；α1d-肾上腺素受体8.2（大鼠）,9.4（人）}。BMY7378对α2c-肾上腺素受体的选择性（pKi：6.54）是其他α2-肾上腺素受体的10倍。在大鼠中缝背核中,BMY7378（1-30 nM）具有剂量依赖性的抑制作用。

体外活性

在大鼠体内,BMY7378（0.25-5 mg/kg,s.c.）剂量依赖性降低8-OH-DPAT（0.75 mg/kg,s.c.）诱导的前爪踩踏和头部摇晃.在麻醉大鼠的腹侧海马体中,大鼠体内微量渗析检测显示,BMY7378使5-HT释放出现剂量依赖性的显著减少.BMY7378 (pA2为8.67)与去甲肾上腺素作用可使大鼠主动脉收缩,效果比育亨宾 (pA2为6.62)高约100倍.BMY7378 (pA2：6.48)会拮抗人体隐静脉(α2C-肾上腺素受体)中去甲肾上腺素引起的收缩响应,效果比育亨宾(pA2为7.56)低10倍.

溶解度

H2O:84 mg/mL (183.24 mM);DMSO:85 mg/mL (185.42 mM);Ethanol:16 mg/mL (34.9 mM)

参考文献

1.Cleary L, et al. Auton Autacoid Pharmacol, 2005, 25(4), 135-141.
2.Goetz AS, et al. Eur J Pharmacol, 1995, 272(2-3), R5-6.
3.Greuel JM, et al. Eur J Pharmacol, 1992, 211(2), 211-219.
4.Sharp T, et al. Eur J Pharmacol, 1990, 176(3), 331-40.

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