产品说明书

Amoxapine

Print
Chemical Structure| 14028-44-5 同义名 : CL-67772
CAS号 : 14028-44-5
货号 : A605472
分子式 : C17H16ClN3O
纯度 : 98%
分子量 : 313.781
MDL号 : MFCD00069210
存储条件：

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 7 mg/mL(22.31 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

5% DMSO+corn oil 1 mg/mL

生物活性
靶点

  • GlyT1

    GlyT1b, IC50:1 mM

  • GlyT2

    GlyT2a, IC50:92 μM
描述 Amoxapine is a tricyclic antidepressant that inhibits norepinephrine and serotonin transport by binding to respective receptors with KD values of 16 and 58 nM, respectively[3]. Amoxapine also showed a selective inhibitory effect on glycine transporter 2a (GlyT2a) transport with an IC50 value of 92 ± 8 μM[4]. In mice bearing CT-26 cells, oral administration of amoxapine twice per day for 12 days successfully delayed or suppressed CPT-11-induced diarrhea and suppressed tumor growth at a dose of 1 or 5 mg/kg/day[5].
作用机制 Amoxapine is a tricyclic antidepressant that selectively inhibits GlyT2a. It also acts as a competitive inhibitor for both glycine and chloride[4].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00704860 Major Depression Phase 4 Completed - Canada, Ontario ... 展开 >> University of Ottawa Institute of Mental Health Research Ottawa, Ontario, Canada, K1Z 7K4 收起 <<
NCT00000317 Cocaine-Related Disorders ... 展开 >> Substance-Related Disorders 收起 << Phase 2 Completed - United States, New York ... 展开 >> NYS Psychiatric Institute New York, New York, United States, 10032 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.19mL

0.64mL

0.32mL

15.93mL

3.19mL

1.59mL

31.87mL

6.37mL

3.19mL
参考文献

[1]Obers S, Staudacher I, et al. Multiple mechanisms of hERG liability: K+ current inhibition, disruption of protein trafficking, and apoptosis induced by amoxapine. Naunyn Schmiedebergs Arch Pharmacol. 2010 May;381(5):385-400.

[2]Núnez E, Lopez-Corcuera B, et al. Differential effects of the tricyclic antidepressant amoxapine on glycine uptake mediated by the recombinant GLYT1 and GLYT2 glycine transporters. Br J Pharmacol. 2000 Jan;129(1):200-6.

[3]Tatsumi M, Groshan K, Blakely RD, Richelson E. Pharmacological profile of antidepressants and related compounds at human monoamine transporters. Eur J Pharmacol. 1997;340(2-3):249-258. doi:10.1016/s0014-2999(97)01393-9

[4]Núñez E, López-Corcuera B, Vázquez J, Giménez C, Aragón C. Differential effects of the tricyclic antidepressant amoxapine on glycine uptake mediated by the recombinant GLYT1 and GLYT2 glycine transporters. Br J Pharmacol. 2000;129(1):200-206. doi:10.1038/sj.bjp.0703049

[5]Kong R, Liu T, Zhu X, et al. Old drug new use--amoxapine and its metabolites as potent bacterial β-glucuronidase inhibitors for alleviating cancer drug toxicity. Clin Cancer Res. 2014;20(13):3521-3530. doi:10.1158/1078-0432.CCR-14-0395