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My CartCAS：14028-44-5
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：HPLC≥98%
Appearance：White to yellow Solid
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| CAS | 14028-44-5 |
| Name | Amoxapine |
| Molecular Formula | C17H16ClN3O |
| Molecular Weight | 313.78 |
| Solubility | Soluble in DMSO |
| Purity | HPLC≥98% |
| Appearance | White to yellow Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| EC | EINECS 237-867-1 |
| MDL | MFCD00069210 |
| SMILES | ClC1=CC=C(OC2=CC=CC=C2N=C3N4CCNCC4)C3=C1 |
| InChIKey | QWGDMFLQWFTERH-UHFFFAOYSA-N |
| InChI | InChI=1S/C17H16ClN3O/c18-12-5-6-15-13(11-12)17(21-9-7-19-8-10-21)20-14-3-1-2-4-16(14)22-15/h1-6,11,19H,7-10H2 |
| PubChem CID | 2170 |
| Target Point | GlyT2a;GlyT1b |
| Passage | Membrane Transporter&Ion Channel |
| Background | It has strong antidepressant activity and invigorating activity, is the main component of antidepressant, and can be used for related research. |
| Biological Activity | Amoxapine (CL 67772)是一种三环类Dibenzoxazepine（N-aryl piperazine），与一些其他的三环类抗抑郁药作用相似，Amoxapine抑制GLYT2a的的运输活性，IC50为92 μM。[1] |
| In Vitro | Amoxapine对GLYT2a选择性抑制，在人类胚胎肾293细胞中，表现出比同种型GLYT1b多出10倍的抑制效果。Amoxapine表现为甘氨酸和氯化物的竞争性抑制剂，也是一个关于钠的混合型抑制剂。[1] Amoxapine引起急性的hERG阻塞，在卵母细胞中IC50为21.6 mM，HEK 293细胞中IC50为5.1 mM。Amoxapine阻滞反向频变，而且会引起加速的、向左移位的失活。Amoxapine的应用导致HEK 293细胞中hERG运输到细胞膜表面的缓慢减少，其IC50为15.3 mM。[2] |
| In Vivo | Amoxapine(10 mg/kg i.p.，每天)不影响强啡肽，P物质和缩胆囊素的水平，但显著增强了大鼠脊髓、大脑皮层和下丘脑中亮氨酸-脑啡肽的水平。Amoxapine(10 mg/kg i.p.，每天)不会引起大鼠大脑皮层阿片受体的改变，但是δ阿片受体和μ阿片受体结合位点的密度在脊髓中增加，在下丘脑中降低。[3] Amoxapine(1 mg/kg，5 mg/kg以及10 mg/kg; i.p.)，尤其在低剂量下，能够减少异相睡眠并增加慢波睡眠。Amoxapine(10 mg/kg; i.p.)在整个治疗中会引起异相睡眠的持续降低，然而在该睡眠状态下，能够观察到关于cericlamine抑制效果的耐受性。[4]Amoxapine降低自发活动，引起眼睑下垂和强直性昏厥，通过改变猴子辨别的回避行为而抑制apomorphine不断阵痛和amphetamine刻板行为。[5] |
| Data Literature Source | [1] Nez E，et al. Br J Pharmacol，2000，129(1)，200-206. [2] Obers S，et al. Naunyn Schmiedebergs Arch Pharmacol，2010，381(5)，385-400. [3] Hamon M，et al. Neuropharmacology，1987，26(6)，531-539. [4] Maudhuit C，et al. Neuropharmacology，1994，33(8)，1017-1025. [5] Greenblatt EN，et al. Arch Int Pharmacodyn Ther，1978，233(1)，107-135. |
| Unit | Bottle |
| Specification | 100mg 200mg 500mg |
有较强的抗抑郁活性和精神振奋活性，是抗抑郁药的主要成分，可用于相关研究。
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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