CAS |
No.386750-22-7 |
中文名称 |
琥珀酸去甲文拉法辛 |
英文名称 |
Desvenlafaxine Succinate |
别名 |
O-Desmethylvenlafaxine succinate hydrate;WY 45233 Succinate |
分子式 |
C20H33NO7 |
分子量 |
399.48 |
溶解性 |
Soluble in DMSO ≥3mg/mL |
纯度 |
≥98% |
外观(性状) |
White to off-white Solid |
储存条件 |
Powder:2-8℃,2 years;Insolvent(母液):-20℃,6 months;-80℃,1 year |
MDL |
MFCD09970707 |
SMILES |
CN(C)CC(C1=CC=C(C=C1)O)C2(CCCCC2)O.C(CC(=O)O)C(=O)O.O |
InChIKey |
PWPDEXVGKDEKTE-UHFFFAOYSA-N |
InChI |
InChI=1S/C16H25NO2.C4H6O4.H2O/c1-17(2)12-15(13-6-8-14(18)9-7-13)16(19)10-4-3-5-11-16;5-3(6)1-2-4(7)8;/h6-9,15,18-19H,3-5,10-12H2,1-2H3;1-2H2,(H,5,6)(H,7,8);1H2 |
PubChem CID |
6918664 |
靶点 |
Serotonin Transporter;Adrenergic Receptor |
通路 |
Neuronal Signaling;Endocrinology & Hormones;GPCR & G Protein |
背景说明 |
是能透过血脑屏障的 5-HT 和 去甲肾上腺素 (norepinephrine) 再摄取的抑制剂。 |
生物活性 |
Desvenlafaxine Succinate 是文拉法辛的活性代谢产物,是一种血清素-去甲肾上腺素再摄取抑制剂,对 hSERT 和 hNET 的 IC50值分别为47.3 nM和531.3 nM。与人多巴胺(DA)转运体的结合亲和力较弱(100 μM 时抑制率为 62%)。[1-2] |
IC50 |
hSERT: 47.3nM;hNET(IC50): 531.3nM[1] |
In Vitro |
Inhibition of [3H]5-HT or [3H]NE uptake by desvenlafaxine succinate(DVS)for the hSERT or hNET produced IC50 values of 47.3 +/- 19.4 and 531.3 +/- 113.0 nM.[1] |
In Vivo |
DVS(30 mg/kg orally)significantly increased extracellular NE levels compared with baseline in the male rat hypothalamus. DVS showed weak binding affinity(62% inhibition at 100 microM)at the human dopamine(DA)transporter.[1] |
数据来源文献 |
[1]. Deecher DC,et al. Desvenlafaxine succinate: A new serotonin and norepinephrine reuptake inhibitor. J Pharmacol Exp Ther. 2006 Aug;318(2):657-65. |
规格 |
100mg 500mg |
单位 |
瓶 |