66504-40-3
中文名称
1-(3,4-二氯苯基)-3-氮杂双环[3.1.0]己烷
英文名称
1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane
CAS
66504-40-3
分子式
11H11Cl2N
分子量
228.118
MOL 文件
66504-40-3.mol
66504-40-3 结构式
基本信息
中文别名
1-(3,4-二氯苯基)-3-氮杂二环[3.1.0]己烷1-(3,4-二氯苯基)-3-氮杂双环[3.1.0]己烷
英文别名
DOV216303DOV-216,303 (Free Base)
1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane
3-Azabicyclo[3.1.0]hexane, 1-(3,4-dichlorophenyl)-
1-(3,4-dichlorophenyl)-3-azabicyclo(3.1.0)hexane 11H11Cl2N
物理化学性质
沸点324.4±37.0 °C(Predicted)
密度1.371
储存条件-20°C储存
溶解度DMSO : ≥ 125 mg/mL (547.96 mM);Water : < 0.1 mg/mL (insoluble)
酸度系数(pKa)10.45±0.40(Predicted)
形态Oil
颜色Colorless to light yellow
常见问题列表
生物活性
DOV-216,303 (Free Base) 是有效的 5-羟色胺、去甲肾上腺素、多巴胺再摄取的三重抑制剂，其对 hSERT、hNET 和 hDAT 的 IC50 值分别为 14 nM，20 nM和78 nM。在嗅球切除大鼠模型中，可增加前额皮质中单胺的释放及具有抗抑郁的作用。靶点
IC50: 14 nM (serotonin), 20 nM (norepinephrine), 78 nM (dopamine).
体内研究
Acute treatment of DOV-216,303 (20 mg/kg, i.p.) significantly increases dopamine, norepinephrine and serotonin levels in both OBX and Sham animals.
Chronic treatment with DOV 216,303 (20 mg/kg, i.p., for 17 days) increases extracellular concentrations of dopamine, norepinephrine and serotonin in the medial prefrontal cortex of both OBX and Sham animals and significantly increases extracellular baseline serotonin concentrations.
| Animal Model: | Male Sprague Dawley rats weighing between 290 and 350 g at time of OBX or Sham surgery. |
| Dosage: | 20 mg/kg. |
| Administration: | I.P. daily for 17days. |
| Result: | Increased extracellular concentrations of dopamine, norepinephrine and serotonin in the medial prefrontal cortex of both OBX and Sham animals and significantly increased extracellular baseline serotonin concentrations. |
| Animal Model: | Male Sprague Dawley rats weighing between 290 and 350 g at time of OBX or Sham surgery. |
| Dosage: | 20 mg/kg. |
| Administration: | I.P. once. |
| Result: | Significant increases in dopamine, norepinephrine and serotonin levels were measured in both OBX and Sham animals. |