1-(3,4-二氯苯基)-3-氮杂双环[3.1.0]己烷

生物活性靶点体内研究 1-(3,4-二氯苯基)-3-氮杂双环[3.1.0]己烷试剂级价格

CAS号:66504-40-3
英文名:1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane
中文名:1-(3,4-二氯苯基)-3-氮杂双环[3.1.0]己烷
CBNumber:CB32561096
分子式:C11H11Cl2N
分子量:228.12
MOL File:66504-40-3.mol

1-(3,4-二氯苯基)-3-氮杂双环[3.1.0]己烷化学性质

沸点 :324.4±37.0 °C(Predicted)
密度 :1.371
储存条件 :Store at -20°C
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

1-(3,4-二氯苯基)-3-氮杂双环[3.1.0]己烷性质、用途与生产工艺

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.