(1S,2R)-N1-(3,4-二氯苯基)环己烷-1,2-二甲酰胺
- CAS号:1445605-23-1
- 英文名:Lu AF21934
- 中文名:(1S,2R)-N1-(3,4-二氯苯基)环己烷-1,2-二甲酰胺
- CBNumber:CB53129361
- 分子式:C14H16Cl2N2O2
- 分子量:315.2
- MOL File:1445605-23-1.mol
- 沸点 :577.6±50.0 °C(Predicted)
- 密度 :1.386±0.06 g/cm3(Predicted)
- 储存条件 :Store at -20°C
- 溶解度 :≥31.5 mg/mL in DMSO; insoluble in H2O; ≥5.03 mg/mL in EtOH with ultrasonic
- 形态 :solid
- 酸度系数(pKa) :13.23±0.70(Predicted)
- 颜色 :White to off-white
(1S,2R)-N1-(3,4-二氯苯基)环己烷-1,2-二甲酰胺性质、用途与生产工艺
- 生物活性 Lu AF21934 是选择性和脑渗透性的 mGlu4 受体正变构调节剂,对 mGlu4 受体的 EC50 为 500。
-
靶点
mGlu4 Receptor
500 nM (EC 50 )
-
体内研究
Lu AF21934 treatment shows a dose-dependent anxiolytic-like effect in the stress-induced hyperthermia, four-plate, and marble-burying tests. The anti-hyperthermic effect of Lu AF21934 (5 mg/kg) in the SIH test is inhibited by the benzodiazepine receptor antagonist flumazenil (10 mg/kg) and is not serotonin dependent. Lu AF21934 does not produce antidepressant-like effects in the tail suspension test in mice; however, it decreases the basal locomotor activity of mice that are not habituated to activity cages. Lu AF21934 (0.5-5 mg/kg sc) does not influence tremor but at doses of 0.5 and 2.5 mg/kg reverses harmaline-induced hyperactivity. Lu AF21934 at a dose of 2.5 mg/kg potentiates the inhibitory influence of harmaline on the exploratory activity and AP1 during the first 30 min of the measurement and counteracts the harmaline-increased basic activity during the period of 30-90 min. Lu AF21934 (0.1-5 mg/kg) dose-dependently inhibits hyperactivity induced by MK-801 or amphetamine. It also antagonizes head twitches and increases frequency of spontaneous excitatory postsynaptic currents in brain slices, induced by DOI.
- 更新日期:2025/02/08
- 产品编号:HY-100366
- 产品名称:(1S,2R)-N1-(3,4-二氯苯基)环己烷-1,2-二甲酰胺 Lu AF21934
- CAS编号:1445605-23-1
- 包装:5mg
- 价格:850元
- 更新日期:2025/02/08
- 产品编号:HY-100366
- 产品名称:(1S,2R)-N1-(3,4-二氯苯基)环己烷-1,2-二甲酰胺 Lu AF21934
- CAS编号:1445605-23-1
- 包装:10mM * 1mLin DMSO
- 价格:935元
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