产品
编 号：F755898
分子式：C30H28FN3O2
分子量：481.56
分子式：C30H28FN3O2
分子量：481.56
产品类型
规格
价格
是否有货
1mg
询价
询价
5mg
询价
询价
10mg
询价
询价
结构图
CAS No: 2769156-00-3
产品详情
生物活性：
MAO-A/5-HT2AR-IN-1 (compound I14) is a potent MAO-A and 5-HT2AR dual inhibitor, with IC50 values of 0.004 and 0.014 μM, respectively. MAO-A/5-HT2AR-IN-1 is a potential antidepressant agent.
体内研究：
MAO-A/5-HT2AR-IN-1 (compound I14) (10 and 20 mg/kg) significantly ameliorates the depression-like behavior of mice. MAO-A/5-HT2AR-IN-1 (0-1 μM, for 7 days) improves zebrafish locomotion and the depression-like behavior.MAO-A/5-HT2AR-IN-1 is able to repair the damage of mice hippocampal neuronal cells and reduce the expression of 5-HT2AR in mice brain tissue. MAO-A/5-HT2AR-IN-1 (2 mg/kg (i.v.) 10 mg/kg (i.g.); once) has a good clearance rate of 345.69 mL/min/kg in rats.Animal Model:ICR male mice (8?10 weeks old, weight 18-20 g)
Dosage:10 mg/kg, 20 mg/kg
Administration:For 2 weeks
Result:Significantly improved depression-like behavior in mice, with the low dose group (10 mg/kg) being more potent than with the positive drug (Flu, 20 mg/kg). Had no relevant toxic effects on the liver, kidney, lung, and spleen of mice during the treatment period.
Animal Model:Zebrafish (AB strain, Reserpine-induced zebrafish depression model)
Dosage:0.1, 0.5, 1 μM
Administration:Given 24 h after reserpine, for 7 days.
Result:Showed that zebrafish in the I14 administered group moved significantly more distance, faster, and spent significantly more time in the upper part compared to the model group.
Animal Model:Sprague-Dawley rats (male)
Dosage:2 mg/kg (i.v.) 10 mg/kg (i.g.)
Administration:IV, IG; once (Pharmacokinetic Analysis)
Result:Pharmacokinetic Parameters of MAO-A/5-HT2AR-IN-1 in male Sprague-Dawley rats.parameter2 mg/kg (i.v.) 10 mg/kg (i.g.)
Tmax (h)0.08 ± 0.001.33 ± 0.33
Cmax (ng/mL)673.33 ± 25.4199.67 ± 6.01
AUC0-24 (ng/mL·h)2230.67 ± 153.78490.67 ± 70.43
AUC0-inf (ng/mL·h)2322.67 ± 178.02504.00 ± 71.08
t1/2 (h)6.31 ± 0.555.22 ± 0.79
CL (mL/min/kg)14.54 ± 1.20345.69 ± 53.40
MRTinf (h)4.19 ± 0.144.94 ± 0.36
F (%)4.40
体外研究：
MAO-A/5-HT2AR-IN-1 (compound I14) (0-4 μM, 24 h) exhibits a significant neurocytoprotective effect on the CORT-induced cell depression model. MAO-A/5-HT2AR-IN-1 is able to occupy the active cavity of 5-HT2AR and MAO-A with multiple hydrogen bonding forces and π–π stacking interaction.MAO-A/5-HT2AR-IN-1 exhibits low proliferation inhibitory activities against L02 cells (IC50 > 100 μM), SH-SY5Y (IC50 > 10 μM) and PC12 (IC50 > 10 μM), indicating it has a good safety profile.
MAO-A/5-HT2AR-IN-1 (compound I14) is a potent MAO-A and 5-HT2AR dual inhibitor, with IC50 values of 0.004 and 0.014 μM, respectively. MAO-A/5-HT2AR-IN-1 is a potential antidepressant agent.
体内研究：
MAO-A/5-HT2AR-IN-1 (compound I14) (10 and 20 mg/kg) significantly ameliorates the depression-like behavior of mice. MAO-A/5-HT2AR-IN-1 (0-1 μM, for 7 days) improves zebrafish locomotion and the depression-like behavior.MAO-A/5-HT2AR-IN-1 is able to repair the damage of mice hippocampal neuronal cells and reduce the expression of 5-HT2AR in mice brain tissue. MAO-A/5-HT2AR-IN-1 (2 mg/kg (i.v.) 10 mg/kg (i.g.); once) has a good clearance rate of 345.69 mL/min/kg in rats.Animal Model:ICR male mice (8?10 weeks old, weight 18-20 g)
Dosage:10 mg/kg, 20 mg/kg
Administration:For 2 weeks
Result:Significantly improved depression-like behavior in mice, with the low dose group (10 mg/kg) being more potent than with the positive drug (Flu, 20 mg/kg). Had no relevant toxic effects on the liver, kidney, lung, and spleen of mice during the treatment period.
Animal Model:Zebrafish (AB strain, Reserpine-induced zebrafish depression model)
Dosage:0.1, 0.5, 1 μM
Administration:Given 24 h after reserpine, for 7 days.
Result:Showed that zebrafish in the I14 administered group moved significantly more distance, faster, and spent significantly more time in the upper part compared to the model group.
Animal Model:Sprague-Dawley rats (male)
Dosage:2 mg/kg (i.v.) 10 mg/kg (i.g.)
Administration:IV, IG; once (Pharmacokinetic Analysis)
Result:Pharmacokinetic Parameters of MAO-A/5-HT2AR-IN-1 in male Sprague-Dawley rats.parameter2 mg/kg (i.v.) 10 mg/kg (i.g.)
Tmax (h)0.08 ± 0.001.33 ± 0.33
Cmax (ng/mL)673.33 ± 25.4199.67 ± 6.01
AUC0-24 (ng/mL·h)2230.67 ± 153.78490.67 ± 70.43
AUC0-inf (ng/mL·h)2322.67 ± 178.02504.00 ± 71.08
t1/2 (h)6.31 ± 0.555.22 ± 0.79
CL (mL/min/kg)14.54 ± 1.20345.69 ± 53.40
MRTinf (h)4.19 ± 0.144.94 ± 0.36
F (%)4.40
体外研究：
MAO-A/5-HT2AR-IN-1 (compound I14) (0-4 μM, 24 h) exhibits a significant neurocytoprotective effect on the CORT-induced cell depression model. MAO-A/5-HT2AR-IN-1 is able to occupy the active cavity of 5-HT2AR and MAO-A with multiple hydrogen bonding forces and π–π stacking interaction.MAO-A/5-HT2AR-IN-1 exhibits low proliferation inhibitory activities against L02 cells (IC50 > 100 μM), SH-SY5Y (IC50 > 10 μM) and PC12 (IC50 > 10 μM), indicating it has a good safety profile.
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