MAO-A/5-HT2AR-IN-1 (compound I14) 是一种有效的MAO-A和5-HT2AR双重抑制剂，其IC50分别为 0.004 和 0.014 μM。MAO-A/5-HT2AR-IN-1 是一种潜在的抗抑郁剂。
| 生物活性 | MAO-A/5-HT2AR-IN-1 (compound I14) is a potentMAO-Aand5-HT2ARdual inhibitor, withIC50values of 0.004 and 0.014 μM, respectively. MAO-A/5-HT2AR-IN-1 is a potential antidepressant agent[1]. |
| IC50& Target | MAO-A 0.004 ± 0. μM (IC50) | 5-HT2AReceptor 0.014 μM (IC50) | MAO-B 1.05 ± 0.0 μM (IC50) |
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体外研究
(In Vitro) | 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[1].
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[1].
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[1].
[1][1] | Cell Line: | PC12 cells | | Concentration: | 4.0, 2.0, 1.0, and 0.5 μM (and 500 μM CORT) | | Incubation Time: | 24 h | | Result: | Showed a significant protective effect on PC12 cells injury at different concentrations compared with the model group, where the best protective effect was observed at 0.5 μM. |
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体内研究
(In Vivo) | MAO-A/5-HT2AR-IN-1 (compound I14) (10 and 20 mg/kg) significantly ameliorates the depression-like behavior of mice[1].
MAO-A/5-HT2AR-IN-1 (0-1 μM, for 7 days) improves zebrafish locomotion and the depression-like behavior[1].
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[1].
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[1].
| Animal Model: | ICR male mice (8–10 weeks old, weight 18-20 g)[1] | | 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)[1] | | 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)[1] | | 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[1].
| parameter | 2 mg/kg (i.v.) | 10 mg/kg (i.g.) | | Tmax(h) | 0.08 ± 0.00 | 1.33 ± 0.33 | | Cmax(ng/mL) | 673.33 ± 25.41 | 99.67 ± 6.01 | | AUC0-24(ng/mL*h) | 2230.67 ± 153.78 | 490.67 ± 70.43 | | AUC0-inf(ng/mL*h) | 2322.67 ± 178.02 | 504.00 ± 71.08 | | t1/2(h) | 6.31 ± 0.55 | 5.22 ± 0.79 | | CL (mL/min/kg) | 14.54 ± 1.20 | 345.69 ± 53.40 | | MRTinf(h) | 4.19 ± 0.14 | 4.94 ± 0.36 | | F (%) | | 4.40 |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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