2769156-00-3
2769156-00-3 structure
- Name: MAO-A/5-HT2AR-IN-1
- Chemical Name: MAO-A/5-HT2AR-IN-1
- CAS Number: 2769156-00-3
- Molecular Formula: C30H28FN3O2
- Molecular Weight: 481.56
- Catalog: Signaling Pathways GPCR/G Protein 5-HT Receptor
- Create Date: 2022-11-21 17:52:05
- Modify Date: 2024-08-09 18:35:55
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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[1].
| Name | MAO-A/5-HT2AR-IN-1 |
|---|
| Description | 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[1]. |
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| Related Catalog | |
| Target |
MAO-A:0.004 ± 0. μM (IC50) 5-HT2A Receptor:0.014 μM (IC50) MAO-B:1.05 ± 0.0 μM (IC50) |
| 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. |
| 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 |
| References |
| Molecular Formula | C30H28FN3O2 |
|---|---|
| Molecular Weight | 481.56 |