2. Neuronal Signaling GPCR/G Protein
  3. Monoamine Oxidase 5-HT Receptor
  4. MAO-A/5-HT2AR-IN-1

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.

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MAO-A/5-HT2AR-IN-1 Chemical Structure

MAO-A/5-HT2AR-IN-1 Chemical Structure

CAS No. : 2769156-00-3

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Based on 1 publication(s) in Google Scholar

MAO-A/5-HT2AR-IN-1 Related Antibodies

Top Publications Citing Use of Products

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MAO-A MAO-B

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5-HT1 Receptor 5-HT2 Receptor 5-HT3 Receptor 5-HT4 Receptor 5-HT5 Receptor 5-HT6 Receptor 5-HT7 Receptor 5-HT Receptor

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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].

IC50 & 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

MAO-A/5-HT2AR-IN-1 Related Antibodies

[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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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
Molecular Weight

481.56

Formula

C30H28FN3O2
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C1C2=C(C3=NC=CC4=CC(OCCCCN5CCN(CC5)C6=C(F)C=CC=C6)=CC1=C43)C=CC=C2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Purity & Documentation
References
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MAO-A/5-HT2AR-IN-1 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

MAO-A/5-HT2AR-IN-12769156-00-3Monoamine Oxidase5-HT ReceptorMAOSerotonin Receptor5-hydroxytryptamine ReceptorneurocytoprotectivePC12 cellsSH-SY5YL02depressionantidepressantInhibitorinhibitorinhibit

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