H77-77
H77-77 is a selective MAO-A inhibitor with blood-brain barrier permeability, exhibiting an IC50 of 7.4 μM against rat MAO-A. H77-77 accumulates via uptake by serotonergic and noradrenergic neurons. H77-77 releases norepinephrine and serotonin from intracellular neuronal storage sites. H77-77 can be used in studies related to neurological disorders.
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- CAS No.: 21618-99-5
- Formule: C10H15NO
- Masse moléculaire:165.24
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
IC50 & Target
[1]|
rMAO-A 7.4 μM (IC50) |
In Vitro
H77-77 selectively inhibits rat brain mitochondrial MAO-A with an IC50 of 7.4 μM, while no detectable inhibitory effect on MAO-B is observed even at concentrations as high as 500 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley (male, 160-200 g)[1]
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Dosage:1.25 mg/kg; 2.5 mg/kg; 5 mg/kg; 10 mg/kg
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Administration:s.c.
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Result:Produced 35% inhibition of MAO inside serotonergic neurons in the hypothalamus, with minimal inhibition outside these neurons at 1.25 mg/kg s.c.
Produced 78% inhibition of MAO inside serotonergic neurons and 15% inhibition outside these neurons, and 60% inhibition inside noradrenergic neurons and 11% inhibition outside these neurons at 10 mg/kg s.c.
Reduced MAO inhibition inside serotonergic neurons to 27% at the 10 mg/kg s.c. dose when pretreated with norzimeldine.
Reduced MAO inhibition inside noradrenergic neurons to 20% at the 10 mg/kg s.c. dose when pretreated with CPP199.
Showed no selective inhibition of MAO inside dopaminergic neurons in the striatum.
Chemical Information
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CAS No. 21618-99-5
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Masse moléculaire 165.24
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Formule C10H15NO
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SMILES
OC1=CC(=CC=C1C)CC(N)C
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocole
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Transepithelial/transendothelial electrical resistance assay
TEER measures electrical resistance across epithelial or endothelial monolayers cultured on permeable supports, and the readout reflects ionic conductance through the cell barrier, especially the paracellular pathway regulated by junctional integrity. TEER can be measured without destroying the monolayer and is commonly used before or during transport, permeability, barrier-disruption, and barrier-maturation experiments. TEER values are influenced by biological maturation and technical conditions; reported factors include temperature, medium formulation, passage number, electrode geometry, membrane properties, and junctional length during early monolayer maturation. Therefore, TEER should be interpreted with blank-insert subtraction, area normalization, repeated readings, and, when possible, orthogonal barrier readouts such as FITC-dextran flux or tight-junction staining.
Pureté et documentation
Références
[1]. Fagervall I, et al. Selective inhibition by 4,alpha-dimethyl-m-tyramine (H77/77) and 4-methyl-alpha-ethyl-m-tyramine (H75/12) of the monoamine oxidase within serotonergic and noradrenergic neurons in the rat brain. Naunyn-Schmiedeberg's archives of pharmacology. 1988 Aug;338(2):143-7. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
H77-77 Related Classifications
HY-124331 Related Classifications
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