Piroheptine
Piroheptine is a muscarinic acetylcholine receptor (mAChR) antagonist and dopamine reuptake inhibitor. Piroheptine blocks the high-affinity dopamine transport system, prevents MPP+ uptake into dopaminergic neurons, and exerts anticholinergic activity. Piroheptine completely prevents MPTP (HY-W114750)-induced loss of striatal dopamine and DOPAC, and increases striatal dopamine levels. Piroheptine can be used in studies related to Parkinson's disease.
For research use only. We do not sell to patients.
- CAS No.: 16378-21-5
- Formula: C22H25N
- Molecular Weight:303.45
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
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Biological Activity
Description
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J (male, 8-week-old, 20-30 g, Parkinsonism induced via 4 intraperitoneal injections of 10 mg/kg MPTP at 1-hour intervals)[1]
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Dosage:20 mg/kg
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Administration:i.p.; 30 minutes before each of 4 MPTP injections (1 hour apart); single treatment (piroheptine-alone group)
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Result:Completely prevented MPTP-induced striatal dopamine loss, resulting in levels of 9.5 μg/g wet tissue.
Completely prevented MPTP-induced striatal DOPAC loss, resulting in levels of 0.8 μg/g wet tissue.
Increased striatal dopamine content to 10.2 μg/g wet tissue (approximately 10% higher than saline controls) when administered alone.
Chemical Information
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CAS No. 16378-21-5
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Molecular Weight 303.45
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Formula C22H25N
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SMILES
C=1C=CC2=C(C1)C(C=3C=CC=CC3CC2)=C4CCN(CC)C4C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Human pluripotent stem cell midbrain dopaminergic neuron differentiation
Human pluripotent stem cells are directed toward midbrain dopaminergic neurons by first inducing a neural floor-plate-like progenitor state, then patterning cells with ventralizing SHH signaling and midbrain/WNT-FGF cues, and finally maturing progenitors into neurons expressing dopaminergic markers such as TH, NURR1/NR4A2, PITX3, DAT/SLC6A3, VMAT2/SLC18A2, GIRK2/KCNJ6, FOXA2, LMX1A, and EN1. The main readouts are loss of pluripotency, acquisition of FOXA2+/LMX1A+ midbrain floor-plate progenitors, emergence of βIII-tubulin+/MAP2+ neurons, and production of TH+ dopaminergic neurons with molecular, dopamine-release, and electrophysiological features of midbrain dopaminergic identity.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Piroheptine Related Classifications
HY-W683866 Related Classifications
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