Fipamezole
Fipamezole (MPV 1730; JP-1730) is a potent and orally active α2-adrenergic receptor antagonist with Ki values of 9.2 nM, 17 nM, and 55 nM for human α2A, α2B, and α2C, receptors, respectively. Fipamezole is an anti-dyskinetic agent, and can be used for the study of Parkinson's disease.
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- CAS No.: 150586-58-6
- 화학식: C14H15FN2
- 분자량:230.28
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보관:
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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All Adrenergic Receptor Isoforms
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Biological Activity
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human α2A-adrenoceptor 9.2 nM (Ki) |
human α2B-adrenoceptor 17 nM (Ki) |
human α2C-adrenoceptor 55 nM (Ki) |
In functional assays, the potent antagonist properties of Fipamezole (JP-1730) are demonstrated by its ability to reduce adrenaline-induced 35S-GTPγS binding with KB values of 8.4 nM, 16 nM, 4.7 nM at human α2A, α2B, and α2C receptors, respectively. Fipamezole also has moderate affinity at histamine H1 and H3 receptors and the serotonin (5-HT) transporter (IC50 of 100 nM-1 μM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Adult common marmosets (Callithrix jacchus, 300-345 g) injected with MPTP hydrochloride (2 mg/kg) and L-DOPA (8 mg/kg)[1]
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Dosage:1 mg/kg, 3 mg/kg, 10 mg/kg
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Administration:po; once
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Result:Significantly reduced L-DOPA-induced dyskinesia.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 150586-58-6
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분자량 230.28
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화학식 C14H15FN2
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SMILES
FC1=CC=C2C(CC(C2)(CC)C3=CN=CN3)=C1
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Synonyms
MPV 1730; JP-1730
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Fipamezole Related Classifications
HY-106444 Related Classifications
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