2. GPCR/G Protein Neuronal Signaling
  3. Adrenergic Receptor
  4. 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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Fipamezole Chemical Structure

Fipamezole Chemical Structure

CAS No. : 150586-58-6

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Fipamezole Related Antibodies

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Description

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[1].

IC50 & Target[1]

human α2A-adrenoceptor

9.2 nM (Ki)

human α2B-adrenoceptor

17 nM (Ki)

human α2C-adrenoceptor

55 nM (Ki)

In Vitro

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.

Fipamezole Related Antibodies
In Vivo

In the MPTP-lesioned marmoset, Fipamezole (1-10 mg/kg; po; once) significantly reduces L-dopa-induced dyskinesia without compromising the anti-parkinsonian action of L-DOPA (HY-N0304)[1].

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

Animal Model: Adult common marmosets (Callithrix jacchus, 300-345 g) injected with MPTP hydrochloride (2 mg/kg) and L-DOPA (8 mg/kg)[1]
Dosage: 1 mg/kg, 3 mg/kg, 10 mg/kg
Administration: po; once
Result: Significantly reduced L-DOPA-induced dyskinesia.
Molecular Weight

230.28

Formula

C14H15FN2
CAS No.
SMILES

FC1=CC=C2C(CC(C2)(CC)C3=CN=CN3)=C1
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Purity & Documentation
References
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Fipamezole 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:

Fipamezole150586-58-6MPV 1730 JP-1730MPV1730MPV-1730JP1730JP 1730JP-1730Adrenergic ReceptorBeta Receptorα2-adrenergic receptor antagonistanti-dyskinetic agentParkinson's diseaseInhibitorinhibitorinhibit

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