EGIS-7625
EGIS-7625 is an orally active and selective competitive antagonist of 5-HT2B receptor, with a human Ki value of 1 nM. EGIS-7625 shows low affinity for 5-HT2A and 5-HT2C receptors. The pKi values of EGIS-7625 for human 5-HT2B, 5-HT2A and 5-HT2C are 9.0, 6.2 and 7.7, respectively. EGIS-7625 alleviates mCPP-induced hypoactivity.
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- CAS. Nr.: 755040-97-2
- Formel: C18H24Cl2N4O2
- Molecular Weight:399.31
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
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5-HT2A Receptor |
5-HT2B Receptor |
5-HT2C Receptor |
5-HT2B Receptor 9.0 (pKi) |
5-HT2A Receptor 6.2 (pKi) |
5-HT2C Receptor 7.7 (pKi) |
EGIS-7625 (1-10 nM) acts as a potent competitive antagonist of 5-HT2B receptor-mediated contraction in rat fundus strips, with a pA2 value of 9.4[1].
EGIS-7625 (1-30 μM; 30 minutes) acts as a weak competitive antagonist of 5-HT2A receptor-mediated contraction in rabbit pulmonary artery strips, with a pA2 value of 6.7[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
EGIS-7625 (3-30 mg/kg; p.o.; single administration) antagonizes mCPP-induced 5-HT2C receptor-mediated hypoactivity in rats at the highest dose of 30.0 mg/kg, while no significant effects are observed at lower doses[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Wistar (male, 180-240 g) rats[1]
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Dosage:3, 10, 30 mg/kg
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Administration:p.o.; single dose
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Result:Significantly diminished mCPP-induced hypomotility at 30 mg/kg p.o.
Did not produce a significant effect at 3.0 mg/kg and 10.0 mg/kg p.o.
Chemical Information
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CAS. Nr. 755040-97-2
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Molecular Weight 399.31
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Formel C18H24Cl2N4O2
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SMILES
NC1=CC(N2CCN(CC3=CC=CC=C3)CC2)=C([N+]([O-])=O)C=C1C.Cl.Cl
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
EGIS-7625 Related Classifications
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