DU125530
DU125530 is a potent and selective5-HT1A receptor antagonist with Ki values of 0.7, 890, 1200, 240, 750, 1100 nM for 5-HT1A, 5-HT1B, 5-HT1D, 5-HT2A, 5-HT2C, 5-HT3, respectively. DU125530 shows antidepressant effects.
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- CAS. Nr.: 161611-99-0
- Formel: C23H26ClN3O5S
- Molecular Weight:491.99
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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
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Alle 5-HT Receptor Isoform-spezifische Produkte anzeigen
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Biologische Aktivität
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5-HT1A Receptor |
5-HT1B Receptor |
5-HT1D Receptor |
5-HT2A Receptor |
5-HT2C Receptor |
5-HT1A Receptor 0.7 nM (Ki) |
5-HT1B Receptor 890 nM (Ki) |
5-HT1C Receptor 1200 nM (Ki) |
5-HT2A Receptor 240 nM (Ki) |
5-HT2C Receptor 750 nM (Ki) |
5-HT3 Receptor 1100 nM (Ki) |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:wild-type mice[2]
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Dosage:3 mg/kg
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Administration:S.c.
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Result:Prevented the reduction of 5-HT release induced by 0.5 mg·kg−1 s.c. 8-OH-DPAT in WT mice, alone had no effect on the extracellular 5-HT concentration in mPFC of wild-type mice (WT) nor in 5-HT1A receptor knock-out mice (KO).
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 161611-99-0
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Molecular Weight 491.99
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Formel C23H26ClN3O5S
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SMILES
O=C(C1=C2C=CC=C1)N(CCCCN3CCN(C4=C5OCCOC5=CC(Cl)=C4)CC3)S2(=O)=O
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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
[1]. Mos J, et al. The putative 5-HT1A receptor antagonist DU125530 blocks the discriminative stimulus of the 5-HT1A receptor agonist flesinoxan in pigeons. Eur J Pharmacol. 1997 May 1;325(2-3):145-53. [Content Brief]
[2]. Scorza MC, et al. Preclinical and clinical characterization of the selective 5-HT(1A) receptor antagonist DU-125530 for antidepressant treatment. Br J Pharmacol. 2012 Nov;167(5):1021-34. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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