UNC9994
Based on 3 publication(s) in Google Scholar
UNC9994, an analog of Aripiprazole, is a functionally selective β-arrestin-biased dopamine D2 receptor (D2R) agonist with EC50 <10 nM for β-arrestin-2 recruitment to D2 receptors. UNC9994 is simultaneously partial agonists of β-arrestin-2 translocation and antagonists of Gi-regulated cAMP production. Antipsychotic Activity.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 98.06%
- CAS. Nr.: 1354030-51-5
- Formel: C21H22Cl2N2OS
- Molecular Weight:421.38
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biologische Aktivität
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Chemical Information
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) UNC9994
MoreAlle Dopamine Receptor Isoform-spezifische Produkte anzeigen
MoreAlle 5-HT Receptor Isoform-spezifische Produkte anzeigen
MoreAlle Histamine Receptor Isoform-spezifische Produkte anzeigen
MoreAlle Arrestin Isoform-spezifische Produkte anzeigen
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Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
D2 Receptor 79 nM (Ki) |
D3 Receptor 17 nM (Ki) |
D4 Receptor 138 nM (Ki) |
5-HT2A Receptor 140 nM (Ki) |
5-HT2B Receptor 25 nM (Ki) |
5-HT2C Receptor 512 nM (Ki) |
5-HT1F Receptor 26 nM (Ki) |
H1 Receptor 2.1 nM (Ki) |
In Vitro
UNC9994 displays a lower binding affinity (Ki=79 nM) to D2R than UNC9975, UNC0006, and aripiprazole. At serotonin (as known as 5-HT) receptors, UNC9994 displays moderate to high binding affinities (Ki=25-512 nM) for 5HT2A, 5HT2B, 5HT2C, and 5HT1A, but is significantly less potent in functional assays (Ca2+ mobilization FLIPR or cAMP biosensor). UNC9994 is an antagonist at 5HT2A and 5HT2B and agonists at 5HT2C and 5HT1A. UNC9994 has relatively high affinities to H1-histamine receptor (Ki=2.4 nM) but is less potent antagonists in H1 functional assays[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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 wild-type and β-arrestin-2 knockout mice (phencyclidine-induced hyperlocomotion)[1]
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Dosage:2 mg/kg
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Administration:I.p. followed 30 min later with 6 mg/kg phencyclidine
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Result:Markedly inhibited PCP-induced hyperlocomotion in wild-type mice. This significant antipsychotic-like activity of UNC9994 was completely abolished in β-arrestin-2 knockout mice.
Chemical Information
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CAS. Nr. 1354030-51-5
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Appearance Solid
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Molecular Weight 421.38
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Formel C21H22Cl2N2OS
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Color White to off-white
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SMILES
ClC1=CC=CC(C2CCN(CC2)CCCOC3=CC4=C(C=C3)SC=N4)=C1Cl
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (3)
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Journal Impact Factor
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Most Recent
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Theranostics
Morphine- and foot shock-responsive neuronal ensembles in the VTA possess different connectivity and biased GPCR signaling pathway. [Abstract]2024 Jan 12;14(3):1126-1146. PMID: 38250036 -
Acta Pharmacol Sin
G protein-dependent dopamine D2 receptor signaling mediates cocaine-primed reinstatement. [Abstract]2026 Jan 14. PMID: 41535707 -
Reinheit & Dokumentation
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Data Sheet (272 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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