Z8779877149
Z8779877149 (Z7149) is a blood-brain barrier-permeable multi-target ligand that targets SERT (Ki=198 nM), α2A adrenergic receptor (Ki=180 nM; EC50=440 nM) and 5-HT2A receptor (EC50=172 nM, Emax=76%). Z8779877149 inhibits 5-HT reuptake and activates Gi and Gq protein signaling pathways, respectively. Z8779877149 effectively alleviates pain responses as well as depression- and anxiety-like behaviors, while exhibiting favorable safety without inducing sedation or motor impairment. Z8779877149 is available for the research of pain, depression and anxiety disorders.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Formel: C16H17F3N2O2
- Molecular Weight:326.31
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
Beschreibung
IC50 & Target
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α2-adrenergic receptor 180 nM (Ki) |
5-HT2A Receptor 172 nM (EC50) |
α2-adrenergic receptor 440 nM (EC50) |
In Vitro
Z8779877149 (z7149) (10-100 μM; 1 h for SERT complex formation) binds to the orthosteric pockets of human α2A adrenergic receptor and human SERT in conformations largely consistent with docking predictions, as confirmed by cryo-EM structures[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
| Species | Dose | Route | Cmax | Brain Concentration | T1/2 |
|---|---|---|---|---|---|
| Mice[1] | 10 mg/kg | i.p. | 79.7 μM | 830 nM | 56 min |
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 (8-10 week-old male; 10-12 week-old male and female); α2A D79N mutant (7-8 week-old female); α2a knockout; VMAT2 heterozygous[1]
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Dosage:0.2 mg/kg (acute antidepressant-like activity); 0.25 mg/kg (anxiolytic-like activity); 0.5 mg/kg (antidepressant-like activity, acute and long-lasting); 10 mg/kg (analgesia, motor function, reward-related behavior); 20 mg/kg (analgesia); 30 mg/kg (analgesia)
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Administration:i.p.
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Result:Produced significant analgesia at 10 mg/kg; produced greater analgesic effects at 20 mg/kg and 30 mg/kg (increased withdrawal latency vs baseline).
Reduced CFA-induced thermal hypersensitivity at 10 mg/kg (significantly increased withdrawal latency vs vehicle-treated CFA mice).
Reduced SNI-induced mechanical allodynia at 10 mg/kg (significantly increased mechanical threshold vs vehicle-treated SNI mice).
Failed to produce significant analgesia at 10 mg/kg in α2A knockout mice.
Significantly increased punished crossings at 0.25 mg/kg, reaching an effect comparable to 0.5 mg/kg diazepam.
Reduced immobility time acutely at 0.2 mg/kg and 0.5 mg/kg with efficacy comparable to 20 mg/kg fluoxetine.
Maintained antidepressant-like efficacy for up to 5 days at 0.5 mg/kg, while fluoxetine efficacy declined by day 3.
Did not induce sedation or motor impairment at 10 mg/kg.
Did not induce conditioned place preference at 10 mg/kg.
Chemical Information
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Molecular Weight 326.31
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Formel C16H17F3N2O2
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SMILES
CN1C=CC2=C1C=C(C3=CCCNC3)C=C2.OC(C(F)(F)F)=O
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Synonyms
Z7149
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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)
Z8779877149 Related Classifications
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