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.
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- Formule: C16H17F3N2O2
- Masse moléculaire:326.31
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Stockage:
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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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Activité biologique
Description
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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Masse moléculaire 326.31
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Formule 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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Z8779877149 Related Classifications
HY-181878 Related Classifications
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