2. Neuronal Signaling GPCR/G Protein
  3. Serotonin Transporter Adrenergic Receptor 5-HT Receptor
  4. 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.

For research use only. We do not sell to patients.

Z8779877149

Z8779877149 Chemical Structure

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Z8779877149 Related Antibodies

Top Publications Citing Use of Products

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α adrenergic receptor β adrenergic receptor

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5-HT Receptor 5-HT1 Receptor 5-HT2 Receptor 5-HT3 Receptor 5-HT4 Receptor 5-HT5 Receptor 5-HT6 Receptor 5-HT7 Receptor

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Description

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[1].
IC50 & Target

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.

Z8779877149 Related Antibodies
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

Z8779877149 (0.2-30 mg/kg; i.p.) produces α2A-dependent analgesia in acute, inflammatory, and neuropathic pain models without sedation or conditioned place preference, and exhibits anxiolytic-like activity at 0.25 mg/kg and long-lasting antidepressant-like activity at 0.5 mg/kg in mouse assays[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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]
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)
Administration: i.p.
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.
Molecular Weight

326.31

Formula

C16H17F3N2O2
SMILES

CN1C=CC2=C1C=C(C3=CCCNC3)C=C2.OC(C(F)(F)F)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Z8779877149 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Z8779877149Z7149Z 8779877149Z-8779877149Z 7149Z-7149Serotonin TransporterAdrenergic Receptor5-HT Receptor5-HTTSERTSLC6A4Beta ReceptorSerotonin Receptor5-hydroxytryptamine Receptordepressionanxiety5-HT2A receptorsGq protein signalingmouse modelsα2A adrenergic receptorsG? protein signalingpaincryo-EM structuresInhibitorinhibitorinhibit

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