2. GPCR/G Protein Neuronal Signaling
  3. 5-HT Receptor Dopamine Receptor
  4. 5-HT7R antagonist 3

5-HT7R antagonist 3 (Compound 6.4) is a selective 5-HT7R antagonist (Ki: 8 nM), with Ki of 511 nM (D2), 8930 nM (5-HT1A) and 5786 nM (5-HT2A), respectively. 5-HT7R antagonist 3 possesses antidepressant and anxiolytic effects in mice.

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5-HT7R antagonist 3 Chemical Structure

5-HT7R antagonist 3 Chemical Structure

CAS No. : 1887043-58-4

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5-HT7R antagonist 3 Related Antibodies

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Description

5-HT7R antagonist 3 (Compound 6.4) is a selective 5-HT7R antagonist (Ki: 8 nM), with Ki of 511 nM (D2), 8930 nM (5-HT1A) and 5786 nM (5-HT2A), respectively. 5-HT7R antagonist 3 possesses antidepressant and anxiolytic effects in mice[1].

IC50 & Target[1]

5-HT7 Receptor

8 nM (Ki)

5-HT1A Receptor

8930 nM (Ki)

5-HT2A Receptor

5786 nM (Ki)

D2 Receptor

511 nM (Ki)

In Vitro

5-HT7R antagonist 3 (1 pM-1 μM) inhibits cAMP production in cells stably expressing human 5-HT, with IC50 of 113 nM, Kb of 14 nM [1].

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

5-HT7R antagonist 3 Related Antibodies
In Vivo

5-HT7R antagonist 3 (1.25-10 mg/kg, intraperitoneal injection, 60 min before testing) exerts significant anxiolytic and antidepressant effects in male BalbC mice (20-25 g)[1].

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

Animal Model: Male BalbC mice weighing 20-25 g[1]
Dosage: 0, 0.63, 1.25, 2.5, 5, 10 mg/kg
Administration: Intraperitoneal injection (i.p.)
Result: Showed significant antidepressant effects in forced swim test (FST) at a dose of 2.5 mg/kg, reducing immobility time by 29%.
Showed anxiolytic activity in four-plate test (FPT) at doses of 1.25, 2.5 and 10 mg/kg.
Reduced spontaneous locomotion during the 60-minute observation period.
Molecular Weight

516.61

Formula

C30H33FN4O3
CAS No.
SMILES

O=C1N(C[C@H](O)CN2CCN(C(C3=CC=CC=C3)C4=CC=CC=C4)CC2)C([C@](C)(C5=CC=C(F)C=C5)N1)=O
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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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5-HT7R antagonist 3 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:

5-HT7R antagonist 31887043-58-45-HT ReceptorDopamine ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorDepressionAnxiolyticcAMPCHO cellsBalbCFSTInhibitorinhibitorinhibit

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