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

5-HT7R antagonist 2 (compound 4h) is a 5-HT7R antagonist that antagonizes the G protein and β-arrestin signaling pathways, with a Ki of 67 nM, the IC50 values in cAMP and Tango tests were 2.59 μM and 39.57 μM, respectively. 5-HT7R antagonist 2 has an effect on neurogenesis and can reduce repetitive behaviors related to autism spectrum disorder (ASD) and restore neurogenesis of ASD impairment.
Pharmacokinetic Analysis ICR Male Mice

药代动力学分析

Plasma Intravenous Administration Intraperitoneal Administration
Tmax (h) 0.08 0.25
T1/2 (h) 0.77 1.06
Cmax (ng/mL) 33.07 156.44
AUClast (ng·h/mL) 28.31 143.27
CL (L/h/kg) 41.61 -
Vss (L/kg) 32.43 -
MRT (h) 0.79 0.93
F (%) 50.60

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5-HT7R antagonist 2 Chemical Structure

5-HT7R antagonist 2 Chemical Structure

CAS No. : 1448808-50-1

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5-HT7R antagonist 2 Related Antibodies

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Description

5-HT7R antagonist 2 (compound 4h) is a 5-HT7R antagonist that antagonizes the G protein and β-arrestin signaling pathways, with a Ki of 67 nM, the IC50 values in cAMP and Tango tests were 2.59 μM and 39.57 μM, respectively. 5-HT7R antagonist 2 has an effect on neurogenesis and can reduce repetitive behaviors related to autism spectrum disorder (ASD) and restore neurogenesis of ASD impairment[1].
Pharmacokinetic Analysis ICR Male Mice[1]

药代动力学分析[1]

Plasma Intravenous Administration Intraperitoneal Administration
Tmax (h) 0.08 0.25
T1/2 (h) 0.77 1.06
Cmax (ng/mL) 33.07 156.44
AUClast (ng·h/mL) 28.31 143.27
CL (L/h/kg) 41.61 -
Vss (L/kg) 32.43 -
MRT (h) 0.79 0.93
F (%) 50.60

IC50 & Target

5-HT7 Receptor

67 nM (Ki)

In Vitro

5-HT7R antagonist 2 (compound 4h) (microsomes, 30 min) has significant metabolic stability and is not cytotoxic[1].
5-HT7R antagonist 2 is a competitive antagonist in both G protein and β-arrestin signaling pathways[1].

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

5-HT7R antagonist 2 Related Antibodies

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In Vivo

5-HT7R antagonist (compound 4h) (intraperitoneal injection, 5 mg/kg, 30 min) has the potential to regulate the repetitive behavior of ASD in the animal model of ASD, and can increase the number of immature ASD neurons[1].

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

Animal Model: ASD animal models
Dosage: 5 mg/kg
Administration: Intraperitoneal injection
Result: 4h can increase the number of immature ASD neurons
Molecular Weight

252.31

Formula

C16H16N2O
CAS No.
SMILES

COC1=C(C2=CC=CC(C3=NCCN3)=C2)C=CC=C1
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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5-HT7R antagonist 2 Related Classifications

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  • 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 21448808-50-15-HT ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorASDShank3 TG miceself-groomingInhibitorinhibitorinhibit

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