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5-HT7R antagonist 3

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Catalog No. T201849Cas No. 1887043-58-4

Compound 6.4, also known as 5-HT7R antagonist 3, is a selective antagonist of the 5-HT7R with a Ki of 8 nM. It exhibits significantly less affinity towards D2R, 5-HT1AR, and 5-HT2AR with Ki values of 511 nM, 8930 nM, and 5786 nM, respectively. In mice, 5-HT7R antagonist 3 demonstrates anti-depressant and anti-anxiety activities.

5-HT7R antagonist 3

5-HT7R antagonist 3

😃Good
Catalog No. T201849Cas No. 1887043-58-4
Compound 6.4, also known as 5-HT7R antagonist 3, is a selective antagonist of the 5-HT7R with a Ki of 8 nM. It exhibits significantly less affinity towards D2R, 5-HT1AR, and 5-HT2AR with Ki values of 511 nM, 8930 nM, and 5786 nM, respectively. In mice, 5-HT7R antagonist 3 demonstrates anti-depressant and anti-anxiety activities.
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Product Introduction

Bioactivity
Description
Compound 6.4, also known as 5-HT7R antagonist 3, is a selective antagonist of the 5-HT7R with a Ki of 8 nM. It exhibits significantly less affinity towards D2R, 5-HT1AR, and 5-HT2AR with Ki values of 511 nM, 8930 nM, and 5786 nM, respectively. In mice, 5-HT7R antagonist 3 demonstrates anti-depressant and anti-anxiety activities.
Targets&IC50
5-HT1A Receptor:8930nM(ki), D2 Receptor:511nM(ki), 5-HT7 Receptor:8nM(ki), 5-HT2A Receptor:5786nM(ki)
In vitro
5-HT 7 R antagonist 3, active across a range of 1 pM to 1 μM, inhibits cAMP production in cells stably expressing human 5-HT, achieving an IC50 of 113 nM and a K_b of 14 nM.
In vivo
The compound 5-HT7R antagonist 3, administered intraperitoneally at doses of 1.25-10 mg/kg to male BalbC mice (20-25 g) 60 minutes before testing, exhibited significant anti-anxiety and antidepressant effects.
Chemical Properties
Molecular Weight516.61
FormulaC30H33FN4O3
Cas No.1887043-58-4
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

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