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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.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
10 mg | Inquiry | 10-14 weeks | |
50 mg | Inquiry | 10-14 weeks |
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. |
Molecular Weight | 516.61 |
Formula | C30H33FN4O3 |
Cas No. | 1887043-58-4 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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