Powder: -20°C for 3 years | In solvent: -80°C for 1 year
AP521 is an agonist of the human 5-HT1A receptor (IC50: 94 nM).
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
25 mg | 6-8 weeks | $ 1,520.00 | |
50 mg | 6-8 weeks | $ 1,980.00 | |
100 mg | 6-8 weeks | $ 2,500.00 |
Description | AP521 is an agonist of the human 5-HT1A receptor (IC50: 94 nM). |
Targets&IC50 | 5-HT1A receptor:94 nM |
In vitro | AP521 is an agonist of human 5-HT1A receptor (IC50s: 135, 94, 254, 5530, 418, 422 and 198 nM for 5-HT1A (rat), 5-HT1A (human), 5-HT1B (rat), 5-HT1B (human), 5-HT1D (human), 5-HT5a (human) and 5-HT7 (rat)). AP521 also decreases the forskolin-induced cAMP accumulation from 10 nM to 10 μM. |
In vivo | AP521, at dosages ranging from 0.5 to 10 mg/kg, notably enhances shock acceptances and, when orally administered at 3 and 10 mg/kg, substantially reduces freezing time. Furthermore, it doubles the duration spent on the open arms compared to the vehicle-treated group, evidencing an anxiolytic-like effect that seems dose-dependent [F(3, 36)=4.21, P<0.05 for AP521]. At a concentration of 10 mg/kg, AP521 significantly boosts the extracellular 5-HT level in the medial prefrontal cortex (mPFC) from 0.5 to 1 hour post-administration. While a 3 mg/kg dose of AP521 suggests a potential increase in the extracellular 5-HT level, this rise is statistically insignificant. |
Molecular Weight | 402.89 |
Formula | C20H19ClN2O3S |
CAS No. | 151227-08-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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AP521 151227-08-6 GPCR/G Protein Neuroscience 5-HT Receptor AP 521 AP-521 inhibitor inhibit