[CAS NO. 151227-08-6] AP521
PRODUCTS SPECIFICATIONS [151227-08-6]
DESCRIPTION [151227-08-6]
Overview
| MDL | MFCD00932423 |
|---|---|
| Molecular Weight | 402.89 |
| Molecular Formula | C20H19ClN2O3S |
| SMILES | O=C([C@H]1CC(C2=CC=CC=C2S3)=C3CN1)NCC4=CC=C(OCO5)C5=C4.[H]Cl |
Summary
AP521 is an agonist of human 5-HT 1A receptor with an IC 50 of 94 nM.
IC50 & Target
|
5-HT 1A Receptor 94 nM (IC 50 , in human) |
5-HT 1A Receptor 135 nM (IC 50 , in rat) |
5-HT 1B Receptor 254 nM (IC 50 , in rat) |
5-HT 1B Receptor 5530 nM (IC 50 , in human) |
|
|
5-HT 1D Receptor 418 nM (IC 50 , in human) |
5-HT 5A Receptor 422 nM (IC 50 , in human) |
5-HT 7 Receptor 198 nM (IC 50 , in rat) |
||
In Vitro
AP521 is an agonist of human 5-HT 1A receptor with IC 50 s of 135, 94, 254, 5530, 418, 422 and 198 nM for 5-HT 1A (rat), 5-HT 1A (human), 5-HT 1B (rat), 5-HT 1B (human), 5-HT 1D (human), 5-HT 5a (human) and 5-HT 7 (rat), respectively. AP521 also decreases the forskolin-induced cAMP accumulation from 10 nM to 10 μM [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
AP521 significantly increases the number of shock acceptances [F(5,105)=4.46, P<0.01] at doses between 0.5 to 10 mg/kg. Oral administration of AP521 at 3 and 10 mg/kg significantly decreases freezing time [F(3,60)=2.89, P<0.05]. AP521 significantly increases the time spent on the open arms by approximately 2-fold as compare to the vehicle treated group [F(3, 36)=4.21, P<0.05 for AP521]. The anxiolytic-like effect of AP521 appears to be dose-related. AP521 significantly increases the extracellular 5-HT level of the medial prefrontal cortex (mPFC) at 10 mg/kg from 0.5 to 1 h after administration. AP521 at 3 mg/kg tends to increase the extracellular 5-HT level, however, this increase is not significant [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)