1. GPCR/G Protein
    Neuronal Signaling
  2. 5-HT Receptor
  3. AP521

AP521 

Cat. No.: HY-100166
Handling Instructions

AP521 is an agonist of human 5-HT1A receptor with an IC50 of 94 nM.

For research use only. We do not sell to patients.

AP521 Chemical Structure

AP521 Chemical Structure

CAS No. : 151227-08-6

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Description

AP521 is an agonist of human 5-HT1A receptor with an IC50 of 94 nM.

IC50 & Target

IC50: 94 nM (5-HT1A (human))[1]

In Vitro

AP521 is an agonist of human 5-HT1A receptor with IC50s of 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), respectively. AP521 also decreases the forskolin-induced cAMP accumulation from 10 nM to 10 μM[1].

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].

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
Cell Assay
[1]

Membranes of neurotransmitter receptors are prepared from the tissues of rat, mouse, and guinea pig or from recombinant cells. These membranes are incubated in assay buffers containing selective radioligand for each receptor and AP521. After the incubation, the mixture is vacuum filtered through a glass membrane filter and washed by cold reaction buffer. Afterward, the radioactivity of the filters is counted[1].

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

Animal Administration
[1]

Male Sprague-Dawley rats weighing 250 to 300 g are anesthetized with pentobarbital sodium (50 mg/kg, i.p.) and placed on a stereotaxic apparatus. Dialysis probes with an outer diameter of 0.105 mm are inserted into the guide cannulae so that 3.0 mm of the probes are exposed to the tissue of the medial prefrontal cortex. Rats are housed individually after these operations. On the following day, perfusion is started in the home cage using artificial cerebrospinal fluid (145 mM NaCl, 3.0 mM KCl, 1.3 mM CaCl2, 1.0 mM MgCl2) at a flow rate of 2 mL/min. AP521 (3, 10 mg/kg), tandospirone (10 mg/kg) or vehicle are administered subcutaneously 60 min after sample collection started. The dialysate samples are collected every 30 min for 180 min and extracellular levels of 5-HT are determined[1].

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

References
Molecular Weight

402.89

Formula

C₂₀H₁₉ClN₂O₃S

CAS No.

151227-08-6

SMILES

O=C([[email protected]]1CC(C2=CC=CC=C2S3)=C3CN1)NCC4=CC=C(OCO5)C5=C4.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere

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AP521
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AP521

Cat. No.: HY-100166