5-HT1AR agonist 1
5-HT1AR agonist 1 (Compound A3) emerges as a relatively balanced multi-target activity profile, including 5-HT1AR agonist with an EC50 value of 34 nM, SERT reuptake ihibitor (IC50 =12 nM), NET reuptake inhibitor (IC50 =78 nM) and DAT reuptake inhibitor (IC50 =135 nM). 5-HT1AR agonist 1 performs significant antidepressant effects and exhibits excellent bioavailability and low clearance in mice, which is promising for research in the field of antidepressant drugs.
For research use only. We do not sell to patients.
- CAS No.: 3048071-20-8
- Formula: C24H26N4O3
- Molecular Weight:418.49
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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All 5-HT Receptor Isoforms
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Biological Activity
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SERT 12 nM (IC50) |
NET 78 nM (IC50) |
DAT 135 nM (IC50) |
In Vivo pharmacokinetic parameters of 5-HT1AR agonist 1 in ICR mice.[1]
| Route | Dose (mg/kg) | Tmax (h) | Cmax (ng/mL) | AUClast (ng·h/mL) | T1/2 (h) | CL (mL/min/kg) | Vd (L/kg) | F (%) |
| A3 | PO. | 2.07 ± 0.15 | 0.42 ± 0.08 | 4980 ± 1590 | 16913 ± 2451 | / | / | 147 % |
| 10 mg/kg | ||||||||
| IV. | 2.64 ± 0.50 | 0.08 ± 0.00 | 2633 ± 104 | 2842 ± 142 | 14.62 ± 0.78 | 3.38 ± 0.79 | ||
| 10 mg/kg |