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.
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- CAS 番号: 3048071-20-8
- 分子式: C24H26N4O3
- 分子量:418.49
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5-HT Receptor アイソフォーム固有の製品をすべて表示
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生物活性
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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 |