2. GPCR/G Protein Neuronal Signaling
  3. 5-HT Receptor
  4. 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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5-HT1AR agonist 1 Chemical Structure

5-HT1AR agonist 1 Chemical Structure

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5-HT1AR agonist 1 Related Antibodies

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Description

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[1].
IC50 & Target[1]

SERT

12 nM (IC50)

NET

78 nM (IC50)

DAT

135 nM (IC50)

In Vivo

5-HT1AR agonist 1 (2.5 MG/ KG, I.V. and 10 MG / KG, P.O.) shows excellent oral bioavailability and low clearance in mice[1].
5-HT1AR agonist 1 (30 MG/KG, i.p., 30 min) shows the robust antidepressant potential in the forced swimming test in mice, similar to the effect of Vilazodone (HY-14262)[1]
In Vivo pharmacokinetic parameters of 5-HT1AR agonist 1 in ICR mice.[1]

药代动力学分析[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

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

Animal Model: Male ICR mice
Dosage: 2.5 MG/ KG, I.V. and 10 MG / KG, P.O.
Administration: I.V. and P.O., a single dose
Result: Showed excellent oral bioavailability in mice[1]
Animal Model: C57 mice
Dosage: 30 MG/KG
Administration: i.p., a single dose
Result: Significantly reduced immobility time in the forced swimming test in mice, similar to the effect of Vilazodone (HY-14262)[1]
Molecular Weight

418.49

Formula

C24H26N4O3
SMILES

NC(C1=CC2=C(O1)C=CC(N3CCN(CCC4=CC=C(CCC(N5)=O)C5=C4)CC3)=C2)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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5-HT1AR agonist 1 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

5-HT1AR agonist 15-HT ReceptorSerotonin Receptor5-hydroxytryptamine Receptor5-HT1AR agonismSERT reuptake ihibitionNET reuptake inhibitionDAT reuptake inhibitionantidepressant effectsdepressant deseaseInhibitorinhibitorinhibit

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