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Cat. No.: HY-I0135

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Azaphen free base

Name: Azaphen free base
Brand: MedChemExpress
SKU: HY-I0135
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(Synonyms: Azafen free base; Pipofezin; Pipofezine)

1 Cited Publications

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Based on 1 publication(s) in Google Scholar

Azaphen free base (Azafen free base) is an orally active tricyclic antidepressant that inhibits the reuptake of serotonin and monoamines, regulates the 5-HT2c receptor, and exerts sedative, antidepressant and anxiolytic effects. Azaphen free base increases the bioavailability of serotonin in the synaptic cleft, does not block muscarinic receptors or affect monoamine oxidase activity, and binds to the human serotonin transporter via salt bridges, π-stacking, π-cation and hydrophobic interactions. Azaphen free base can be used in studies related to depression.

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

CAS No.: 24886-52-0
Formula: C₁₆H₁₉N₅O
Molecular Weight:297.35

Storage:

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

Azaphen free base Chemical Structure

CAS No.: 24886-52-0

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Biological Activity
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- In Vitro
- In Vivo
Chemical Information
Publications (1)
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Biological Activity

Description

All 5-HT Receptor Isoforms :

In Vitro

Azaphen (Less than 1 mg; 0.5 s exposure per frame, 2° s^-1 rotation rate, 120° total rotation angle) free base (Azafen free base) has its first atomic solid-state structure solved by MicroED at 0.82 Å resolution, revealing two inversion-related conformers with minimal conformational flexibility that supports binding to its target protein^[3].
Azaphen free base binds preferentially to the allosteric (S2) site of hSERT with minimal conformational change from its solid-state structure, stabilized by multiple key interactions including a salt bridge, pi-stacking, and pi-cation interactions^[3].

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

In Vivo

Azaphen (5-20 mg/kg; p.o.; single dose) free base (Azafen free base) exhibits pronounced antidepressant activity in the Porsolt behavioral despair test, with significant reductions in immobility duration at oral doses of 5, 10, and 20 mg/kg^[2].
Azaphen free base exhibits pronounced antidepressant activity in the Normura forced swimming test with significant reductions in depressive state duration^[2].

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

Animal Model:

Mongrel albino rats (70-90 days old, 200-250 g, behavioral despair induced via Porsolt forced swimming test)^[2]
Dosage:

5 mg/kg; 10 mg/kg; 20 mg/kg
Administration:

p.o.; single dose
Result:

Significantly shortened the duration of immobility (depressive state) compared to control.

Related Protocols :

Protocol for Pharmacokinetic Study

Chemical Information

CAS No. 24886-52-0
Molecular Weight 297.35
Formula C₁₆H₁₉N₅O
SMILES

CN1C2=C(C=CC=C2)OC3=NN=C(N4CCN(CC4)C)C=C31
Synonyms

Azafen free base; Pipofezin; Pipofezine
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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

Publications (1)

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Biochim Biophys Acta Gen Subj

5-Hydroxytryptamine activates a 5-HT/c-Myc/SLC6A4 signaling loop in non-small cell lung cancer. [Abstract]

2022 Apr;1866(4):130093. PMID: 35066124

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Imran M, et al. Study of various pyridazine and phthalazine drugs with diverse therapeutically and agrochemically activities. Russ J Bioorg Chem. 2020;46(5):745-767.

[2]. Aleeva GN, et al. Comparison of antidepressant effects of azafan, tianeptine, and paroxetine. Bulletin of experimental biology and medicine. 2009 Jul;148(1):54-6.

[3]. Lin J, et al. Uncovering the Elusive Structures and Mechanisms of Prevalent Antidepressants. Advanced therapeutics. 2024 Sep;7(9):2400117.

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Azaphen free base

1 Cited Publications

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Biological Activity
- Description
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Purity & Documentation
References

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Azaphen free base

Publications Citing Use of MedChemExpress (MCE) Azaphen free base

All 5-HT Receptor Isoforms