Azaphen
Based on 1 publication(s) in Google Scholar
Azaphen (Azafen) 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 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 can be used in studies related to depression.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 24853-80-3
- 分子式: C16H21Cl2N5O
- 分子量:370.28
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- プロトコル
- 純度とドキュメンテーション
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Help & FAQs
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MedChemExpress（MCE）の使用を引用している文献 Azaphen
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生物活性
製品説明
体外実験
Azaphen (Azafen) (Less than 1 mg; 0.5 s exposure per frame, 2° s-1 rotation rate, 120° total rotation angle) 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 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. Further protocols information, click here.
体内実験
Azaphen 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.
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Animal Model:Mongrel albino rats (70-90 days old, 200-250 g, behavioral despair induced via Porsolt forced swimming test)[2]
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Dosage:5 mg/kg; 10 mg/kg; 20 mg/kg
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Administration:p.o.; single dose
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Result:Significantly shortened the duration of immobility (depressive state) compared to control.
化学情報
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CAS 番号 24853-80-3
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分子量 370.28
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分子式 C16H21Cl2N5O
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SMILES
[H]Cl.[H]Cl.CN1C2=CC=CC=C2OC3=C1C=C(N4CCN(C)CC4)N=N3
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別名
Azafen; Pipofezin hydrochloride; Pipofezine hydrochloride
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Structure Classification
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Initial Source
from the cadaveric material
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (1)
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Journal Impact Factor
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Most Recent
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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
プロトコル
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Protocol for Pharmacokinetic Study
Pharmacokinetic studies quantify how an organism handles a drug over time through absorption, distribution, metabolism, and excretion, and the core experimental readout is the concentration-time profile of parent drug and, when relevant, metabolites in biological matrices such as plasma, whole blood, urine, bile, or tissue. Pharmacokinetic analysis links dose, route, exposure, clearance, half-life, distribution, bioavailability, and systemic exposure to drug efficacy and toxicity hypotheses rather than measuring a signaling pathway directly. The literature links pharmacokinetics to drug-development phenotypes by showing that drug metabolism and pharmacokinetics influence compound progression, exposure-response interpretation, safety margins, dosing strategy, and failure risk during discovery and development. DMPK science contributes to compound optimization by integrating physicochemical properties, in vitro metabolism, transporter behavior, in vivo exposure, and pharmacodynamic contex
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Azaphen 関連分類
HY-A0022 関連分類
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