(Z)-Doxepin
(Z)-Doxepin is an isomer of Doxepin (HY-B0725A). Doxepin is an orally active, blood-brain barrier penetrant tricyclic antidepressant with multiple activities including hypnosis, sedation, analgesia and vasodilation. Doxepin enhances the expression of PSD-95 and synapsin 1 via the PI3K/AKT/mTOR signaling pathway, and is metabolized to Desmethyldoxepin in vivo. Doxepin can be used in research related to various diseases such as depression, anxiety, obesity and atopic dermatitis.
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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: 3607-18-9
- 分子式: C19H21NO
- 分子量:279.38
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
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Akt |
mTOR |
Doxepin exerts protective effects by upregulating the expression of PSD-95 and synapsin 1 through activating the PI3K/AKT/mTOR signaling pathway[1].
Doxepin is almost ineffective in inhibiting serotonin (5-HT) uptake in rat platelets[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Doxepin (4.65-24.00 mg/kg; intraperitoneal injection; single administration; 5-120 minutes before electroshock) exerts dose- and time-dependent anticonvulsant activity against maximal electroshock-induced seizures in mice, with the peak efficacy observed at 5 minutes after intraperitoneal administration and an ED50 of 6.6 mg/kg[4].
Doxepin (6.70-11.63 mg/kg; i.p.; single administration; 5 minutes prior to Isoniazid (HY-B0329) challenge) exhibits anticonvulsant activity against isoniazid-induced seizures in Mus musculus mice, with an ED50 of 8.8 mg/kg and a protective index of 3.0[4].
Doxepin (3.88-8.04 mg/kg; intraperitoneal injection; single administration; 5 minutes prior to 3-mercaptopropionic acid challenge) exhibits anticonvulsant activity against 3-mercaptopropionic acid-induced seizures in mice, with an ED50 of 5.1 mg/kg and a protective index of 5.2[4].
Doxepin (4.65-8.04 mg/kg; i.p.; single administration; 5 min prior to Bicuculline (HY-N0219) challenge) exhibits anticonvulsant activity against Bicuculline-induced seizures in mice, with an ED50 of 5.9 mg/kg and a protective index of 4.5[4].
Doxepin (3.23-5.58 mg/kg; i.p.; single administration; 5 min prior to thiosemicarbazide challenge) exhibits the strongest anticonvulsant activity against thiosemicarbazide-induced seizures in mice, with an ED50 of 4.3 mg/kg and a protective index of 6.1[4].
Doxepin (24.11-72.00 mg/kg; intraperitoneal injection; single administration; 5-120 minutes before rotarod test) induces time-dependent neurotoxicity in mice by impairing motor coordination, with toxicity peaking at 5 minutes after intraperitoneal administration and a TD50 of 26.4 mg/kg[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 3607-18-9
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分子量 279.38
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分子式 C19H21NO
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SMILES
C(\CCN(C)C)=C\1/C=2C(COC=3C1=CC=CC3)=CC=CC2
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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.
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)
- (Z)-Doxepin
- 3607-18-9
- Akt
- mTOR
- Drug Intermediate
- Drug Isomer
- histamine H1 receptors
- guinea pig muscarinic acetylcholine receptor
- rat muscarinic acetylcholine receptor
- norepinephrine
- serotonin
- 5-hydroxytryptamine receptors
- human serotonin transporter
- alpha1-adrenergic receptors
- adenylate cyclase
- monoamine oxidase B
- Inhibitor
- inhibitor
- inhibit