Amitifadine
Amitifadine (DOV-21947; EB-1010) is a serotonin-norepinephrine-dopamine reuptake inhibitor (SNDRI), with IC50s of 12, 23, 96 nM for serotonin, norepinephrine and dopamine in HEK 293 cells , respectively.
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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: 410074-73-6
- 分子式: C11H11Cl2N
- 分子量:228.12
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
Dopamine 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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Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
10 μM
Compound: 4, DOV-21947
|
Inhibition of human ERG expressed in CHO cells
Inhibition of human ERG expressed in CHO cells
|
[PMID: 18954985] |
| CHO | IC50 |
93.8 nM
Compound: 5, DOV-216303
|
Inhibition of dopamine reuptake at human dopamine transporter expressed in CHO cells
Inhibition of dopamine reuptake at human dopamine transporter expressed in CHO cells
|
[PMID: 20724153] |
| HEK293 | IC50 |
215 nM
Compound: 5, DOV-216303
|
Inhibition of serotonin reuptake at human SERT expressed in HEK293 cells
Inhibition of serotonin reuptake at human SERT expressed in HEK293 cells
|
[PMID: 20724153] |
| HEK293 | IC50 |
143 nM
Compound: DOV216,303
|
Inhibition of norepinephrine reuptake at human NET expressed in HEK293 cells after 15 mins by fluorescence neurotransmitter transporter assay
Inhibition of norepinephrine reuptake at human NET expressed in HEK293 cells after 15 mins by fluorescence neurotransmitter transporter assay
|
[PMID: 24974340] |
| HEK293 | IC50 |
394 nM
Compound: DOV216,303
|
Inhibition of DA reuptake at human DAT expressed in HEK293 cells after 15 mins by fluorescence neurotransmitter transporter assay
Inhibition of DA reuptake at human DAT expressed in HEK293 cells after 15 mins by fluorescence neurotransmitter transporter assay
|
[PMID: 24974340] |
| HEK293 | IC50 |
723 nM
Compound: DOV216,303
|
Inhibition of serotonin reuptake at human SERT expressed in HEK293 cells after 15 mins by fluorescence neurotransmitter transporter assay
Inhibition of serotonin reuptake at human SERT expressed in HEK293 cells after 15 mins by fluorescence neurotransmitter transporter assay
|
[PMID: 24974340] |
| HEK293 | IC50 |
159.3 nM
Compound: DOV21947
|
Inhibition of [3H]-DA uptake in human dopamine transporter expressed in HEK293 cells by scintillation counting
Inhibition of [3H]-DA uptake in human dopamine transporter expressed in HEK293 cells by scintillation counting
|
[PMID: 25164761] |
| HEK293 | IC50 |
411.5 nM
Compound: DOV21947
|
Inhibition of [3H]-serotonin uptake in human SERT expressed in HEK293 cells by scintillation counting
Inhibition of [3H]-serotonin uptake in human SERT expressed in HEK293 cells by scintillation counting
|
[PMID: 25164761] |
| HEK293 | IC50 |
71.4 nM
Compound: DOV21947
|
Inhibition of [3H]-NE uptake in human norepinephrine transporter expressed in HEK293 cells by scintillation counting
Inhibition of [3H]-NE uptake in human norepinephrine transporter expressed in HEK293 cells by scintillation counting
|
[PMID: 25164761] |
| MDCK | IC50 |
72.4 nM
Compound: 5, DOV-216303
|
Inhibition of norepinephrine reuptake at human NET expressed in MDCK cells
Inhibition of norepinephrine reuptake at human NET expressed in MDCK cells
|
[PMID: 20724153] |
化学情報
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CAS 番号 410074-73-6
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分子量 228.12
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分子式 C11H11Cl2N
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SMILES
ClC1=C(Cl)C=CC([C@]23[C@](CNC3)([H])C2)=C1
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別名
DOV-21947; EB-1010
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輸送条件
Room temperature in continental US; may vary elsewhere.
-
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
[1]. Skolnick P1, et al. Antidepressant-like actions of DOV 21,947: a "triple" reuptake inhibitor. Eur J Pharmacol. 2003 Feb 14;461(2-3):99-104. [Content Brief]
[2]. Levin ED, et al. Amitifadine, a triple monoamine re-uptake inhibitor, reduces nicotine self-administration in female rats. Eur J Pharmacol. 2015 Jun 20;764:30-37. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)