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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- CAS No.: 410074-73-6
- Formule: C11H11Cl2N
- Masse moléculaire:228.12
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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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] |
Chemical Information
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CAS No. 410074-73-6
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Masse moléculaire 228.12
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Formule C11H11Cl2N
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SMILES
ClC1=C(Cl)C=CC([C@]23[C@](CNC3)([H])C2)=C1
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Synonyms
DOV-21947; EB-1010
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[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
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)