1. Neuronal Signaling GPCR/G Protein
  2. Dopamine Receptor Dopamine Transporter Serotonin Transporter
  3. 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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Amitifadine

Amitifadine Chemical Structure

CAS No. : 410074-73-6

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Description

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.

Cellular Effect
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]
CHO-K1 IC50
78 nM
Compound: DOV-216, 303
Inhibition of [3H]dopamine reuptake at human DAT expressed in CHOK1 cells by scintillation counting
Inhibition of [3H]dopamine reuptake at human DAT expressed in CHOK1 cells by scintillation counting
[PMID: 21093273]
CHO-K1 IC50
96 nM
Compound: DOV-21, 947
Inhibition of [3H]dopamine reuptake at human DAT expressed in CHOK1 cells by scintillation counting
Inhibition of [3H]dopamine reuptake at human DAT expressed in CHOK1 cells by scintillation counting
[PMID: 21093273]
HEK293 IC50
12 nM
Compound: DOV-21, 947
Inhibition of [3H]serotonin reuptake at human SERT expressed in HEK293 cells by scintillation counting
Inhibition of [3H]serotonin reuptake at human SERT expressed in HEK293 cells by scintillation counting
[PMID: 21093273]
HEK293 IC50
14 nM
Compound: DOV-216, 303
Inhibition of [3H]serotonin reuptake at human SERT expressed in HEK293 cells by scintillation counting
Inhibition of [3H]serotonin reuptake at human SERT expressed in HEK293 cells by scintillation counting
[PMID: 21093273]
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
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
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
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
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]
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]
MDCK IC50
20 nM
Compound: DOV-216, 303
Inhibition of [3H]norepinephrine reuptake at human NET expressed in MDCK cells by scintillation counting
Inhibition of [3H]norepinephrine reuptake at human NET expressed in MDCK cells by scintillation counting
[PMID: 21093273]
MDCK IC50
23 nM
Compound: DOV-21, 947
Inhibition of [3H]norepinephrine reuptake at human NET expressed in MDCK cells by scintillation counting
Inhibition of [3H]norepinephrine reuptake at human NET expressed in MDCK cells by scintillation counting
[PMID: 21093273]
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]
Molecular Weight

228.12

Formula

C11H11Cl2N

CAS No.
SMILES

ClC1=C(Cl)C=CC([C@]23[C@](CNC3)([H])C2)=C1

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Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Amitifadine
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