1. Neuronal Signaling
  2. Serotonin Transporter
    Dopamine Transporter
  3. Amitifadine hydrochloride

Amitifadine hydrochloride (Synonyms: DOV-21947 hydrochloride; EB-1010 hydrochloride)

Cat. No.: HY-18332A Purity: 99.92%
Handling Instructions

Amitifadine hydrochloride 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.

For research use only. We do not sell to patients.

Amitifadine hydrochloride Chemical Structure

Amitifadine hydrochloride Chemical Structure

CAS No. : 410074-74-7

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 385 In-stock
Estimated Time of Arrival: December 31
5 mg USD 350 In-stock
Estimated Time of Arrival: December 31
10 mg USD 600 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1800 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
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Other Forms of Amitifadine hydrochloride:

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Description

Amitifadine hydrochloride 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.

IC50 & Target

IC50: 12 nM (serotonin), 23 nM (norepinephrine), 96 nM (dopamine)[1].

In Vitro

Amitifadine (DOV 21,947) is an antidepressant drug. Ki values for SERT, NET, and DAT are 99 nM, 262 nM, and 213 nM. The IC50 values for serotonin, norepinephrine and dopamine uptake are 12, 23 and 96 nM, respectively[1].

In Vivo

The 30 mg/kg Amitifadine dose significantly reduces nicotine self-administration. The 5 and 10 mg/kg doses reduce nicotine self-administration during the first 15 min. of the session when the greatest amount of nicotine is self-administered. The 30 mg/kg Amitifadine dose, but not the lower doses cause a significant reduction in locomotor activity averaged over the 1-hour session and reduce food motivated responding. The 10 mg/kg dose causes hypoactivity at the beginning of the session, but 5 mg/kg does not cause any hypoactivity. The effect of chronic Amitifadine treatment (10 mg/kg) over the course of 15 sessions is also determined. Amitifadine causes a significant reduction in nicotine self-administration, which is not seen to diminish over two consecutive weeks of treatment and a week after enforced abstinence. Amitifadine significantly reduces nicotine self-administration. This prompts further research to determine if Amitifadine might be an effective treatment for smoking cessation[2].

Clinical Trial
Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (377.96 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.7796 mL 18.8979 mL 37.7958 mL
5 mM 0.7559 mL 3.7796 mL 7.5592 mL
10 mM 0.3780 mL 1.8898 mL 3.7796 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.75 mg/mL (10.39 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.75 mg/mL (10.39 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.75 mg/mL (10.39 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Molecular Weight

264.58

Formula

C₁₁H₁₂Cl₃N

CAS No.

410074-74-7

SMILES

ClC(C=C1[[email protected]]2(CNC3)[[email protected]@H]3C2)=C(C=C1)Cl.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
Amitifadine hydrochloride
Cat. No.:
HY-18332A
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Amitifadine hydrochloride

Cat. No.: HY-18332A