1. GPCR/G Protein
    Neuronal Signaling
  2. 5-HT Receptor
  3. Eltoprazine

Eltoprazine (Synonyms: DU 28853)

Cat. No.: HY-16687 Purity: >95.0%
Handling Instructions

Eltoprazine(DU28853) is a serenic or antiaggressive agent which as an agonist at the 5-HT1A and 5-HT1B receptors and as an antagonist at the 5-HT2C receptor.

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

Eltoprazine Chemical Structure

Eltoprazine Chemical Structure

CAS No. : 98224-03-4

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Description

Eltoprazine(DU28853) is a serenic or antiaggressive agent which as an agonist at the 5-HT1A and 5-HT1B receptors and as an antagonist at the 5-HT2C receptor. IC50 value: Target: 5-HT1A/1B agonist; 5-HT2C antagonist in vitro: The binding of [3H]eltoprazine to whole tissue sections was saturable and revealed an apparent dissociation constant (Kd) of 11 nM. Specific [3H]eltoprazine binding was completely displaced by 5-HT; conversely, unlabelled eltoprazine reduced [3H]5-HT binding to the levels of non-specific binding [1]. Eltoprazine evoked membrane changes that were similar to but much weaker than those induced by 5HT. Both the 5HT- and eltoprazine-evoked membrane hyperpolarizations were largely suppressed in the presence of spiperone [2]. in vivo: eltoprazine is extremely effective in suppressing dyskinesia in experimental models, although this effect was accompanied by a partial worsening of the therapeutic effect of l-dopa. Interestingly, eltoprazine was found to (synergistically) potentiate the antidyskinetic effect of amantadine. The current data indicated that eltoprazine is highly effective in counteracting dyskinesia in preclinical models [3]. Rats were chronically treated with mianserin (10 mg/kg i.p.) or eltoprazine (1 mg/kg i.p.) and were tested in the elevated plus-maze test for anxiety. Mianserin and eltoprazine displayed opposite effects in the elevated plus-maze: mianserin induced anxiolytic-like effects, while eltoprazine showed anxiogenic-like ones [4].

IC50 & Target

5-HT1A Receptor

 

5-HT1B Receptor

 

5-HT2C Receptor

 

Clinical Trial
Molecular Weight

220.27

Formula

C₁₂H₁₆N₂O₂

CAS No.

98224-03-4

SMILES

N1(C2=C3OCCOC3=CC=C2)CCNCC1

Shipping

Room temperature in continental US; may vary elsewhere.

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 : ≥ 25 mg/mL (113.50 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.5399 mL 22.6994 mL 45.3988 mL
5 mM 0.9080 mL 4.5399 mL 9.0798 mL
10 mM 0.4540 mL 2.2699 mL 4.5399 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

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

    Solubility: ≥ 2.5 mg/mL (11.35 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (11.35 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.5 mg/mL (11.35 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

EltoprazineDU 28853DU28853DU-288535-HT ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorInhibitorinhibitorinhibit

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Eltoprazine
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HY-16687
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