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Eltoprazine hydrochloride

5-HT2C receptor partial agonist CAS# 98224-03-4

Eltoprazine hydrochloride

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Chemical structure

Eltoprazine hydrochloride

3D structure

Chemical Properties of Eltoprazine hydrochloride

Cas No. 98224-03-4 SDF Download SDF
PubChem ID 3025067 Appearance Powder
Formula C12H17ClN2O2 M.Wt 256.73
Type of Compound N/A Storage Desiccate at -20°C
Solubility DMSO : ≥ 25 mg/mL (113.50 mM)
*"≥" means soluble, but saturation unknown.
Chemical Name 1-(2,3-dihydro-1,4-benzodioxin-5-yl)piperazine;hydrochloride
SMILES C1CN(CCN1)C2=C3C(=CC=C2)OCCO3.Cl
Standard InChIKey JFSOSUNPIXJCIX-UHFFFAOYSA-N
Standard InChI InChI=1S/C12H16N2O2.ClH/c1-2-10(14-6-4-13-5-7-14)12-11(3-1)15-8-9-16-12;/h1-3,13H,4-9H2;1H
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of Eltoprazine hydrochloride

Description5-HT1 and 5-HT2C receptor partial agonist (Ki values are 40, 52 and 81 nM for 5-HT1A, 5-HT1B and 5-HT2C receptors respectively). Reduces 5-HIAA levels in the striatum and exhibits antiaggressive behavior in vivo.

Eltoprazine hydrochloride Dilution Calculator

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Eltoprazine hydrochloride Molarity Calculator

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Preparing Stock Solutions of Eltoprazine hydrochloride

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 3.8951 mL 19.4757 mL 38.9514 mL 77.9029 mL 97.3786 mL
5 mM 0.779 mL 3.8951 mL 7.7903 mL 15.5806 mL 19.4757 mL
10 mM 0.3895 mL 1.9476 mL 3.8951 mL 7.7903 mL 9.7379 mL
50 mM 0.0779 mL 0.3895 mL 0.779 mL 1.5581 mL 1.9476 mL
100 mM 0.039 mL 0.1948 mL 0.3895 mL 0.779 mL 0.9738 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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References on Eltoprazine hydrochloride

Effects of eltoprazine hydrochloride on reactivity to conspecific or novel odors and activity.[Pubmed:1584837]

Pharmacol Biochem Behav. 1992 Mar;41(3):581-5.

Treatment with eltoprazine (DU 28853) increased the number of entries by male mice into compartments containing the odors of male and female conspecifics. This effect was most pronounced when odors were provided by previously defeated males. In contrast, the drug had no effect upon responsiveness to the odors of cinnamon and chocolate. The results suggest that eltoprazine may selectively increase reactivity to conspecific odors and that this effect is further enhanced by agonistic experience. Eltoprazine also substantially increased activity levels in all experiments. Since hyperactivity occurred both in the presence and absence of conspecific odors, however, the drug's effects on activity and olfaction seem to be largely independent. The results suggest that the aggression-modulating effects of eltoprazine, as well as other drugs, may be mediated in part by their effects on normal olfactory function.

The effects of intraventricular administration of eltoprazine, 1-(3-trifluoromethylphenyl)piperazine hydrochloride and 8-hydroxy-2-(di-n-propylamino)tetralin on resident intruder aggression in the rat.[Pubmed:1534769]

Eur J Pharmacol. 1992 Mar 3;212(2-3):295-8.

Various serotonergic agents may reduce aggression in rats, but how they act in different parts of the brain is unknown. This study attempted to unravel part of this question by application of different serotonergic ligands into the lateral ventricle (i.c.v.) of male rats (resident-intruder aggression). 8-OH-DPAT (8-hydroxy-2-(di-n-propylamino)tetralin; 1 and 10 micrograms), a specific 5-HT1A agonist, affected neither aggression nor any other behaviour. The mixed 5-HT1A,B,C agonist, TFMPP (1-(3-trifluoromethylphenyl)piperazine hydrochloride), and the 5-HT1A/1B agonist, eltoprazine ((1-(2,3)-dihydro-1,4-benzodioxin-5-yl)piperazine hydrochloride), suppressed aggression at i.c.v. doses of 10 and 30 micrograms. This reduction was not caused by sedation. These data suggest a role of postsynaptic 5-HT1B receptors in mediating the anti-aggressive effects of mixed 5-HT1 agonists.

Effects of eltoprazine hydrochloride on exploratory behavior and social attraction in mice.[Pubmed:1871192]

Pharmacol Biochem Behav. 1991 Apr;38(4):759-62.

The effects of eltoprazine (DU 28853) on exploratory behavior and conspecific social attraction were examined in four experiments. Drug treatments somewhat enhanced three forms of exploratory behavior but decreased social attraction. The results indicate that eltoprazine, in sharp contrast to fluprazine, weakly ameliorates neophobic responses. Both eltoprazine and fluprazine seem to increase the aversiveness of encounters with other organisms, however. The latter effects may be mediated, in part at least, by some alteration in olfactory function.

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.

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