Eltoprazine

Modify Date: 2024-01-11 11:51:02

Eltoprazine Structure
Eltoprazine structure
Common Name Eltoprazine
CAS Number 98224-03-4 Molecular Weight 220.26800
Density 1.18g/cm3 Boiling Point 384.3ºC at 760mmHg
Molecular Formula C12H16N2O2 Melting Point N/A
MSDS N/A Flash Point 186.2ºC

 Use of Eltoprazine


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 antagonistin 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].

 Names

Name 1-(2,3-Dihydrobenzo[b][1,4]dioxin-5-yl)piperazine hydrochloride
Synonym More Synonyms

 Eltoprazine Biological Activity

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 antagonistin 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].
Related Catalog
References

[1]. Sijbesma H, et al. Eltoprazine, a drug which reduces aggressive behaviour, binds selectively to 5-HT1 receptor sites in the rat brain: an autoradiographic study. Eur J Pharmacol. 1990 Feb 20;177(1-2):55-66.

[2]. Joels M, et al. Eltoprazine suppresses hyperpolarizing responses to serotonin in rat hippocampus. J Pharmacol Exp Ther. 1990 Apr;253(1):284-9.

[3]. Bezard E, et al. Study of the antidyskinetic effect of eltoprazine in animal models of levodopa-induced dyskinesia. Mov Disord. 2013 Jul;28(8):1088-96.

[4]. Rocha B, et al. Chronic mianserin or eltoprazine treatment in rats: effects on the elevated plus-maze test and on limbic 5-HT2C receptor levels. Eur J Pharmacol. 1994 Sep 1;262(1-2):125-31.

 Chemical & Physical Properties

Density 1.18g/cm3
Boiling Point 384.3ºC at 760mmHg
Molecular Formula C12H16N2O2
Molecular Weight 220.26800
Flash Point 186.2ºC
Exact Mass 220.12100
PSA 33.73000
LogP 1.26120

 Safety Information

HS Code 2934999090

 Synthetic Route

~49%

Eltoprazine Structure

Eltoprazine

CAS#:98224-03-4

Literature: THE UNIVERSITY OF NORTH CAROLINA AT CHAPEL HILL; JIN, Jian; ROTH, Bryan; FRYE, Stephen Patent: WO2012/3418 A2, 2012 ; Location in patent: Page/Page column 97 ; WO 2012/003418 A2

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Eltoprazine Structure

Eltoprazine

CAS#:98224-03-4

Literature: Tetrahedron Letters, , vol. 39, # 15 p. 2219 - 2222

~%

Eltoprazine Structure

Eltoprazine

CAS#:98224-03-4

Literature: WO2012/3418 A2, ; WO 2012/003418 A2

~%

Eltoprazine Structure

Eltoprazine

CAS#:98224-03-4

Literature: WO2012/3418 A2, ; WO 2012/003418 A2

 Customs

HS Code 2934999090
Summary 2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

 Synonyms

1-(2,3-dihydro-1,4-benzodioxin-5-yl)piperazine,hydrochloride
Eltoprazine
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