Eltoprazine
Modify Date: 2024-01-11 11:51:02
Eltoprazine structure
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Common Name | Eltoprazine | ||
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| 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 EltoprazineEltoprazine(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]. |
| Name | 1-(2,3-Dihydrobenzo[b][1,4]dioxin-5-yl)piperazine hydrochloride |
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| Synonym | More Synonyms |
| 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]. |
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| Related Catalog | |
| References |
| Density | 1.18g/cm3 |
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| 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 |
| HS Code | 2934999090 |
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~49%
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 CAS#:98224-03-4 |
| Literature: Tetrahedron Letters, , vol. 39, # 15 p. 2219 - 2222 |
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~%
Eltoprazine CAS#:98224-03-4 |
| Literature: WO2012/3418 A2, ; WO 2012/003418 A2 |
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~%
Eltoprazine CAS#:98224-03-4 |
| Literature: WO2012/3418 A2, ; WO 2012/003418 A2 |
![5-isocyanato-2,3-dihydrobenzo[b][1,4]dioxine structure](https://www.chemsrc.com/caspic/437/1155139-88-0.png)
| HS Code | 2934999090 |
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| Summary | 2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0% |
| 1-(2,3-dihydro-1,4-benzodioxin-5-yl)piperazine,hydrochloride |
| Eltoprazine |