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98206-09-8 (Eltoprazine (hydrochloride))

1

Identification

Eltoprazine (hydrochloride) Eltoprazine (hydrochloride)
Name Eltoprazine (hydrochloride)
Formula C12H17ClN2O2
MW 256.73
CAS No. 98206-09-8
EINECS
Smiles [H]Cl.N1(C2=C3OCCOC3=CC=C2)CCNCC1
Synonyms DU-28853 hydrochloride;DU28853 hydrochloride;DU 28853 hydrochloride; 1-(2,3-dihydrobenzo[b][1,4]dioxin-5-yl)piperazine hydrochloride
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
2

Introduction

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.

Background Information

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]. ......by MedChemexpress Co., Ltd.
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Protocol(Only for Reference)

Cell Experiment

Animal Experiment

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Physical and Chemical Properties

Appearance: EBNumber:EB000010125

Storage condition

Solubility

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Mechanism and Indication

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Clinical Information

Product Name Sponsor & Collaborators Indications Start Date End Date Phase
Eltoprazine (hydrochloride) PsychoGenics Inc. Cognitive Impairment 2010/12/21 2012/5/1 Phase 2 Clinical
Eltoprazine (hydrochloride) PsychoGenics Inc. Schizophrenia 2010/12/21 2012/5/1 Phase 2 Clinical
Eltoprazine (hydrochloride) - No Development Reported
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Safety Data of Eltoprazine (hydrochloride)

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Spectral Information

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Suppliers List

Company Price and Availability Country/Region
CHEMSCENE, LLC USA
Carbosynth Limited 25mg/USD132()
Cayman Chemical Company 1mg/USD25() USA
MedChemexpress Co., Ltd. 10mg/USD92(Get quote);50mg/USD352(Get quote) USA
Shanghai Haoyuan Chemexpress Co., Ltd. 10mg/USD92(Get quote);50mg/USD352(Get quote) China
Tocris Bioscience Inc. 10mg/USD125() USA
Toronto Research Chemicals Inc. 5mg/USD175() Canada
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Related Products

Other Forms of 98206-09-8

Name CAS No Formula MW
Eltoprazine 98224-03-4 C12H16N2O2 220.27

Recommended Compounds in 5-HT Receptor

Name CAS No Formula MW
RU 24969 66611-26-5 C14H16N2O 228.29
Eltoprazine 98224-03-4 C12H16N2O2 220.27
Dolasetron 115956-12-2 C19H20N2O3 324.37
Cyclobenzaprine (hydrochloride) 6202-23-9 C20H22ClN 311.85
Dihydroergotamine (mesylate) 6190-39-2 C34H41N5O8S 679.78
Ramosetron (Hydrochloride) 132907-72-3 C17H18ClN3O 315.8
Alverine (citrate) 5560-59-8 C26H35NO7 473.56
Trazodone (hydrochloride) 25332-39-2 C19H23Cl2N5O 408.32
Clomipramine (hydrochloride) 17321-77-6 C19H24Cl2N2 351.31
Chlorpromazine (hydrochloride) 69-09-0 C17H20Cl2N2S 355.33
Almotriptan (malate) 181183-52-8 C21H31N3O7S 469.55
Cyproheptadine (hydrochloride) 969-33-5 0.0
Urapidil (hydrochloride) 64887-14-5 C20H30ClN5O3 423.94
Mirtazapine 85650-52-8 C17H19N3 265.35
Zolmitriptan 139264-17-8 C16H21N3O2 287.36
Rizatriptan (benzoate) 145202-66-0 C22H25N5O2 391.47
Naratriptan 121679-13-8 0.0
Mosapride 112885-41-3 C21H25ClFN3O3 421.89
Mosapride (citrate) 112885-42-4 C27H37ClFN3O12 650.05
Risperidone (mesylate) 666179-96-0 C24H31FN4O5S 506.59

Recommended Compounds in Same Indication

Name CAS No Formula MW
Rifabutin 72559-06-9 C46H62N4O11 847.0
Asenapine (maleate) 85650-56-2 C21H20ClNO5 401.84
Cariprazine 839712-12-8 C21H32Cl2N4O 427.41
PF-2545920 898562-94-2 C25H20N4O 392.45
lumateperone (methylbenzenesulfonate) 1187020-80-9 C31H36FN3O4S 565.7
Lu AE58054 467459-31-0 C20H19F5N2O 398.37
EVP-6124 550999-75-2 C16H17ClN2OS 320.84
Asenapine 65576-45-6 C17H16ClNO 285.77
Adoprazine 222551-17-9 C24H24FN3O2 405.46
Clozapine 5786-21-0 C18H19ClN4 326.82
Bitopertin 845614-11-1 C21H20F7N3O4S 543.46
Bitopertin (R enantiomer) 845614-12-2 C21H20F7N3O4S 543.46
Lurasidone (Hydrochloride) 367514-88-3 C28H37ClN4O2S 529.14
Preladenant 377727-87-2 C25H29N9O3 503.56
Ziprasidone (hydrochloride monohydrate) 138982-67-9 C21H24Cl2N4O2S 467.41
Ziprasidone 146939-27-7 C21H13D8ClN4OS 420.98
Talnetant 174636-32-9 C25H22N2O2 382.45
Talnetant (hydrochloride) 204519-66-4 C25H23ClN2O2 418.92
TAK-063 1238697-26-1 C23H17FN6O2 428.42
Iloperidone 133454-47-4 C24H27FN2O4 426.48
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Route of Synthesis

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References

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More Information

Eltoprazine (hydrochloride)

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