Eltoprazine

Last updated
Eltoprazine
Eltoprazine.png
Clinical data
Other namesDU-28,853; DU-28853
Identifiers
  • 1-(2,3-dihydro-1,4-benzodioxin-5-yl)piperazine
CAS Number
PubChem CID
ChemSpider
UNII
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
Formula C12H16N2O2
Molar mass 220.272 g·mol−1
3D model (JSmol)
  • C1CN(CCN1)C2=C3C(=CC=C2)OCCO3
  • InChI=1S/C12H16N2O2/c1-2-10(14-6-4-13-5-7-14)12-11(3-1)15-8-9-16-12/h1-3,13H,4-9H2
  • Key:WVLHGCRWEHCIOT-UHFFFAOYSA-N

Eltoprazine (developmental code name DU-28,853) is a serotonergic drug of the phenylpiperazine class which is described as a serenic or antiaggressive agent. [1] [2] [3] It acts as an agonist of the serotonin 5-HT1A and 5-HT1B receptors and as an antagonist of the serotonin 5-HT2C receptor. [3] [4] The drug is closely related to fluprazine and batoprazine, which are similarly acting agents, and is also a known chemical precursor to S-15535 and lecozotan. Eltoprazine is or was under development for the treatment of aggression, attention deficit hyperactivity disorder (ADHD), cognition disorders, and drug-induced dyskinesia, but no recent development has been reported for these indications as of February 2022. [1] It was also under development for the treatment of psychotic disorders, but development for this indication was discontinued. [1] Eltoprazine was originated by Solvay and was developed by Elto Pharma, PsychoGenics, and Solvay. [1]

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References

  1. 1 2 3 4 "Eltoprazine - Elto Pharma - AdisInsight".
  2. ↑ Olivier B, Mos J, Rasmussen D (1990). "Behavioural pharmacology of the serenic, eltoprazine". Drug Metabol Drug Interact. 8 (1–2): 31–83. doi:10.1515/DMDI.1990.8.1-2.31. PMID   2091890. S2CID   27279453.
  3. 1 2 de Boer SF, Koolhaas JM (December 2005). "5-HT1A and 5-HT1B receptor agonists and aggression: a pharmacological challenge of the serotonin deficiency hypothesis". Eur J Pharmacol. 526 (1–3): 125–39. doi:10.1016/j.ejphar.2005.09.065. PMID   16310183.
  4. ↑ Schipper J, Tulp MT, Sijbesma H (1990). "Neurochemical profile of eltoprazine". Drug Metabol Drug Interact. 8 (1–2): 85–114. doi:10.1515/dmdi.1990.8.1-2.85. PMID   1982626. S2CID   30096596.
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