Eltoprazine Explained

Cas Number:98224-03-4
Pubchem:65853
Chemspiderid:59265
Unii:510M006KO6
Chembl:282614
Synonyms:DU-28,853; DU-28853
Iupac Name:1-(2,3-dihydro-1,4-benzodioxin-5-yl)piperazine
C:12
H:16
N:2
O:2
Smiles:C1CN(CCN1)C2=C3C(=CC=C2)OCCO3
Stdinchi: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
Stdinchikey: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] 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] 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.[4] It was also under development for the treatment of psychotic disorders, but development for this indication was discontinued. Eltoprazine was originated by Solvay and was developed by Elto Pharma, PsychoGenics, and Solvay.

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Notes and References

  1. Olivier B, Mos J, Rasmussen D . Behavioural pharmacology of the serenic, eltoprazine . Drug Metabol Drug Interact. . 8 . 1–2 . 31–83 . 1990 . 2091890 . 10.1515/DMDI.1990.8.1-2.31. 27279453 .
  2. de Boer SF, Koolhaas JM . 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 . December 2005 . 16310183 . 10.1016/j.ejphar.2005.09.065 .
  3. Schipper J, Tulp MT, Sijbesma H . Neurochemical profile of eltoprazine. . Drug Metabol Drug Interact. . 8 . 1–2 . 85–114 . 1990 . 1982626 . 10.1515/dmdi.1990.8.1-2.85. 30096596 .
  4. Web site: Eltoprazine - Elto Pharma - AdisInsight .