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Eltoprazine

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Eltoprazine
Clinical data
Other namesDU-28,853; DU-28853
ATC code
  • None
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
FormulaC12H16N2O2
Molar mass220.272 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 anti-aggressive 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 was first described in the scientific literature by 1987.[5][6] It is or was under development for the treatment of aggression, attention deficit hyperactivity disorder (ADHD), cognitive 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 is said to have shown signs of effectiveness for treatment of aggression, but was rejected for marketing authorization on the basis of the fact that aggression is a symptom rather than a disorder.[7][8] The drug was originated by Solvay and was developed by Elto Pharma, PsychoGenics, and Solvay.[1]

See also

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References

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  1. ^ a b c d "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. ^ a b 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.
  5. ^ Olivier, B., Mos, J., Heyden, V. D. J. A., Zethof, T., Aken, V. H., Oorschot, V. R., & Ramirez, J. M. (1987). Effects of DU 28853, a new serenic drug, in several experimental models for aggression. Research on Aggression, 93. https://scholar.google.com/scholar?cluster=5474933454486255245
  6. ^ Schipper, J., Olivier, B., Mos, J., Tulp, M. T. M., Sijbesma, H., & Bevan, P. (1987). Eltoprazine (DU 28853): Effects on aggressive behaviour and its serotonergic properties. In International Conference on the Behavioral Pharmacology of [...]. https://scholar.google.com/scholar?cluster=17685819389699199278
  7. ^ Nutt DJ (March 2025). "Drug development in psychiatry: 50 years of failure and how to resuscitate it". Lancet Psychiatry. 12 (3): 228–238. doi:10.1016/S2215-0366(24)00370-5. PMID 39952266. Marketing authorisations are awarded for diagnoses, whereas in clinical practice psychiatrists and primary care physicians commonly treat symptoms, such as insomnia, which occurs in many different disorders as well as being a disorder itself.72 A good example of the discrepancy that thus arises was the development of the serotonin agonist eltoprazine, which proved effective for aggression in people with learning disabilities.53 EMA marketing authorisation was denied on the grounds that aggression was a symptom, not a diagnosis. Perversely, 18 years later, the dopamine–serotonin antagonist antipsychotic risperidone was approved for the same indication.73 [...] 53 de Koning P, Mak M, de Vries MH, et al. Eltoprazine in aggressive mentally handicapped patients: a double-blind, placebo- and baseline-controlled multi-centre study. Int Clin Psychopharmacol 1994; 9: 187–94.
  8. ^ de Koning P, Mak M, de Vries MH, Allsopp LF, Stevens RB, Verbruggen R, Van den Borre R, van Peteghem P, Kohen D, Arumainayagam M (September 1994). "Eltoprazine in aggressive mentally handicapped patients: a double-blind, placebo- and baseline-controlled multi-centre study. The Eltoprazine Aggression Research Group". Int Clin Psychopharmacol. 9 (3): 187–194. PMID 7814828.
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