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Eltoprazine

Chemical compound

Field	Value
image	Eltoprazine.svg
image_class	skin-invert-image
width	200px
routes_of_administration	Oral
class	Non-selective serotonin receptor modulator; Serotonin [5-HT1A receptor](5-ht1a-receptor) agonist; Serotonin [5-HT1B receptor](5-ht1b-receptor) agonist; Serotonin [5-HT2C receptor](5-ht2c-receptor)
ATC_prefix	None
bioavailability	95%
onset	1–4 hours ()
elimination_half-life	7–9 hours
excretion	Urine: 40% unchanged
CAS_number	98224-03-4
PubChem	65853
ChemSpiderID	59265
UNII_Ref
UNII	510M006KO6
ChEBI	234413
ChEMBL	282614
synonyms	DU-28,853; DU-28853; DU28853
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

| Drugs.com =

| elimination_half-life = 7–9 hours

Eltoprazine (; developmental code name DU-28,853) is a non-selective serotonin receptor modulator of the phenylpiperazine family which was under development for the treatment of aggression, attention deficit hyperactivity disorder (ADHD), cognition disorders, drug-induced dyskinesia, and psychotic disorders but was never marketed. It has been described as a "serenic" or antiaggressive agent. The drug is taken orally.

It acts as an agonist of the serotonin 5-HT1A and 5-HT1B receptors and as an antagonist of the serotonin 5-HT2C receptor (Ki = 40nM, 52nM, and 81nM, respectively). The drug also shows weaker affinity for certain other serotonin receptors and targets. The pharmacokinetics of eltoprazine have been studied. Eltoprazine 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. It was originated by Solvay and was developed by Elto Pharma, PsychoGenics, and Solvay. The drug is or was under development for the treatment of aggression, ADHD, cognitive disorders, and drug-induced dyskinesia, but no recent development has been reported for these indications as of 2022. It was also under development for the treatment of psychotic disorders, but development for this indication was discontinued. Eltoprazine reached phase 2 or 3 clinical trials. According to David Nutt, eltoprazine showed shown signs of effectiveness in the treatment of aggression but was rejected for marketing authorization on the basis of aggression being a symptom rather than a disorder.

References

"Eltoprazine - Elto Pharma". AdisInsight.
(18 June 2025). "Delving into the Latest Updates on Eltoprazine Hydrochloride with Synapse".
(1 January 1900). "Eltoprazine Drug Profile".
(1990). "Behavioural pharmacology of the serenic, eltoprazine". Drug Metabolism and Drug Interactions.
(December 2005). "5-HT1A and 5-HT1B receptor agonists and aggression: a pharmacological challenge of the serotonin deficiency hypothesis". European Journal of Pharmacology.
(1990). "Neurochemical profile of eltoprazine". Drug Metabolism and Drug Interactions.
(1991). "Dose-proportionality of eltoprazine. Pharmacokinetics of single oral doses in healthy subjects". European Journal of Clinical Pharmacology.
(1990). "Pharmacokinetics of eltoprazine in healthy subjects". Drug Metabolism and Drug Interactions.
(December 2005). "5-HT1B receptors and aggression: a review". European Journal of Pharmacology.
(28 July 2005). "Novartis Foundation Symposia". Wiley.
(2020). "Engineering of heme-dependent monooxygenases towards heterocycle conversion". RWTH Aachen University.
(1987). "Effects of DU 28853, a new serenic drug, in several experimental models for aggression.". Research on Aggression.
(1987). "Eltoprazine (DU 28853): Effects on aggressive behaviour and its serotonergic properties.".
(March 2025). "Drug development in psychiatry: 50 years of failure and how to resuscitate it". The Lancet. Psychiatry.
(September 1994). "Eltoprazine in aggressive mentally handicapped patients: a double-blind, placebo- and baseline-controlled multi-centre study. The Eltoprazine Aggression Research Group". International Clinical Psychopharmacology.

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This article was imported from Wikipedia and is available under the Creative Commons Attribution-ShareAlike 4.0 License. Content has been adapted to SurfDoc format. Original contributors can be found on the article history page.

5-ht1a-agonists 5-ht1b-agonists 5-ht2c-antagonists antiaggressive-drugs antidyskinetic-agents benzodioxins eltoprazines experimental-drugs 1-piperazinyl-compounds serotonin-receptor-agonists

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