Jump to content

Elopiprazole

From Wikipedia, the free encyclopedia
Elopiprazole
Clinical data
Other namesDU-29840; DU29840; DU-29894; DU29894
Routes of
administration		Oral[1][2]
ATC code
  • None
Legal status
Legal status
  • In general: uncontrolled
Pharmacokinetic data
Elimination half-life≥30–40 hours[2]
Identifiers
  • 1-(1-benzofuran-7-yl)-4-[[5-(4-fluorophenyl)-1H-pyrrol-2-yl]methyl]piperazine
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC23H22FN3O
Molar mass375.447 g·mol−1
3D model (JSmol)
  • Fc1ccc(cc1)c2ccc([nH]2)CN5CCN(c4cccc3c4occ3)CC5
  • InChI=1S/C23H22FN3O/c24-19-6-4-17(5-7-19)21-9-8-20(25-21)16-26-11-13-27(14-12-26)22-3-1-2-18-10-15-28-23(18)22/h1-10,15,25H,11-14,16H2
  • Key:PGNHBJGIQAEIHD-UHFFFAOYSA-N

Elopiprazole (INNTooltip International Nonproprietary Name; developmental code names DU-29840 and DU-29894) is an experimental antipsychotic drug of the phenylpiperazine family which was under development for the treatment of psychotic disorders but was never marketed.[1][3][2][4] It is taken orally.[1][2] The drug acts as a dual dopamine D2 and D3 receptor antagonist and serotonin 5-HT1A receptor agonist (Ki = 0.45 nM, 1.29 nM, and 1.45 nM, respectively).[1][2] Conversely, it shows more than 50-fold lower affinity for the serotonin 5-HT2A and 5-HT2C receptors and various other targets.[2] Elopiprazole was under development by Solvay Duphar.[1][3] It reached phase 1 clinical trials for psychotic disorders prior to the discontinuation of its development.[1][3]

See also

[edit]

References

[edit]
  1. 1 2 3 4 5 6 "Elopiprazole". AdisInsight. 6 December 2006. Retrieved 29 July 2026.
  2. 1 2 3 4 5 6 de Koning P, de Vries MH (January 1995). "A comparison of the neuro-endocrinological and temperature effects of DU 29894, flesinoxan, sulpiride and haloperidol in normal volunteers". Br J Clin Pharmacol. 39 (1): 7–14. doi:10.1111/j.1365-2125.1995.tb04403.x. PMC 1364975. PMID 7756102. DU 29894, 1-(7-benzofuranyl)-4-[[5-(4-fluorophenyl)-1-H-pyrrol-2yl]methyl] piperazine, is a potent dopamine receptor (DA2) antagonist (Ki = 0.45 nM) and serotonin (5HT1A) agonist (Ki = 1.45 nM). High affinity also exists for the DA3 receptor (Ki = 1.29 nM) while next highest affinities (sigma receptors, 5HT1c receptors, verapamil type Ca2+ channel, 5HT, receptors) are at least a factor 50 less (Solvay Duphar B.V., data on file).
  3. 1 2 3 "Delving into the Latest Updates on Elopiprazole with Synapse". Synapse. 2 May 2026. Retrieved 29 July 2026.
  4. ↑ van Wijngaarden I, Kruse CG, van Hes R, van der Heyden JA, Tulp MT (November 1987). "2-Phenylpyrroles as conformationally restricted benzamide analogues. A new class of potential antipsychotics. 1". Journal of Medicinal Chemistry. 30 (11): 2099–104. doi:10.1021/jm00394a028. PMID 2889830.
Retrieved from "https://en.wikipedia.org/w/index.php?title=Elopiprazole&oldid=1366661325"