Chemistry:Elopiprazole

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Elopiprazole (INN; 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][2][3][4] It is taken orally.[1][3] 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][3] Conversely, it shows more than 50-fold lower affinity for the serotonin 5-HT2A and 5-HT2C receptors and various other targets.[3] Elopiprazole was under development by Solvay Duphar.[1][2] It reached phase 1 clinical trials for psychotic disorders prior to the discontinuation of its development.[1][2]

See also

References

  1. ↑ 1.0 1.1 1.2 1.3 1.4 "Elopiprazole". 6 December 2006. https://adisinsight.springer.com/drugs/800001422. 
  2. ↑ 2.0 2.1 2.2 "Delving into the Latest Updates on Elopiprazole with Synapse". 2 May 2026. https://synapse.patsnap.com/drug/1357539cd0cd4b0ab391b7f9d4c00b49. 
  3. ↑ 3.0 3.1 3.2 3.3 "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. January 1995. doi:10.1111/j.1365-2125.1995.tb04403.x. 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).". 
  4. ↑ "2-Phenylpyrroles as conformationally restricted benzamide analogues. A new class of potential antipsychotics. 1". Journal of Medicinal Chemistry 30 (11): 2099–104. November 1987. doi:10.1021/jm00394a028. PMID 2889830. 



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