Antiangiogenic Effect of (±)-Haloperidol Metabolite II Valproate Ester [(±)-MRJF22] in Human Microvascular Retinal Endothelial Cells.

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Antiangiogenic Effect of (±)-Haloperidol Metabolite II Valproate Ester [(±)-MRJF22] in Human Microvascular Retinal Endothelial Cells.

J Med Chem. 2016 Nov 10;59(21):9960-9966

Authors: Olivieri M, Amata E, Vinciguerra S, Fiorito J, Giurdanella G, Drago F, Caporarello N, Prezzavento O, Arena E, Salerno L, Rescifina A, Lupo G, Anfuso CD, Marrazzo A

Abstract
(±)-MRJF22 [(±)-2], a novel prodrug of haloperidol metabolite II (sigma-1 receptor antagonist/sigma-2 receptor agonist ligand) obtained by conjugation to valproic acid (histone deacetylase inhibitor) via an ester bond, exhibits antiangiogenic activity, being able to reduce human retinal endothelial cell (HREC) viability in a comparable manner to bevacizumab. Moreover, (±)-2 was able to significantly reduce viable cells count, endothelial cell migration, and tube formation in vascular endothelial growth factor A (VEGF-A) stimulated HREC cultures.

PMID: 27739690 [PubMed - indexed for MEDLINE]

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