Synthesis and characterization of N, N-dialkyl and N-alkyl-N-aralkyl fenpropimorph-derived compounds as high affinity ligands for sigma receptors

AR Hajipour, D Fontanilla, UB Chu, M Arbabian…

Index: Hajipour, Abdol R.; Fontanilla, Dominique; Chu, Uyen B.; Arbabian, Marty; Ruoho, Arnold E. Bioorganic and Medicinal Chemistry, 2010 , vol. 18, # 12 p. 4397 - 4404

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Citation Number: 9

Abstract

The sigma-1 receptor is a unique non-opioid, non-PCP binding site that has been implicated in many different pathophysiological conditions including psychosis, drug addiction, retinal degeneration and cancer. Based on the structure of fenpropimorph, a high affinity (Ki= 0.005 nM) 1 sigma-1 receptor ligand and strong inhibitor of the yeast sterol isomerase (ERG2), we previously deduced a basic sigma-1 receptor pharmacophore or chemical backbone ...