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Overview
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Background
PD 144418 oxalate is a highly potent and selective ligand of the sigma-1 (σ1) receptor, with Ki values being 0.08 and 1377 nM for σ1 and σ2 receptors, respectively. The σ1 receptor, one of two σ receptor subtypes, is a transmembrane protein widely expressed in a variety of tissues, and it is relatively concentrated in certain regions of the central nervous system. The σ receptor has been implicated in many neuronal processes, as well as in the pathophysiology of certain psychiatric disorders, including depression, schizophrenia, motor disturbances, pain, drug addiction, attention deficit disorders, and probably cancer.
1. Akunne HC, Whetzel SZ, Wiley JN, et al. The pharmacology of the novel and selective sigma ligand, PD 144418. Neuropharmacology, 1997, 36(1): 51-62.
2. Guitart X, Codony X, Monroy X. Sigma receptors: biology and therapeutic potential. Psychopharmacology (Berl), 2004, 174(3): 301-319.
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