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  • Title: Up-regulation of rat cortical sigma receptors after subchronic administration of rimcazole and 1,3-di(2-tolyl)guanidine.
    Author: Manallack DT, Beart PM.
    Journal: Neuropharmacology; 1988 Nov; 27(11):1201-3. PubMed ID: 2849732.
    Abstract:
    The effects of subchronic administration of rimcazole and 1,3-di(2-tolyl)guanidine (DTG) on the central R(+)[3H]-3-[3-hydroxyphenyl]-N-(1-propyl)piperidine (R(+)[3H]-3-PPP) binding site were investigated in the rat. Subchronic treatment with rimcazole was characterized by a 30% increase in the density and a two-fold decrease in the affinity of R(+)[3H]-3-PPP binding sites relative to saline-treated animals. DTG, a more potent sigma ligand, produced a similar alteration to the affinity but a 130% increase in the density of R(+)[3H]-3-PPP binding sites. These data thus provide evidence for the functional involvement of sigma receptors in the central nervous system.
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