{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2025,11,2]],"date-time":"2025-11-02T19:50:07Z","timestamp":1762113007130,"version":"3.32.0"},"reference-count":31,"publisher":"Wiley","issue":"7","license":[{"start":{"date-parts":[[2006,7,6]],"date-time":"2006-07-06T00:00:00Z","timestamp":1152144000000},"content-version":"vor","delay-in-days":0,"URL":"http:\/\/onlinelibrary.wiley.com\/termsAndConditions#vor"}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Acta Anaesthesiol Scand"],"published-print":{"date-parts":[[2006,8]]},"abstract":"<jats:p><jats:bold>Background:\u2002<\/jats:bold>The sigma\u20101 receptor is functionally linked with psychotomimetic effects of various drugs. A sigma\u20101 receptor agonist enhances bradykinin\u2010induced intracellular Ca<jats:sup>2+<\/jats:sup>concentration ([Ca<jats:sup>2+<\/jats:sup>]i) increase and induces c\u2010Fos expression in a part of the brain. The aim of this study was to investigate the effects of several intravenous anaesthetics on the sigma\u20101 receptor.<\/jats:p><jats:p><jats:bold>Methods:\u2002<\/jats:bold>First, using Wistar rat brains, (+)[<jats:sup>3<\/jats:sup>H]SKF\u201010,047, a selective sigma\u20101 receptor agonist was displaced by propofol, dexmedetomidine, droperidol, and thiopental. Second, Fura\u20102 loaded NG\u2010108 cells were incubated with (+)pentazocine, a selective sigma\u20101 receptor agonist, and propofol and then its fluorescence was observed after stimulation with bradykinin. Third, male ICR mice received Intrafat\u00ae or propofol intraperitoneally (i.p.), followed by pentazocine i.p. Brain slices were prepared and Fos\u2010like immunoreactivity was detected using an immunohistochemical method.<\/jats:p><jats:p><jats:bold>Results:\u2002<\/jats:bold>Propofol, droperidol, and dexmedetomidine displaced (+)[<jats:sup>3<\/jats:sup>H]SKF\u201010,047 binding in a concentration\u2010dependent manner with Ki50s of 10.2 \u00b1 0.6, 0.17 \u00b1 0.03, 5.73 \u00b1 1.2 \u03bcM, respectively. Thiopental sodium was practically ineffective. Propofol produced a statistically significant reduction in the maximal binding capacity (Bmax) but did not affect the dissociation constant (<jats:italic>K<\/jats:italic><jats:sub>d<\/jats:sub>). (+)Pentazocine significantly enhanced bradykinin\u2010induced [Ca<jats:sup>2+<\/jats:sup>]i increases, but propofol did not affect it. Pentazocine induced marked Fos\u2010LI positive cells in the posterior cingulate and retrosplenial cortices (PC\/RS), which was significantly reduced by propofol.<\/jats:p><jats:p><jats:bold>Conclusions:\u2002<\/jats:bold>These results suggest that propofol may be a sigma\u20101 receptor antagonist, and that various effects of propofol on the brain may be mediated, at least partly, by the sigma\u20101 receptor.<\/jats:p>","DOI":"10.1111\/j.1399-6576.2006.01033.x","type":"journal-article","created":{"date-parts":[[2006,7,7]],"date-time":"2006-07-07T14:29:46Z","timestamp":1152282586000},"page":"875-881","source":"Crossref","is-referenced-by-count":9,"title":["Propofol acts at the sigma\u20101 receptor and inhibits pentazocine\u2010induced c\u2010Fos expression in the mouse posterior cingulate and retrosplenial 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