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In the present study, the experimental conditions of agonist\u2010induced [\n                    <jats:sup>35<\/jats:sup>\n                    S]GTP\u03b3S binding in postmortem human brain membranes were optimized, and the responses induced by a series of agonists were pharmacologically characterized. The [\n                    <jats:sup>35<\/jats:sup>\n                    S]GTP\u03b3S binding assay was performed in postmortem human prefrontal cortical membranes by means of filtration techniques, and standardized as to GDP concentration, membrane protein content, MgCl\n                    <jats:sub>2<\/jats:sub>\n                    and NaCl concentrations in assay buffer, incubation period and effect of white matter contamination. Under the standard assay conditions, the specific [\n                    <jats:sup>35<\/jats:sup>\n                    S]GTP\u03b3S binding was stimulated by the addition of 15 compounds in a concentration\u2010dependent manner. Of these agonists,\n                    <jats:italic>R<\/jats:italic>\n                    (+)\u20108\u2010OH\u2010DPAT, UK\u201014,304, DAMGO and DPDPE showed apparently biphasic concentration\u2010response curves. As for these four responses, only higher\u2010potency site was pharmacologically characterized. The receptors involved in the responses investigated were 5\u2010HT\n                    <jats:sub>1A<\/jats:sub>\n                    receptor (probed with\n                    <jats:italic>R<\/jats:italic>\n                    (+)\u20108\u2010OH\u2010DPAT or 5\u2010HT), \u03b1\n                    <jats:sub>2A<\/jats:sub>\n                    \u2010adrenoceptor (UK\u201014,304 or (\u2212)\u2010epinephrine), M\n                    <jats:sub>2<\/jats:sub>\n                    \/M\n                    <jats:sub>4<\/jats:sub>\n                    mAChRs (carbachol), adenosine A\n                    <jats:sub>1<\/jats:sub>\n                    receptor (adenosine), histamine H\n                    <jats:sub>3<\/jats:sub>\n                    receptor (histamine), group II mGlu (\n                    <jats:sc>l<\/jats:sc>\n                    \u2010glutamate), GABA\n                    <jats:sub>B<\/jats:sub>\n                    receptor (baclofen), \u03bc\u2010opioid receptor (DAMGO or endomophin\u20101), \u03b4\u2010opioid receptor (DPDPE or SNC\u201080) and NOP (nociceptin). Although dopamine also activated specific [\n                    <jats:sup>35<\/jats:sup>\n                    S]GTP\u03b3S binding, this response was likely mediated via \u03b1\n                    <jats:sub>2A<\/jats:sub>\n                    \u2010adrenoceptor, but not dopamine receptor subtypes. The present study provides us with fundamental aspects of the strategy for elucidation of probable abnormalities of neural signalling mediated by G proteins activated through multiple GPCRs in the brain of psychiatric patients.\n                  <\/jats:p>","DOI":"10.1111\/bcpt.13183","type":"journal-article","created":{"date-parts":[[2018,12,3]],"date-time":"2018-12-03T04:25:40Z","timestamp":1543811140000},"page":"649-659","update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":6,"title":["Optimization and pharmacological characterization of receptor\u2010mediated G\n                    <sub>i\/o<\/sub>\n                    activation in postmortem human prefrontal cortex"],"prefix":"10.1111","volume":"124","author":[{"given":"Yuji","family":"Odagaki","sequence":"first","affiliation":[{"name":"Department of Psychiatry, Faculty of Medicine Saitama Medical University Saitama Japan"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Masakazu","family":"Kinoshita","sequence":"additional","affiliation":[{"name":"Department of Psychiatry, Faculty of Medicine Saitama Medical University Saitama Japan"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Toshio","family":"Ota","sequence":"additional","affiliation":[{"name":"Department of Psychiatry, Faculty of Medicine Saitama Medical University Saitama Japan"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"J. 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