{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,8,18]],"date-time":"2026-08-18T14:37:09Z","timestamp":1787063829478,"version":"build-2736575974"},"reference-count":18,"publisher":"Wiley","issue":"5","license":[{"start":{"date-parts":[[2009,2,5]],"date-time":"2009-02-05T00:00:00Z","timestamp":1233792000000},"content-version":"vor","delay-in-days":4114,"URL":"http:\/\/onlinelibrary.wiley.com\/termsAndConditions#vor"}],"content-domain":{"domain":["bpspubs.onlinelibrary.wiley.com"],"crossmark-restriction":true},"short-container-title":["British J Pharmacology"],"published-print":{"date-parts":[[1997,11]]},"abstract":"<jats:p>\n                    <jats:list list-type=\"explicit-label\">\n                      <jats:list-item>\n                        <jats:p>\n                          We discovered a novel \u03b3\u2010aminobutyric acid\n                          <jats:sub>A<\/jats:sub>\n                          (GABA\n                          <jats:sub>A<\/jats:sub>\n                          ) receptor ligand displaying seemingly opposite functionalities, depending on the \u03b1 isoform of the \u03b1x\u03b22\u03b32 subtypes. PNU\u2010107484A enhanced GABA\u2010induced Cl\n                          <jats:sup>\u2212<\/jats:sup>\n                          currents in the \u03b11\u03b22\u03b32 subtype, but inhibited the currents in the \u03b13\u03b22\u03b32 and \u03b16\u03b22\u03b32 subtypes, and its half\u2010maximal concentrations in the subtypes were 3.1\u00b10.5, 4.2\u00b11, and 3.5\u00b10.2\u2003\u03bc\n                          <jats:sc>M<\/jats:sc>\n                          , respectively, without showing much dependency on \u03b1 isoforms.\n                        <\/jats:p>\n                      <\/jats:list-item>\n                      <jats:list-item>\n                        <jats:p>\n                          In the \u03b11\u03b22 subtype, the drug at concentrations up to 40\u2003\u03bc\n                          <jats:sc>M<\/jats:sc>\n                          showed no effect on GABA\u2010induced Cl\n                          <jats:sup>\u2212<\/jats:sup>\n                          currents, suggesting the requirement of the \u03b3 subunit for its action.\n                        <\/jats:p>\n                      <\/jats:list-item>\n                      <jats:list-item>\n                        <jats:p>\n                          PNU\u2010107484A behaved like a positive allosteric modulator of the \u03b11\u03b22\u03b32 subtype with its binding site distinct from those for benzodiazepines, barbiturates and neurosteroids. With the \u03b13\u03b22\u03b32 subtype, the drug behaved like a non\u2010competitive inhibitor of GABA, thus blocking Cl\n                          <jats:sup>\u2212<\/jats:sup>\n                          currents by GABA alone or in the presence of pentobarbitone and neurosteroids.\n                        <\/jats:p>\n                      <\/jats:list-item>\n                      <jats:list-item>\n                        <jats:p>\n                          It appears that PNU\u2010107484A is a unique GABA\n                          <jats:sub>A<\/jats:sub>\n                          receptor ligand with \u03b1 isoform\u2010dependent functionalities, which may provide a basis for development of \u03b1 isoform\u2010selective ligands, and it could be useful as a probe to investigate the physiological roles of the various \u03b1 isoform subtypes.\n                        <\/jats:p>\n                      <\/jats:list-item>\n                    <\/jats:list>\n                  <\/jats:p>\n                  <jats:p>\n                    <jats:italic>British Journal of Pharmacology<\/jats:italic>\n                    (1997)\n                    <jats:bold>122<\/jats:bold>\n                    , 821\u2013824; doi:\n                    <jats:ext-link xmlns:xlink=\"http:\/\/www.w3.org\/1999\/xlink\" ext-link-type=\"doi\" xlink:href=\"10.1038\/sj.bjp.0701450\">10.1038\/sj.bjp.0701450<\/jats:ext-link>\n                  <\/jats:p>","DOI":"10.1038\/sj.bjp.0701450","type":"journal-article","created":{"date-parts":[[2005,1,28]],"date-time":"2005-01-28T14:15:39Z","timestamp":1106921739000},"page":"821-824","update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":2,"title":["PNU\u2010107484A with\n                    <i>\u03b1<\/i>\n                    isoform\u2010dependent functional changes in\n                    <i>\u03b1<\/i>\n                    x\n                    <i>\u03b2<\/i>\n                    2\u03b32 subtypes of rat recombinant GABA\n                    <sub>A<\/sub>\n                    receptors"],"prefix":"10.1111","volume":"122","author":[{"given":"Haesook K.","family":"Im","sequence":"first","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Wha Bin","family":"Im","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Donald B.","family":"Carter","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Theresa M.","family":"Schwartz","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Gordon L.","family":"Bundy","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Philip F.","family":"Von Voigtlander","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"311","published-online":{"date-parts":[[2009,2,5]]},"reference":[{"key":"e_1_2_5_2_1","doi-asserted-by":"publisher","DOI":"10.1111\/j.1749-6632.1993.tb38047.x"},{"key":"e_1_2_5_3_1","doi-asserted-by":"publisher","DOI":"10.1111\/j.1471-4159.1991.tb11443.x"},{"key":"e_1_2_5_4_1","doi-asserted-by":"publisher","DOI":"10.1016\/0896-6273(90)90337-F"},{"key":"e_1_2_5_5_1","first-page":"166","article-title":"Recent advances in the molecular biology of benzodiazepine receptors and in the structure activity relationship of their agonists and antagonists","volume":"14","author":"Hafely W.","year":"1985","journal-title":"Adv. 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