{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2025,10,18]],"date-time":"2025-10-18T10:18:23Z","timestamp":1760782703307},"reference-count":58,"publisher":"Wiley","issue":"8","license":[{"start":{"date-parts":[[2009,2,2]],"date-time":"2009-02-02T00:00:00Z","timestamp":1233532800000},"content-version":"vor","delay-in-days":2499,"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":[[2002,4]]},"abstract":"<jats:p>\n<jats:list list-type=\"explicit-label\">\n<jats:list-item><jats:p>We examine the sensitivity of GABA<jats:sub>A<\/jats:sub> and glycine receptors (same ionotropic superfamily) to oleamide. We address subunit\u2010dependence\/modulatory mechanisms and analogies with depressant drugs.<\/jats:p><\/jats:list-item>\n<jats:list-item><jats:p>Oleamide modulated human GABA<jats:sub>A<\/jats:sub> currents (\u03b1<jats:sub>1<\/jats:sub>\u03b2<jats:sub>2<\/jats:sub>\u03b3<jats:sub>2L<\/jats:sub>) in oocytes (EC<jats:sub>50<\/jats:sub>, 28.94\u00b1s.e.mean of 1.4\u2003\u03bc<jats:sc>M<\/jats:sc>; Maximum 216%\u00b135 of control, <jats:italic>n<\/jats:italic>=4). Modulation of human \u03b11 glycine homo\u2010oligomers (significant), was less marked, with a lower EC<jats:sub>50<\/jats:sub> (<jats:italic>P<\/jats:italic>&lt;0.05) than GABA receptors (EC<jats:sub>50<\/jats:sub>, 22.12\u00b11.4\u2003\u03bc<jats:sc>M<\/jats:sc>; Maximum 171%\u00b130, <jats:italic>n<\/jats:italic>=11).<\/jats:p><\/jats:list-item>\n<jats:list-item><jats:p>Only the hypnogenic <jats:italic>cis<\/jats:italic> geometric isomer enhanced glycine currents (without altering slope or maximal current, it reduced the glycine EC<jats:sub>50<\/jats:sub> from 322 to 239\u2003\u03bc<jats:sc>M<\/jats:sc>: <jats:italic>P<\/jats:italic>&lt;0.001). Modulation was not voltage\u2010dependent or associated with a shift in E<jats:sub>r<\/jats:sub>.<\/jats:p><\/jats:list-item>\n<jats:list-item><jats:p>\u03b21 containing GABA<jats:sub>A<\/jats:sub> receptors (insensitive to many depressant drugs) were positively modulated by oleamide. Oleamide efficacy was <jats:italic>circa<\/jats:italic> 2\u00d7 greater at \u03b1<jats:sub>1<\/jats:sub>\u03b2<jats:sub>1<\/jats:sub>\u03b3<jats:sub>2L<\/jats:sub> than \u03b1<jats:sub>1<\/jats:sub>\u03b2<jats:sub>2<\/jats:sub>\u03b3<jats:sub>2L<\/jats:sub> (<jats:italic>P<\/jats:italic>=0.007). Splice variation in \u03b3 subunits did not alter oleamide sensitivity.<\/jats:p><\/jats:list-item>\n<jats:list-item><jats:p><jats:italic>cis<\/jats:italic>\u20109,10\u2010Octadecenoamide had no effect on the equilibrium binding of [<jats:sup>3<\/jats:sup>H]\u2010muscimol or [<jats:sup>3<\/jats:sup>H]\u2010EBOB to mouse brain membranes. It does not directly mimic GABA, or operate as a neurosteroid\u2010, benzodiazepine\u2010 or barbiturate\u2010like modulator of GABA<jats:sub>A<\/jats:sub>\u2010receptors.<\/jats:p><\/jats:list-item>\n<jats:list-item><jats:p>The transport of [<jats:sup>3<\/jats:sup>H]\u2010GABA into mouse brain synaptoneurosomes was unaffected by high micromolar concentrations of <jats:italic>cis<\/jats:italic>\u20109,10\u2010octadecenoamide. Oleamide does not enhance GABA\u2010ergic currents or prolong IPSCs by inhibiting GABA transport.<\/jats:p><\/jats:list-item>\n<jats:list-item><jats:p>Oleamide is a non\u2010selective modulator of inhibitory ionotropic receptors. The sleep lipid exerts its effects indirectly, or at a novel recognition site on the GABA<jats:sub>A<\/jats:sub> complex.<\/jats:p><\/jats:list-item>\n<\/jats:list>\n<\/jats:p><jats:p><jats:italic>British Journal of Pharmacology<\/jats:italic> (2002) <jats:bold>135<\/jats:bold>, 1977\u20131987; doi:<jats:ext-link xmlns:xlink=\"http:\/\/www.w3.org\/1999\/xlink\" ext-link-type=\"doi\" xlink:href=\"10.1038\/sj.bjp.0704651\">10.1038\/sj.bjp.0704651<\/jats:ext-link><\/jats:p>","DOI":"10.1038\/sj.bjp.0704651","type":"journal-article","created":{"date-parts":[[2005,1,28]],"date-time":"2005-01-28T21:51:22Z","timestamp":1106949082000},"page":"1977-1987","update-policy":"http:\/\/dx.doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":28,"title":["The sleep hormone oleamide modulates inhibitory ionotropic receptors in mammalian CNS <i>in vitro<\/i>"],"prefix":"10.1111","volume":"135","author":[{"given":"Leanne","family":"Coyne","sequence":"first","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"George","family":"Lees","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Russell A","family":"Nicholson","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Jian","family":"Zheng","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Katherine D","family":"Neufield","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"311","published-online":{"date-parts":[[2009,2,2]]},"reference":[{"key":"e_1_2_7_2_1","doi-asserted-by":"publisher","DOI":"10.1097\/00001756-199904060-00010"},{"key":"e_1_2_7_3_1","doi-asserted-by":"publisher","DOI":"10.1016\/0006-8993(78)90385-2"},{"key":"e_1_2_7_4_1","doi-asserted-by":"publisher","DOI":"10.1073\/pnas.94.20.11031"},{"key":"e_1_2_7_5_1","doi-asserted-by":"publisher","DOI":"10.1016\/S0165-6147(99)01405-4"},{"key":"e_1_2_7_6_1","doi-asserted-by":"publisher","DOI":"10.1016\/S0197-0186(99)00037-6"},{"key":"e_1_2_7_7_1","first-page":"11","article-title":"Inhibition of \u03b3\u2010aminobutyric acid\u2010stimulated chloride flux in mouse brain vesicles by polychlorocycloalkane and pyrethroid insecticides","volume":"7","author":"BLOOMQUIST J.R.","year":"1986","journal-title":"NeuroToxicol."},{"key":"e_1_2_7_8_1","doi-asserted-by":"publisher","DOI":"10.1073\/pnas.95.9.4810"},{"key":"e_1_2_7_9_1","doi-asserted-by":"publisher","DOI":"10.1073\/pnas.95.8.4102"},{"key":"e_1_2_7_10_1","doi-asserted-by":"publisher","DOI":"10.1016\/S0952-3278(96)90100-3"},{"key":"e_1_2_7_11_1","doi-asserted-by":"publisher","DOI":"10.1016\/S0028-3908(98)00208-1"},{"key":"e_1_2_7_12_1","doi-asserted-by":"publisher","DOI":"10.1016\/0048-3575(92)90002-H"},{"key":"e_1_2_7_13_1","doi-asserted-by":"publisher","DOI":"10.1126\/science.7770779"},{"key":"e_1_2_7_14_1","first-page":"598","article-title":"Barbiturate\u2010benzodiazepine interactions at the gamma\u2010aminobutyric acid\u2010A receptor in rat cerebrocortical synaptoneurosomes","volume":"77","author":"DELORY T.M.","year":"1993","journal-title":"Anesth. & Analg."},{"key":"e_1_2_7_15_1","doi-asserted-by":"publisher","DOI":"10.1038\/sj.bjp.0701417"},{"key":"e_1_2_7_16_1","doi-asserted-by":"publisher","DOI":"10.1038\/367607a0"},{"key":"e_1_2_7_17_1","doi-asserted-by":"publisher","DOI":"10.1016\/S0014-5793(99)01630-0"},{"key":"e_1_2_7_18_1","doi-asserted-by":"publisher","DOI":"10.1016\/0922-4106(95)90190-6"},{"key":"e_1_2_7_19_1","doi-asserted-by":"publisher","DOI":"10.1046\/j.1460-9568.1999.00709.x"},{"key":"e_1_2_7_20_1","doi-asserted-by":"publisher","DOI":"10.1126\/science.2581319"},{"key":"e_1_2_7_21_1","doi-asserted-by":"publisher","DOI":"10.1016\/0922-4106(94)90150-3"},{"key":"e_1_2_7_22_1","doi-asserted-by":"publisher","DOI":"10.1006\/abio.1999.4083"},{"key":"e_1_2_7_23_1","first-page":"1191","article-title":"Characterization of [3H]ethynylbicycloorthobenzoate ([3H]EBOB) binding and the action of insecticides on the \u03b3\u2010aminobutyric acid\u2010gated chloride channel in cultured cerebellar granule neurons","volume":"279","author":"HUANG J.","year":"1997","journal-title":"J. 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