{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,8,13]],"date-time":"2026-08-13T22:24:03Z","timestamp":1786659843553,"version":"build-2736575974"},"reference-count":34,"publisher":"Wiley","issue":"4","license":[{"start":{"date-parts":[[2003,9,29]],"date-time":"2003-09-29T00:00:00Z","timestamp":1064793600000},"content-version":"vor","delay-in-days":0,"URL":"http:\/\/onlinelibrary.wiley.com\/termsAndConditions#vor"}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Synapse"],"published-print":{"date-parts":[[2003,12,15]]},"abstract":"<jats:title>Abstract<\/jats:title><jats:p>The effects of dopamine (DA) on the function of human 5\u2010HT<jats:sub>1A<\/jats:sub> receptors expressed in <jats:italic>Xenopus<\/jats:italic> oocytes and CHO\u2010K1 cells were investigated. In addition, the effect of DA on the activation of three different types of human 5\u2010HT receptors (5\u2010HT<jats:sub>1A<\/jats:sub>, 5\u2010HT<jats:sub>2C<\/jats:sub>, and 5\u2010HT<jats:sub>3<\/jats:sub>) were studied comparatively in <jats:italic>Xenopus<\/jats:italic> oocyte expression system. Application of 5\u2010HT or DA in oocytes coexpressing 5\u2010HT<jats:sub>1A<\/jats:sub> receptors and G\u2010protein\u2010activated inwardly rectifying potassium channels (GIRK1) induced inward currents with respective EC<jats:sub>50<\/jats:sub> values of 4.2 nM and 11.2 \u03bcM. Maximal responses induced by DA were 85 \u00b1 4% of maximal 5\u2010HT currents and DA responses were blocked by the specific 5\u2010HT<jats:sub>1A<\/jats:sub> antagonist, WAY\u2010100635 (50 nM). In CHO\u2010K1 cells expressing 5\u2010HT<jats:sub>1A<\/jats:sub> receptors, 5\u2010HT and DA inhibited the specific binding of selective antagonist [<jats:sup>3<\/jats:sup>H]\u20108\u2010OH\u2010DPAT with IC<jats:sub>50<\/jats:sub> values of 10.2 nM and 1.4 \u03bcM, and both 5\u2010HT and DA inhibited the forskolin\u2010induced accumulation of cAMP. In oocytes expressing 5\u2010HT<jats:sub>2C<\/jats:sub> receptors, 5\u2010HT and DA induced inward currents with respective EC<jats:sub>50<\/jats:sub> values of 6.2 nM and 67.7 \u03bcM. Magnitudes of maximal DA induced currents were 42 \u00b1 3% of maximal 5\u2010HT responses and blocked by the 5\u2010HT<jats:sub>2<\/jats:sub> antagonist, piperazine (1 \u03bcM). In oocytes expressing 5\u2010HT<jats:sub>3<\/jats:sub> receptors, 5\u2010HT and DA induced fast inward currents with respective EC<jats:sub>50<\/jats:sub> values of 2.1 \u03bcM and 266.3 \u03bcM. Maximal DA induced currents were 37 \u00b1 3% of maximal 5\u2010HT responses and blocked the specific 5\u2010HT<jats:sub>3<\/jats:sub> antagonist LY\u2010278584 (0.1 \u03bcM). Comparison of the potencies and efficacies of 5\u2010HT and DA indicated that the relative potency of DA increased in the order of 5\u2010HT<jats:sub>3<\/jats:sub> &gt; 5\u2010HT<jats:sub>1A<\/jats:sub> &gt; 5\u2010HT<jats:sub>2C<\/jats:sub>, and relative efficacy increased in the order of 5\u2010HT<jats:sub>1A<\/jats:sub> &gt; 5\u2010HT<jats:sub>2C<\/jats:sub> &gt; 5\u2010HT<jats:sub>3<\/jats:sub>. These results suggest that although DA activates different subtypes of human 5\u2010HT receptors directly, the potency and efficacy of the binding site varies significantly among different receptors. Synapse 50:303\u2013313, 2003. Published 2003 Wiley\u2010Liss, Inc.<\/jats:p>","DOI":"10.1002\/syn.10273","type":"journal-article","created":{"date-parts":[[2003,10,7]],"date-time":"2003-10-07T08:05:04Z","timestamp":1065513904000},"page":"303-313","source":"Crossref","is-referenced-by-count":20,"title":["Direct activation by dopamine of recombinant human 5\u2010HT<sub>1A<\/sub> receptors: Comparison with human 5\u2010HT<sub>2C<\/sub> and 5\u2010HT<sub>3<\/sub> 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