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Figure 4


Fig. 4. 5-HT is the only biogenic amine that acts as a potent agonist at 5-HT2βPan and 5-HT2βPro. (A) Non-transfected parental HEK cells do not show significant IP responses to any of the amines tested. (B) IP release in response to biogenic amines (10–3 mol l–1) in cells transiently expressing 5-HT2βPan. Cells expressing 5-HT2βPan demonstrate a greater than sixfold increase in IP release in response to 5-HT and a smaller but significant increase in response to dopamine and tyramine. Values are means ± s.e.m., N=3, **P<0.001 and *P<0.05 versus no drug control. (C) Dose–response curves of 5-HT2βPan to biogenic amines in IP assay. 5-HT2βPan responds to 5-HT (squares) with an EC50 of 52 nmol l–1. Dopamine (DA; circles) and tyramine (Tyr; triangles) activate the receptors only at very high concentrations. Non-transfected HEK cells do not respond to 5-HT (crosses). Values are means ± s.e.m., N=3. (D) IP release in response to biogenic amines (10–3 mol l–1) in cells transiently expressing 5-HT2βPro. IP release is increased more than fourfold in response to 1 mmol l–1 5-HT in cells expressing 5-HT2βPro. A smaller but significant increase in response to dopamine is observed. Values are means ± s.e.m., N=3, **P<0.001 vs no drug control. (E) Dose–response curves of 5-HT2βPro to biogenic amines in IP assay. 5-HT2βPro responds to 5-HT (squares) with an EC50 of 270 nmol l–1. Dopamine (circles) activates the receptor only at very high concentrations. Non-transfected HEK cells do not respond to 5-HT (crosses). Values are means ± s.e.m., N=3.