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.