Skip to main content
. Author manuscript; available in PMC: 2012 Dec 30.
Published in final edited form as: Eur J Pharmacol. 2011 Oct 12;673(1-3):1–12. doi: 10.1016/j.ejphar.2011.10.006

Table 3.

EC/IC50 and E/IMAX values of ligands to activate/inactivate 5-HT2C receptor-mediated phospholipase C signaling. Functional assays were performed in HEK cells transiently expressing WT, S3.36A or Y7.43A 5-HT2C receptors. EMAX/IMAX values represent percent change from baseline. Data shown are means and S.E.M. (shown in parentheses) of at least 3 independent experiments performed with triplicates. EC/IC50 fold change represents the quantitative fold difference between EC/IC50 values of WT and S3.36A or WT and Y7.43A 5-HT2C receptors, respectively.

LIGAND WT 5-HT2C S3.36A Y7.43A FOLD
CHANGE
EC/IC50
(nM)
E/Imax EC/IC50
(nM)
E/Imax EC/IC50
(nM)
E/Imax EC/IC50
Serotonin 5.5 (1.3) 204.7 (11.6) 289.1
(40.4)a
998.4
(137.1)b
158.7
(19.9)a
223.4 (22.7) 52.6, 28.9
N(CH3)2-
PAT
61.1 (18.2) 163.0 (9.7) 682.5
(102.5)a
588.0 (62.0)
b
519.7
(98.8)a
180.8
(14.2)
11.2, 8.5
Mesulergine 23.9 (8.3) 82.9 (1.9) 19.9 (8.2) 152.0 (9.2)b 38.9 (13.3) 79.3 (2.5) 0.8, 1.6
a

significantly different from WT 5-HT2C.