TABLE 1

Wild-type and chimeric 5-HT3A receptor potencies and efficacies

Two-way ANOVA revealed a significant effect of receptor construct on 5-HT concentration-response curves [F(5, 349) = 92.5, P < 0.0001].

5-HT
2-OHMBA
2-OHMBA
EC50
 EC50/Emax
 IC50
μM mM μM
MWT 0.9 ± 0.06 2.0 ± 0.24, 63% NA
M244H 1.2 ± 0.02 1.3 ± 0.15, 43% NA
H176M244H 1.7 ± 0.3a 5.0 ± 0.4,b 57% NA
HWT 1.5 ± 0.01 NA 1.5 ± 0.1
H239M 3.9 ± 0.03b,d NA 2.0 ± 0.08c
H181H239M
1.2 + 0.03
NA
3.0 + 0.13d

  • NA, not applicable.

  • ↵ a P < 0.01 compared with MWT.

  • ↵ b P < 0.001 compared with MWT.

  • ↵ c P < 0.05 compared with HWT.

  • ↵ d P < 0.001 compared with HWT, Bonferroni's multiple comparison test.