Table 3.

EC50 values (μm) and Hill coefficients for 5-HT activation of 153-Tyr mutant receptors (n = 3-6) (A) and [3H]granisetron binding affinities of Tyr mutants (B)

A
153- EC50 ± SE nH ± SE
Ala 120 ± 9.43* 2.43 ± 0.38
Ser 84.1 ± 5.60* 2.54 ± 0.37
Phe 22.5 ± 0.43* 2.60 ± 0.11
4-F-Phe 19.7 ± 1.22* 1.82 ± 0.14*
F5-Phe (>500)
Tyr (WT) 1.15 ± 0.04 2.78 ± 0.20
mTyr (>500)
4-Me-Phe 18.2 ± 0.48* 2.48 ± 0.11
4-MeO-Phe 6.65 ± 0.27* 1.98 ± 0.12*
B
153- Kd (nm) n
Ala 3.62 ± 1.75* 3
Ser NB 6
Phe 0.90 ± 0.20 5
Tyr (WT) 0.32 ± 0.035 7
  • Data in B are from Price and Lummis (2004). Substitutions have been approximately ordered by increasing size. The asterisk indicates a significant difference (p<0.05) to Tyr. NB, No binding; WT, wild type.