TABLE 1

Affinity constants (Ki) for SNF binding to wild-type and mutant 5-HT2 receptors

p values were obtained from F tests comparing curve fits of competition binding isotherms for two receptors. Where applicable, values are presented as mean ± S.E.

Receptor pKi S-NF (Ki S-NF)
nM
5-HT2B WT 7.66 ± 0.02 (22)
A1.35P 7.81 ± 0.07a (15)
A1.35S 7.77 ± 0.07 (17)
L1.38S 7.76 ± 0.06 (17)
I1.39T 7.84 ± 0.07a (14)
V1.42I 7.82 ± 0.09 (15)
V2.53L 6.43 ± 0.04a (370)
V2.53I 7.45 ± 0.04a (35)
V2.53A 5.48 ± 0.08a (3,300)
L3.29I 7.65 ± 0.07 (22)
M5.39V 6.65 ± 0.06a (220)
V2.53L, M5.39V 6.09 ± 0.08abc (810)
E7.36N 7.80 ± 0.06 (16)
S7.45C 7.65 ± 0.05 (22)
5-HT2A WT 5.73 ± 0.04 (1900)
5 HT2A L2.53V 5.74 ± 0.04 (1800)
5-HT2C WT 6.77 ± 0.05 (170)
5-HT2C V2.53L 5.8 ± 0.1a (2000)
  • a P < 0.05 compared with the appropriate wild type 5-HT2 receptor.

  • b P < 0.05 compared with the V2.53L 5-HT2B receptor.

  • c P < 0.05 compared with the M5.39V 5-HT2B receptor.