TABLE 3

Affinity constants (Ki) for SNF and congeners at wild-type and V2.53L 5-HT2B receptors and wild-type 5-HT2C and 5-HT2A 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.

Drug pKi(Ki)
WT V2.53L WT2C WT2A
nM
SNF 7.76 ± 0.05 (17) 6.64 ± 0.07d (230) 7.16 ± 0.07 (69) 5.74 ± 0.08 (1,800)
RNF 7.21 ± 0.04 (62) 6.84 ± 0.07d (140) 7.07 ± 0.08 (85) 5.85 ± 0.07 (1,400)
α-Desmethyl-NF 7.26 ± 0.06a (55) 6.58 ± 0.05bd (260) 7.06 ± 0.07 (87) 5.87 ± 0.06 (1,300)
α-Ethyl-NF 6.11 ± 0.08abc (780) 6.44 ± 0.08abcd (360) 6.0 ± 0.1abc (1,000) 5.0 ± 0.1abc (10.000)

  • ↵ a P < 0.05 compared with S-(+)-NF.

  • ↵ b P < 0.05 compared with R-(-)-NF.

  • ↵ c P < 0.05 compared with α-desmethyl-NF.

  • ↵ d P < 0.05 compared with WT.