TABLE 1

Competition parameters of several antagonists for [3H](±)DOB-labeled receptors (binding assays) and for inhibition of 1 μM 5-HT-induced [3H]IP accumulation and [3H]AA release (functional assays) in CHO-FA4 cells expressing human 5-HT2A receptors

Values represent mean ± S.E.M. of at least three independent experiments performed in triplicate.



Binding Assays

Functional Assays
Ki
[3H]AA
High
Low
High [3H]IP IC50 IC50
High



High
Low
nM % nM nM %
Clozapine 3.47 ± 0.50 1819 ± 166 64.9 89.12 ± 3.10 2.04 ± 0.51 4176 ± 1458 56.33
Ketanserina 4.36 ± 0.82 10964 ± 1021 24.1 9.77 ± 1.01 1.73 ± 0.60 7658 ± 139 29.74
Risperidone 0.16 ± 0.03 549.5 ± 195 60.4 0.89 ± 0.51 0.11 ± 0.03 309.1 ± 147.5 53.80
MDL100,907a 0.16 ± 0.02 380.2 ± 148 59.5 0.13 ± 0.02 0.07 ± 0.05 76.8 ± 18.2 49.95
Haloperidol 416.8 ± 59.4 223.8 ± 26.2 234.4 ± 33.1
Mesulerginea

151.3 ± 9.95

199 ± 82

524.8 ± 124.0

  • a Binding data are from López-Giménez et al. (2001).