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Table 1 Binding affinities of olanzapine, compounds 8a, 8b, and 8c for 5HT 2A , D 2 , and H 1 receptors

From: Novel olanzapine analogues presenting a reduced H1 receptor affinity and retained 5HT2A/D2 binding affinity ratio

Compound K i ± SDa(nM) pKiratio 5HT2A/D2
D2 5HT2A H1
olanzapine 67.72 ± 9.21 4.22 ± 0.77 0.13 ± 0.02 1.17
8c 54.51 ± 12.12 3.70 ± 0.74 1.95 ± 0.33* 1.16
8b 791.08 ± 83.19** 81.20 ± 2.43* 13.63 ± 2.68*** 1.16
8a 3939.90 ± 437.35*** 787.00 ± 29.81*** 33.50 ± 7.39*** 1.16
  1. a Values are the mean ± SD of four to six experiments and represent the concentration giving half maximal inhibition of [3H]-Spiperone (D2), [3H]-Ketanserine (5HT2A), and [3H]-Pyrilamine (H1) binding to rat tissue homogenate. *P < 0.05, **P < 0.01, and ***P < 0.001vs olanzapine values.