TABLE 2

Affinity of FMPD and olanzapine for key neuronal receptors


Receptor

FMPD Ki

Olanzapine Ki
Mean ± S.E.M.
n
Mean ± S.E.M.
n
Human dopamine D1 30.3 ± 7.75 nM 4 150 ± 11.0 nM 3
Human dopamine D2s 6.33 ± 0.33 nM 4 10.5 ± 0.22 nM 732
Human dopamine D3 79.7 ± 8.18 nM 3 43.7 ± 8.95 nM 3
Human dopamine D4.4 102 ± 22.5 nM 3 57.3 ± 6.3 nM 3
Human dopamine D5 54.2 ± 8.38 nM 3 292 ± 68.8 nM 3
Rat dopamine D2 5.17 ± 1.9 nM 3 10.8 ± 0.96 nM 11
Human 5-HT1A 744 ± 123 nM 3 957 ± 43.3 nM 7
Human 5-HT1B 1093 ± 77.1 nM 3 759 ± 71.8 nM 7
Human 5-HT1D 629 ± 170 nM 3 954 ± 140 nM 7
Human 5-HT1E >3 μM 3 >2.5 μM 7
Human 5-HT1F 1435 ± 928 nM 2a 801 ± 72.0 nM 7
Human 5-HT2A 10.2 ± 2.57 nM 6 7.48 ± 0.79 nM 10
Human 5-HT2B 31.0 ± 12.6 nM 6 11.9 ± 2.26 nM 10
Human 5-HT2C 104 ± 16.9 nM 6 70.2 ± 4.98 nM 9
Human 5-HT4B >6 μM 3 >6 μM 3
Human 5-HT5A >6 μM 3 3395 ± 717 nM 3
Human 5-HT6 8.26 ± 1.36 nM 7 10.5 ± 0.38 nM 147
Human 5-HT7A 867 ± 90.5 nM 6 389 ± 62.6 nM 10
Rat histamine H1 72.0 ± 3.8 nM 3 4.2 ± 0.41 nM 3
Human histamine H1 30.3 ± 4.7 nM 6 3.74 ± 1.29 nM 3
Rat α1-adrenergic 19.9 ± 5.16 nM 7 37.3 ± 3.46 nM 6
Human α1A-adrenergic 101 ± 37.33 nM 4 183 ± 59.9 nM 4
Human α1B-adrenergic 126 ± 26.30 nM 4 723 ± 191 nM 4
Human α1D-adrenergic 408 ± 35.48 nM 3 812 ± 85.1 nM 3
Rat α2-adrenergic 295 ± 26.4 nM 5 265 ± 39.2 nM 4
Human α2A-adrenergic 767 ± 90.3 nM 6 2027 ± 134 nM 5
Human α2B-adrenergic 754 ± 82.0 nM 6 591 ± 53.4 nM 5
Human α2C-adrenergic 109 ± 7.94 nM 6 330 ± 38.4 nM 5
Rat muscarinic 59.2 ± 1.67 nM 3 7.87 ± 0.90 nM 4
Human muscarinic M1 84.1 ± 30.6 nM 3 149 ± 31.5 nM 7
Human muscarinic M2 206 ± 36.3 nM 3 142 ± 39.5 nM 7
Human muscarinic M3 1935 ± 612 nM 3 255 ± 62.5 nM 7
Human muscarinic M4 182 ± 24.9 nM 3 213 ± 56.1 nM 7
Human muscarinic M5 199 ± 50.6 nM 3 154 ± 44.2 nM 7
Human β1-adrenergic >1 μM 2 >10 μM 2
Human β2-adrenergic
>1 μM
2
>10 μM
2
  • a Where n = 2, the variance is expressed as ± 50% of the range.