Table 1

Affinities of pimavanserin and antipsychotic drugs for monoamine receptors

DrugKi
5-HT2AD25-HT1A5HT2C5-HT65-HT7α1α2D1D3D4H1
nM
Pimavanserin0.13NDNDND50ND***#**
Haloperidol730.15260010,0005,0002632616002121153002
Melperone321992200^13421254578180150>10004.9230580
NDMC10.9^115^13.911.99.414.910513814.3^34203.4
Olanzapine3.07.5>1000^246104601403949107
Risperidone0.201.6025032251.40.775212.818.688
  • ND, not determined

  • * >1000;

  • # 88% inhibition at 10 μM (Vanover et al., 2006).

  • All other data are obtained from the National Institute of Mental Health Psychoactive Drug Screening Program web site (http://pdsp.med.unc.edu/) and are almost all for rat-cloned receptors, with the exception of data indicated by ^, which are from human-cloned receptors.