Table 1

Catalepsy, in vivo receptor occupancy, and in vitro Kivalues of the tested drugs for D1, D2, and mACh receptor

DoseCatalepsyReceptor Occupancy (%)Ki (nM)
D1D2mAChD1D2mACh
mg/kg sec
Haloperidol0.556.1  ± 16.941.3  ± 6.884.0  ± 1.90741.12,333
Flunarizine1017.9  ± 6.828.7  ± 8.168.3  ± 9.726.7  ± 3.9905713,513
Manidipine2016.4  ± 8.924.3  ± 5.538.0  ± 9.914.3  ± 6.5124117>10,000
Oxatomide1,00034.4  ± 12.58.0  ± 6.954.4  ± 8.935.7  ± 10.8>10,00025>10,000
Hydroxyzine100058.7  ± 7.975.1  ± 6.048.8  ± 10.6>10,000378>10,000
Meclizine300012.9  ± 5.836.9  ± 1.140.8  ± 11.0>10,000109>10,000
Homochlorcyclizine200036.8  ± 7.072.8  ± 14.487.3  ± 5.71,835157102
  • 3H-SCH23390, 3H-raclopride, and3H-QNB were used for labeling of dopamine D1, D2, and mACh receptor, respectively, both in vivo and in vitro. Data are means ± SE (receptor occupancy: N = 3–5; catalepsy: N = 7–8).