Figure 14.
(Top) Neuroleptic doses for catalepsy (in rats) versus the selectivity ratio of the antipsychotic radioligand-independent dissociation constants (K values, Table 3) for the cloned dopamine D2 and the human cloned serotonin-2A receptors. (Bottom) Neuroleptic doses for catalepsy versus the selectivity ratio of the neuroleptic K values for the dopamine D2 and D4 receptors. Neuroleptics with low affinity for D2 (remoxipride, perlapine, seroquel and melperone) (i.e., K > 30 nM) were omitted in both correlations, based on the concept that these loosely bound neuroleptics are atypical by virtue of being readily displaced by endogenous dopamine. The correlation coefficient is given for those drugs which are encircled by a "balloon," omitting thioridazine because of its uniquely potent anticholinergic and anticataleptic action. The correlation coefficient of 0.77 (bottom) was statistically significant at the P<0.02 level. The data for Glaxo 1192U90 and clozapine are for catalepsy in the mouse (67,136).
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published 2000