(Top) Neuroleptic doses for catalepsy (in rats) versus the
selectivity ratio of the antipsychotic radioligand-independent dissociation
constants (K values,  )
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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