The discovery of a novel high-affinity and selective dopamine D4 recep
tor antagonist, L-745,870, and the results of clinical trials with thi
s compound are reviewed. Despite several lines of evidence which sugge
st that a selective D4 receptor antagonist may be an effective antipsy
chotic agent with a lower propensity to induce extrapyramidal side-eff
ects, L-745,870 was ineffective as an antipsychotic in humans.