Effects of dopaminergic agonists and antagonists on [3H]apomorphine binding to striatal membranes of rat brain was examined. Haloperidol and spiroperidol exhibited biphasic inhibition of [3H]apomorphine binding; one of which had the Hill coefficient of 0.9, whereas the other had that of 0.4. The former accounted for 65% of [3H]apomorphine binding while the latter consisted of 35% of the binding. Furthermore, the latter disappeared after kainic acid lesions. On the other hand, sulpiride and metoclopramide reduced [3H]apomorphine binding to 31% with the Hill coefficient of 0.9. The inhibition of [3H]apomorphine binding with the Hill coefficient of 0.4 which was shown by haloperidol and spiroperidol was not observed for sulpiride and metoclopramide. Previously, we demonstrated non- and positive-cooperative [3H]apomorphine binding to stiatal membranes. In the present study, it has been also shown that sulpiride inhibits non-cooperative [3H]apomorphine binding leaving that with allosteric properties unaffected. No inhibition of dopamine-sensitive adenylate cyclase was observed by 10(-4) M sulpiride while 90% inhibition was obtained with 10(-5) M haloperidol. From those results, it is suggested that non-cooperative [3H]spomorphine binding is not coupled with dopamine-sensitive adenylate cyclase.