Binding of antiparkinsonian ergot derivatives to the dopamine receptor

The effects of bromocriptine, lisuride and apomorphine on specific binding of 3H-spiroperidol to homogenates of rat caudate nucleus were studied. (+)-Butaclamol was used to define specific binding. Bromocriptine and lisuride inhibited binding markedly, in vitro and also 30 min after in vivo injection. Bromocriptine continued to inhibit binding 24h after a single injection and also after 4 days of drug administration. Lisuride did not affect net specific binding at these periods. Apomorphine produced a mild reduction in binding after 30 min but none after 4 days. It appears that the ergot alkaloids inhibit binding of 3H-spiroperidol by binding strongly to the dopamine receptor.