The binding of the neuroleptic, [3H] spiperone, to rabbit spermatozoa was investigated. Binding was partially inhibited by haloperidol, mianserin or epinephrine. Mixtures of two of the three inhibitors reduced binding further, but binding of the radioligand to spermatozoa was lowest in the presence of all three inhibitors. Unlabeled spiperone eliminated binding. Cholinergic ligands, GABA, and beta-adrenergic ligands, had little effect on binding. Spiperone binding occurred to both heads and tails suggesting that alpha 1-adrenergic, D2-dopamine and S2-serotonin binding sites are present in the head and/or tail of rabbit spermatozoa.