Metaphit, the first electrophilic affinity ligand specific for phencyclidine receptors, initially prepared by us in the form of its hydrochloride salt, was converted to its more water soluble methanesulfonate salt. The metaphit methanesulfonate has been found to be a very useful compound for discerning the multiplicity of phencyclidine receptors in various brain areas. The compound has been examined in vitro, in vivo in the rat and the pigeon, and in electrophysiological studies. Several other affinity ligands for the phencyclidine receptor were also synthesized.