Synthesis of [N-C3-H3]-racemic-trans-1-phenyl-3-dimethylamino-6-chloro-7-hydroxy-1,2,3,4-tetra-hydronaphthalene (PAT-6)

The biological function of the sigma receptor in the central nervous system is not well understood at the present time. Once thought to be an opiate receptor, the sigma receptor has now been shown to have a neuromodulatory effect upon the synthesis of dopamine in the striatal nerve terminal. A novel sigma agonist, racemic-trans-1-phenyl-3-dimethylamino-6-chloro-7-hydroxy-1,2,3,4-tetrahydronaphthalene, PAT-6, has demonstrated the greatest potency of any compound tested to date as a sigma agonist in stimulating the synthesis of dopamine in vitro and may be functioning at a novel sigma receptor subtype. The synthesis of tritiated PAT-6 at high specific activity is described herein. This labeled ligand was prepared for use in radioreceptor binding studies in order to identify the putative sigma receptor subtype responsible for mediation of the stimulatory effect on in vitro dopamine synthesis. (author)