NE-100, A NOVEL SIGMA-RECEPTOR LIGAND - IN-VIVO TESTS

It has been suggested that sigma receptor antagonists may be useful as antipsychotic drugs. N, -2-[4-methoxy-3-(2-phenylethoxy)phenyl]-ethyl amine monohydrochloride (NE-100) is a novel compound with high affinit y for the sigma receptor (IC50 = 4.16 nM), but low affinity (IC50 > 10 000 nM) for D1, D2, 5-HT1A, 5-HT2 and phencyclidine (PCP) receptors. T he head-weaving behavior induced by either (+)SKF10047 or PCP was dose -dependently antagonized by NE-100 with oral ED50 at 0.27 and 0.12 mg/ kg, respectively. NE-100 did not affect dopamine agonists-induced ster eotyped behavior and/or hyperactivity. NE-100 failed to induce catalep sy in rats. These findings indicate that NE-100 may have antipsychotic activity without the liability of motor side effects typical of neuro leptics.