Patent Evaluation: Novel N-cycloalkylamines as Sigma Agonists

Abstract

SummaryNovelty: N-Cycloalkylamines are disclosed with activity as a receptor agonists. These compounds are potentially useful as antipsychotic, anticonvulsant and anti-ulcer agents.Biology: Competitive binding data are presented showing that the compounds have selective affinity for the sigma receptor in comparison to the, μ, δ and PCP receptors. Psychotropic activity is demonstrated by inhibition of picrotoxin-induced convulsion (ED50 values about 50 mg/kg, ip, and 100 mg/kg, po). Anti-ulcer activity is shown by inhibition of cysteamine induced gastrointestinal ulceration.Chemistry: Syntheses of the compounds are outlined in two schemes, forming a subsidiary part of the claim with ten examples. 1-[2-(N-Cycloproyimethyl-N-methyl)amino-2-phenyl-butyl]-2-(2-thienyl)cyclopropane is one of two specifically claimed compounds.