2-Phenyl-4-(aminomethyl)imidazoles as Potential Antipsychotic Agents. Synthesis and Dopamine D2 Receptor Binding

Andrew Thurkauf, Alan Hutchison, John Peterson, Linda J. Cornfield, Robin Meade, K. Kwasind Huston, Kristine Harris, Philip C. Ross, T V Ramabhadran

Journal of Medicinal Chemistry · 1995 · 25 citations · 0 references

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Abstract

A series of 1-phenyl-3-(aminomethyl)pyrroles were prepared in two steps from aniline and their affinities for D2, D3, and D4 dopamine receptor subtypes determined. A 15-fold selectivity for cloned human D4 receptors over cloned African Green monkey D2 receptors was observed with 1-(2-pyridyl)-4-[[3-(1-phenylpyrrolyl)]methyl]piperazine.