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Bioorg Med Chem Lett. 2003 Feb 24;13(4):749-51.

1,4-dibenzylpiperazines possess anticocaine activity.

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Department of Pharmaceutical Sciences, University of Maryland School of Pharmacy, 20 North Pine Street, Baltimore, MD 21201, USA.


N,N-dibenzylpiperazines have high affinity for sigma receptors, and we aimed to increase their anticocaine activity by introducing substituents known to enhance such activity in other sigma ligands. Ligands with high affinity for sigma-1 receptors resulted, but their activity in attenuating cocaine-induced convulsions did not correlate with sigma-1 binding affinity, and may be more closely related to their sigma-2 binding affinities.

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