Sigma receptors are associated with various central nervous system disorders schizophrenia, regulation of motor behavior, convulsions, anxiety, and the psychostimulant effects of drugs of abuse. At least two different types of sigma (sigma-1 and sigma-2) receptors have been identified. It has been demonstrated that antagonism of the sigma-1 receptor can attenuate the toxic and stimulant effects of methamphetamine. We have designed and synthesized several piperazine derivatives that possess high affinity and selectivity for sigma receptors.  These compounds have been tested in vivo and demonstrated blockade of the behavioral and toxic effects of methamphetamine.

Investigation of piperazine derivatives as sigma receptor ligands with methamphetamine antagonist activity

244th National Meeting (2012)

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