Tags: Drug.
Vanoxerine (GBR-12909) is a piperazine derivative which is a potent and selective DRI. GBR-12909 binds to the target site on the DAT ~ 500 times more strongly than cocaine[citation needed] but simultaneously inhibits the release of dopamine. This combined effect only slightly elevates dopamine levels giving vanoxerine only mild stimulant effects. Vanoxerine has also been observed to be a potent blocker of the IKr (hERG) channel.