Vanoxerine dihydrochloride (GBR-12909; I-893) is a novel, potent, competitive and highly selective dopamine ruptake inhibitor (Ki=1 nM) with the potential for the treatment of atrial fibrillation. GBR 12909 effectively inhibits dopamine uptake in vivo. GBR-12909 binds to the target site on the dopamine transporter (DAT) ~ 50 times more strongly than cocaine, but simultaneously inhibits the release of dopamine. This combined effect only slightly elevates dopamine levels, giving vanoxerine only mild stimulant effects.[2] Vanoxerine has also been observed to be a potent blocker of the IKr (hERG) channel. GBR-12909 also binds with nanomolar affinity to the serotonin transporter.

纯度：≥98%

CAS：67469-78-7