GZ-11608, a selective and potent inhibitor of vesicular monoamine transporter-2 (VMAT2), presents a high affinity with a Ki value of 25 nM. It effectively reduces dopamine release induced by methamphetamine from isolated synaptic vesicles in brain dopaminergic neurons. GZ-11608 also demonstrates rapid penetration into the brain without exhibiting neurotoxicity, making it a valuable compound for researching methamphetamine use disorder [1].
GZN39838, also known as 6beta-Acetoxy-7alpha-hydroxyroyleanone is a natural blocker of Kv1.2 channels, not involving direct occlusion of the outer pore but depending on C-type inactivation.