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].