GZ-11608 is a potent and selective vesicular monoamine transporter-2 (VMAT2) inhibitor with high affinity (Ki = 25 nM) . GZ-11608 decreases methamphetamine-induced dopamine release from isolated synaptic vesicles from brain dopaminergic neurons. GZ-11608 exhibits rapid brain penetration and without neurotoxicity. GZ-11608 can be used for the research of methamphetamine use disorder[1].