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David B. Horton, Justin R. Nickell, Guangrong Zheng, Peter A. Crooks and Linda P. Dwoskin GZ-793A, a lobelane analog, interacts with the vesicular monoamine transporter-2 to inhibit the effect of methamphetamine Journal of Neurochemistry 127

Version of Record online: 19 AUG 2013 | DOI: 10.1111/jnc.12371

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GZ-793A inhibits methamphetamine-evoked dopamine release from synaptic vesicles through a surmountable allosteric mechanism and interacts with several sites on the vesicular monoamine transporter-2 (VMAT2), including high- and-low affinity intravesicular dopamine release sites, high-affinity extravesicular dopamine uptake sites and low-affinity extravesicular dihydrotetrabenazine binding sites. VMAT2 interactions likely underlie the ability of GZ-793A to attenuate the neurochemical and behavioral effects of methamphetamine.

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