Catalog No.: PC-47107Not For Human Use, Lab Use Only.
GZ-11608 is a potent and selective vesicular monoamine transporter-2 (VMAT2) inhibitor with Ki of 25 nM, GZ-11608 (EC50=620 nM) released vesicular dopamine 25-fold less potently than it inhibited VMAT2 dopamine uptake.
GZ-11608 is a potent and selective vesicular monoamine transporter-2 (VMAT2) inhibitor with Ki of 25 nM, GZ-11608 (EC50=620 nM) released vesicular dopamine 25-fold less potently than it inhibited VMAT2 dopamine uptake.
GZ-11608 displays selectivity (92-1180-fold) for VMAT2 over nicotinic receptors, dopamine transporter, and hERG, suggesting low side-effects.
GZ-11608 competitively inhibited methamphetamine-evoked vesicular dopamine release.
GZ-11608 decreased methamphetamine sensitization without altering striatal dopamine content or exacerbating methamphetamine-induced dopamine depletion, revealing efficacy without neurotoxicity.
GZ-11608 exhibited linear pharmacokinetics and rapid brain penetration.
GZ-11608 decreased methamphetamine self-administration in drug-naive rats.
