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Chemical Structure : GZ-11608
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.
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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.
| M.Wt | 283.415 | |
| Formula | C19H25NO | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Lee NR, et al. J Pharmacol Exp Ther. 2019 Nov;371(2):526-543.
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