Synthesis and in vitro evaluation of water-soluble 1,4-diphenethylpiperazine analogs as novel inhibitors of the vesicular monoamine transporter-2

A small library of 1,4-diphenethylpiperazine analogs was synthesized and evaluated for inhibition of [(3)H]dihydrotetrabenazine binding and [(3)H]dopamine uptake at the vesicular monoamine transporter-2 (VMAT2). Results from these studies identified three novel molecules, 6b, 6e and 9a (K(i) = 35 nM...

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Vydáno v:Bioorg Med Chem Lett
Hlavní autoři: Nickell, Justin R., Culver, John P., Janganati, Venumadhav, Zheng, Guangrong, Dwoskin, Linda P., Crooks, Peter A.
Médium: Artigo
Jazyk:Inglês
Vydáno: 2016
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On-line přístup:https://ncbi.nlm.nih.gov/pmc/articles/PMC5002989/
https://ncbi.nlm.nih.gov/pubmed/27524311
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.bmcl.2016.08.001
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