Novel, achiral aminoheterocycles as selective monoamine reuptake inhibitors.

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Lucas MC, Carter DS, Cai HY, Lee EK, Schoenfeld RC, Steiner S, Villa M, Weikert RJ, Iyer PS

Novel, achiral aminoheterocycles as selective monoamine reuptake inhibitors.

Bioorg Med Chem Lett. 2009 Aug 15;19(16):4630-3. doi: 10.1016/j.bmcl.2009.06.076. Epub 2009 Jun 25.

PubMed ID

19592243 [ View in PubMed

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Abstract

A variety of novel aminoheterocycle scaffolds as selective monoamine reuptake inhibitors have been prepared and one of these scaffolds is achiral. The main elements responsible for hERG channel, CYP2D6 and CYP3A4 inhibition were identified.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Duloxetine	Sodium-dependent dopamine transporter	Ki (nM)	251.19	N/A	N/A	Details
Duloxetine	Sodium-dependent noradrenaline transporter	Ki (nM)	7.94	N/A	N/A	Details
Duloxetine	Sodium-dependent serotonin transporter	Ki (nM)	0.501	N/A	N/A	Details