N-Benzyl-N-(tetrahydro-2H-pyran-4-yl)pyrrolidin-3-amines as selective dual serotonin/noradrenaline reuptake inhibitors.

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Fish PV, Fray MJ, Stobie A, Wakenhut F, Whitlock GA

N-Benzyl-N-(tetrahydro-2H-pyran-4-yl)pyrrolidin-3-amines as selective dual serotonin/noradrenaline reuptake inhibitors.

Bioorg Med Chem Lett. 2007 Apr 1;17(7):2022-5. Epub 2007 Jan 19.

PubMed ID

17267217 [ View in PubMed

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Abstract

A series of N-benzyl-N-(tetrahydro-2H-pyran-4-yl)pyrrolidin-3-amine monoamine reuptake inhibitors are described. Selective dual 5-HT and NA reuptake inhibition was achieved, and analogues with weak CYP2D6 inhibition, good human in vitro metabolic stability and wide ligand selectivity, such as 12b, were identified.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Duloxetine	Sodium-dependent dopamine transporter	IC 50 (nM)	870	N/A	N/A	Details
Duloxetine	Sodium-dependent noradrenaline transporter	IC 50 (nM)	19	N/A	N/A	Details
Duloxetine	Sodium-dependent serotonin transporter	IC 50 (nM)	6	N/A	N/A	Details