(R)-Sila-venlafaxine: A selective noradrenaline reuptake inhibitor for the treatment of emesis

Sila-substitution of drugs (the carbon/silicon switch) is a concept that is being successfully used for the development of new chemical entities. The (R)-sila-analogue of the antidepressant venlafaxine is devoid of the serotonin reuptake inhibition observed with the marketed drug, leading to a selective noradrenaline reuptake inhibitor displaying anti-emetic properties.

Graphical abstractThe in vitro profile and in vivo anti-emetic activity of the selective noradrenaline reuptake inhibitor (R)-2 are reported.Figure optionsDownload full-size imageDownload as PowerPoint slide