Title

Vascular effects of diphenylmethoxypiperidine-derived dopamine uptake inhibitors

Document Type

Article

Date of Publication

6-1-2014

Publication Title

Bioorganic & Medicinal Chemistry Letters

First Page

2429

Last Page

2432

Abstract

Abstract

Vascular effects of 4-aryl methoxypiperidinol compounds previously shown to share with cocaine the ability to inhibit the dopamine transporter are described. All the compounds tested inhibit KCl-induced and noradrenaline-dependent contractions in mesenteric arteries ex vivo. Thus, diphenylpyraline and its analogs may have a role as therapeutic options for the treatment of some of the cardiotoxic effects of cocaine intoxications.

Graphical abstract

Studies of the in vitro vascular properties of 4-(arylmethoxy)-1-alkylpiperidine inhibitors of the dopamine transporter are reported. The lipophilicity given by the size of the N-aryl substituent potentiated the inhibitory effect with 4a being the most effective blocker of KCl and noradrenaline-induced contractions.

DOI

https://doi.org/10.1016/j.bmcl.2014.04.040

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