Vascular effects of diphenylmethoxypiperidine-derived dopamine uptake inhibitors
Date of Publication
Bioorganic & Medicinal Chemistry Letters
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.
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.
Pulgar, V. M. and Harp, J. K., "Vascular effects of diphenylmethoxypiperidine-derived dopamine uptake inhibitors" (2014). Pharmaceutical Sciences. 2181.