Letters in Drug Design & Discovery

Author(s): Marilena Vlachou, Vasiliki Ioannidou, Maria Vertzoni, Andrew Tsotinis, Pandelis A. Afroudakis and David Sugden

DOI: 10.2174/1570180811666141024005226

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Controlled Release from Solid Pharmaceutical Formulations of two Nalkanoyl- 4-methoxybicyclo[4.2.0]octa-1,3,5-trien-7-ethanamines with Melatoninergic Activity

Page: [259 - 262] Pages: 4

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Abstract

The design, pharmacological properties and delivery characteristics in gastric and intestinal fluids of N-alkanoyl-4-methoxybicyclo[4.2.0]octa-1,3,5-trien-7-ethanamines, (I) and (II), are described. The biological activity of compounds (I) and (II) was determined in a specific model of melatonin action, the pigment aggregation response of Xenopus laevis melanophores. Both analogues were found to be powerful melatonin receptor agonists and showed satisfactory release characteristics, comparable to melatonin, from solid pharmaceutical formulations.

Keywords: Design, drug delivery, melatoninergic potency, N-alkanoyl-4-methoxybicyclo[4.2.0]octa-1, 3, 5-trien-7-ethanamines.

Graphical Abstract