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Letters in Drug Design & Discovery

Editor-in-Chief

ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

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

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

Volume 12, Issue 4, 2015

Page: [259 - 262] Pages: 4

DOI: 10.2174/1570180811666141024005226

Price: $65

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


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