Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
USA
Email: lddd@benthamscience.org

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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

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

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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.

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Article Details

VOLUME: 12
ISSUE: 4
Year: 2015
Page: [259 - 262]
Pages: 4
DOI: 10.2174/1570180811666141024005226
Price: $58