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