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

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.