Loriga, Giovanni and Manca, Ilaria and Murineddu, Gabriele and Chelucci, Giorgio Adolfo and Villa, Stefania and Gessi, Stefania and Toma, Lucio and Cignarella, Giorgio and Pinna, Gérard Aimé (2006) Synthesis of 3,6-diazabicyclo[3.1.1]heptanes as novel ligands for the opioid receptors. Bioorganic & Medicinal Chemistry, Vol. 14 (3), p. 676-691. ISSN 0968-0896. Article.
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In an effort to improve diazabicycloalkane-based opioid receptor ligands, N-3(6)-arylpropenyl-N-6(3)-propionyl-3,6-diazabicyclo[3.1.1]heptanes (3A,Ba–i) were synthesized and their affinity and selectivity towards μ-, δ- and κ-receptors were evaluated. The results of the current study revealed a number of compounds (3Bb, 3Bg and 3Bh) having a high affinity for μ (Ki at μ-receptors ranging from 2.7 to 7.9 nM) versus δ (Ki at δ-receptors >2000 nM) and versus κ (Ki at κ-receptors >5000 nM) receptors. Molecular modelling carried out on the pair 3Aa/3Ba and on the 3Bh was consistent with the hypothesis that the two series of compounds 3A and 3B interact with the μ-receptor in very different ways.
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