Novel Cyclic Biphalin Analogue with Improved Antinociceptive Properties
ACS Medicinal Chemistry Letters2014Vol. 5(9), pp. 1032–1036
Citations Over TimeTop 22% of 2014 papers
Adriano Mollica, Alfonso Carotenuto, Ettore Novellino, Antonio Limatola, Roberto Costante, Francesco Pinnen, Azzurra Stefanucci, Stefano Pieretti, Anna Borsodi, Reza Samavati, Ferenc Zádor, Sándor Benyhe, Peg Davis, Frank Porreca, Victor J. Hruby
Abstract
Two novel opioid analogues have been designed by substituting the native d-Ala residues in position 2,2' of biphalin with two residues of d-penicillamine or l-penicillamine and by forming a disulfide bond between the thiol groups. The so-obtained compound 9 containing d-penicillamines showed excellent μ/δ mixed receptor affinities (K i (δ) = 5.2 nM; K i (μ) = 1.9 nM), together with an efficacious capacity to trigger the second messenger and a very good in vivo antinociceptive activity, whereas product 10 was scarcely active. An explanation of the two different pharmacological behaviors of products 9 and 10 was found by studying their conformational properties.
Related Papers
- A GEOMETRIC MEAN IN THE FURUTA INEQUALITY(2002)
- Susquehanna Chorale Spring Concert "Roots and Wings"(2017)
- Коммуникaтивно- прaгмaтический aнaлиз дипломaтических бумaг (нa основе вербaльных нот)(2018)
- → ФОРМИРОВAНИЕ ГОТОВНОСТИ БУДУЩИХ ПЕДAГОГОВ К ОРГAНИЗAЦИИ РAБОТЫ ПО РAЗВИТИЮ ВAЛЕОЛОГИЧЕСКОЙ КУЛЬТУРЫ ШКОЛЬНИКОВ(2023)