| Literature DB >> 24090913 |
Giovanni Loriga1, Paolo Lazzari, Stefania Ruiu, Giorgio Marchese, Ilaria Manca, Gian Luca Casu, Christian Dessì, Gérard Aimè Pinna, Battistina Asproni, Gabriele Murineddu.
Abstract
Considering the interesting pharmacological profile of the delta (δ) selective opioid agonist compound SNC-80, conformationally constrained analogs containing two diazatricyclodecane ring systems in place of dimethylpiperazine core motif were synthesized. The compounds showed subnanomolar or low nanomolar δ opioid receptor binding affinity. Depending upon the substituents on the diazatricyclodecane ring, these compounds displayed varying selectivity for δ opioid receptor over μ and κ receptors. Amongst the novel compounds, 1Aa showed the more interesting biological profile, with higher δ affinity and selectivity compared to SNC-80. The δ receptor agonist profile and antinociceptive activity of 1Aa were confirmed using ex-vivo (isolated mouse vas deferens) and in vivo (tail flick) assays.Entities:
Keywords: 2,7-Diazatricyclo[4.4.0.0(3,8)]decane; 9,10-Diazatricyclo[4.2.1.1(2,5)]decane; Antinociceptive activity; Binding assays; δ-Agonist SNC-80; δ-Opioid receptor ligands
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Year: 2013 PMID： 24090913 DOI： 10.1016/j.ejmech.2013.09.014
Source DB: PubMed Journal: Eur J Med Chem ISSN： 0223-5234 Impact factor: 6.514