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Titolo: Synthesis and biological evaluation of novel delta (δ)opioid receptor ligands with diazatricyclodecane skeletons
Autori: 
Data di pubblicazione: 2013
Rivista: 
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY  
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.
Handle: http://hdl.handle.net/11584/87382
Tipologia:1.1 Articolo in rivista

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