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EnglishThe Aba-Gly scaffold, incorporated into Dmt-Tic ligands (H-Dmt-Tic-Gly-NH-CH2-Ph, H-Dmt-Tic-Gly-NH-Ph, H-Dmt-Tic-NH-CH2-Bid), exhibited mixed micro/delta or delta opioid receptor activities with micro agonism. Substitution of Tic by Aba-Gly coupled to -NH-CH2-Ph (1), -NH-Ph (2), or -Bid (Bid=1H-benzimidazole-2-yl) (3) shifted affinity (Ki(micro)=0.46, 1.48, and 19.9 nM, respectively), selectivity, and bioactivity to micro-opioid receptors. These compounds represent templates for a new class of lead opioid agonists that are easily synthesized and suitable for therapeutic pain relief.
New 2',6'-Dimethyl-L-Tyrosine (Dmt) Opioid Peptidomimetics Based on the Aba-Gly Scaffold. Development of Unique mu-Opioid Ligands / BALLET S; SALVADORI S; TRAPELLA C; BRYANT S. D; JINSMAA Y; LAZARUS L. H; NEGRI L; GIANNINI E; LATTANZI R; TOURWE' D; BALBONI G. - 49(2006), pp. 3990-3993.
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| Titolo: | New 2',6'-Dimethyl-L-Tyrosine (Dmt) Opioid Peptidomimetics Based on the Aba-Gly Scaffold. Development of Unique mu-Opioid Ligands |
| Autori: | |
| Data di pubblicazione: | 2006 |
| Rivista: | |
| Citazione: | New 2',6'-Dimethyl-L-Tyrosine (Dmt) Opioid Peptidomimetics Based on the Aba-Gly Scaffold. Development of Unique mu-Opioid Ligands / BALLET S; SALVADORI S; TRAPELLA C; BRYANT S. D; JINSMAA Y; LAZARUS L. H; NEGRI L; GIANNINI E; LATTANZI R; TOURWE' D; BALBONI G. - 49(2006), pp. 3990-3993. |
| Abstract: | The Aba-Gly scaffold, incorporated into Dmt-Tic ligands (H-Dmt-Tic-Gly-NH-CH2-Ph, H-Dmt-Tic-Gly-NH-Ph, H-Dmt-Tic-NH-CH2-Bid), exhibited mixed micro/delta or delta opioid receptor activities with micro agonism. Substitution of Tic by Aba-Gly coupled to -NH-CH2-Ph (1), -NH-Ph (2), or -Bid (Bid=1H-benzimidazole-2-yl) (3) shifted affinity (Ki(micro)=0.46, 1.48, and 19.9 nM, respectively), selectivity, and bioactivity to micro-opioid receptors. These compounds represent templates for a new class of lead opioid agonists that are easily synthesized and suitable for therapeutic pain relief. |
| Handle: | http://hdl.handle.net/11584/17744 |
| Tipologia: | 1.1 Articolo in rivista |
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