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 í/ä or ä opioid receptor activities with í 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(í) ) 0.46, 1.48, and 19.9 nM, respectively), selectivity, and bioactivity to í-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 receptor ligands
SALVADORI, Severo;TRAPELLA, Claudio;
2006
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 í/ä or ä opioid receptor activities with í 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(í) ) 0.46, 1.48, and 19.9 nM, respectively), selectivity, and bioactivity to í-opioid receptors. These compounds represent templates for a new class of lead opioid agonists that are easily synthesized and suitable for therapeutic pain relief.File in questo prodotto:
Non ci sono file associati a questo prodotto.
I documenti in SFERA sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
