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 mu/delta or delta opioid receptor activities with A 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( mu)) 0.46, 1.48, and 19.9 nM, respectively), selectivity, and bioactivity to mu-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 / Ballet, S.; Salvadori, S.; Trapella, C.; Bryant, S. D.; Jinsmaa, Y.; Lazarus, L. H.; Negri, Lucia; Giannini, Elisa; Lattanzi, Roberta; Tourwe, D.; Balboni, G.. - In: JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0022-2623. - STAMPA. - 49:(2006), pp. 3990-3993. [10.1021/jm0603264]
New 2 ',6 '-dimethyl-L-tyrosine (Dmt) opioid peptidomimetics based on the Aba-Gly scaffold. Development of unique mu-opioid receptor ligands
NEGRI, Lucia;GIANNINI, Elisa;LATTANZI, Roberta;
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 mu/delta or delta opioid receptor activities with A 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( mu)) 0.46, 1.48, and 19.9 nM, respectively), selectivity, and bioactivity to mu-opioid receptors. These compounds represent templates for a new class of lead opioid agonists that are easily synthesized and suitable for therapeutic pain relief.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
