Adelaide Research & Scholarship
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https://hdl.handle.net/2440/47169
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| Type: | Journal article |
| Title: | New 2',6'-Dimethyl-L-tyrosine (Dmt) opioid peptidomimetics based on the Aba-Gly scaffold. Development of unique μ-opioid receptor ligands |
| Other Titles: | New 2',6'-Dimethyl-L-tyrosine (Dmt) opioid peptidomimetics based on the Aba-Gly scaffold. Development of unique mu-opioid receptor ligands |
| Author: | Ballet, Steven Salvadori, Severo Trapella, Claudio Bryant, Sharon D. Jinsmaa, Yunden Lazarus, Lawrence H. Negri, Lucia Giannini, Elisa Lattanzi, Roberta Tourwe, Dirk Balboni, Gianfranco |
| Citation: | Journal of Medicinal Chemistry, 2006; 49(13):3990 -3993 |
| Publisher: | American Chemical Society |
| Issue Date: | 2006 |
| School/Discipline: | School of Chemistry and Physics : Chemistry |
| 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 μ/δ or δ opioid receptor activities with μ 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(μ) = 0.46, 1.48, and 19.9 nM, respectively), selectivity, and bioactivity to μ-opioid receptors. These compounds represent templates for a new class of lead opioid agonists that are easily synthesized and suitable for therapeutic pain relief. |
| Description: | © 2006 American Chemical Society |
| DOI: | 10.1021/jm0603264 |
| Appears in Collections: | Chemistry and Physics publications |
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