Introduction The introduction of 2' ,6'-dimethyl-L'tyrosine (Dmt) at the N-terminus of Tyr-Tic (1,2,3,4-tetra-hydroisoquinoline-3-carboxylic acid )-containing δ-opioid antagonists enhances receptor affinity ...Introduction The introduction of 2' ,6'-dimethyl-L'tyrosine (Dmt) at the N-terminus of Tyr-Tic (1,2,3,4-tetra-hydroisoquinoline-3-carboxylic acid )-containing δ-opioid antagonists enhances receptor affinity and in vitro bioactivity to several orders of magnitude and its application in the formation of ligands with new properties, such as potent inverse agonism. For example, the δ2 agonist,展开更多
文摘Introduction The introduction of 2' ,6'-dimethyl-L'tyrosine (Dmt) at the N-terminus of Tyr-Tic (1,2,3,4-tetra-hydroisoquinoline-3-carboxylic acid )-containing δ-opioid antagonists enhances receptor affinity and in vitro bioactivity to several orders of magnitude and its application in the formation of ligands with new properties, such as potent inverse agonism. For example, the δ2 agonist,