Novel TIPP (H-Tyr-Tic-Phe-Phe-OH) analogues displaying a wide range of efficacies at the delta opioid receptor. Discovery of two highly potent and selective delta opioid agonists

[摘要]：Analogues of the delta opioid antagonist peptide TIPP (H-Tyr-Tic-Phe-Phe-OH; Tic = 1,2,3,4-tetrahydroisoquinoline3-carboxylic acid) containing various 4 '-[N-(alkyl or aralkyl) carboxamido] phenylalanine analogues in place of Tyr(1) were synthesized. The compounds showed subnanomolar or low nanomolar delta opioid receptor binding affinity and various efficacy at the d receptor (antagonism, partial agonism, full agonism) in the [S-35] GTP gamma S binding assay. Two analogues, [1-Ncp(1)]TIPP (1- Ncp = 4 '-[N-(2-(naphthalene-1-yl)ethyl)carboxamido]phenylalanine) and [2-Ncp(1)]TIPP (2-Ncp = 4 '-[ N-(2-(naphthalene-2-yl) ethyl)carboxamido] phenylalanine), were identified as potent and selective delta opioid agonists. (c) 2012 Elsevier Ltd. All rights reserved.

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