AI Article Synopsis
- Researchers synthesized new analogues of the δ opioid antagonist peptide TIPP by replacing a key amino acid with various 4'-[N-(alkyl or aralkyl)carboxamido]phenylalanine analogues.
- These compounds exhibited strong binding affinity to δ opioid receptors, with some displaying a range of effects from antagonism to full agonism in specific assays.
- Two of the new analogues, [1-Ncp(1)]TIPP and [2-Ncp(1)]TIPP, were found to be particularly potent and selective δ opioid agonists.
Article Abstract
Analogues of the δ 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 δ opioid receptor binding affinity and various efficacy at the δ receptor (antagonism, partial agonism, full agonism) in the [(35)S]GTPγS 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 δ opioid agonists.
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|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3288262 | PMC |
| http://dx.doi.org/10.1016/j.bmcl.2012.01.063 | DOI Listing |
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