Abstract
Derivatives of the δ opioid receptor selective peptide Tyr-Tic-Phe-Phe-OH (TIPP) containing a p-bromoacetamide moiety on the phenyl ring of Phe3 or Phe4 were prepared by solid phase synthesis. [Phe(p-NHCOCH2Br)4]TIPP exhibited high affinity for cloned δ receptors (IC50 = 5.4 nM), and incubation with only 2.5 nM resulted in 85% wash resistant inhibition of radioligand binding to δ receptors. Therefore, this peptide is a potent affinity label for further study of δ opioid receptors.
Original language | English (US) |
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Pages (from-to) | 3820-3823 |
Number of pages | 4 |
Journal | Journal of Medicinal Chemistry |
Volume | 45 |
Issue number | 18 |
DOIs | |
State | Published - Aug 29 2002 |
Externally published | Yes |
All Science Journal Classification (ASJC) codes
- Molecular Medicine
- Drug Discovery