Peptidic and non-peptidic neurotensin analogs

Feng Hong, Bernadette Cusack, Abdul Fauq, Elliott Richelson

Research output: Contribution to journalReview articlepeer-review

14 Scopus citations

Abstract

The structure-activity relationship studies of neurotensin and its analogs have revealed that i) the C-terminal hexapeptide NT (8-13) (H-Arg8-Arg9-Pro10-Tyr11- Ile12-Leu13-OH) is equipotent to or more potent than the native NT(1-13) and retains all the intrinsic biological properties of neurotensin, ii) the N-terminal peptide fragment up to NT(1-7) does not significantly contribute to the binding potency, iii) Pro10 that can form a reverse-turn conformation is required, iv) an aromatic amino acid is important at Tyr11 position, v) the lipophilic side chain of Leu13 is also crucial to the biological activities, and, vi) L-form amino acids are essential at critical positions for the binding potency. In addition to many peptidic neurotensin analogs, highly potent, orally active, and selective non-peptidic analogs as antagonists of NT receptors, which have long lasting effects and the ability to cross the bloodbrain barrier (e. g. SR 142948 A and SR 48692), have been discovered.

Original languageEnglish (US)
Pages (from-to)421-434
Number of pages14
JournalCurrent Medicinal Chemistry
Volume4
Issue number6
StatePublished - 1997

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Pharmacology
  • Drug Discovery
  • Organic Chemistry

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