Characterization of N,N(Me)2-Dmt-Tic-OH, a delta selective opioid dipeptide antagonist

Krisztina Monory, Sharon D. Bryant, István Kertész, Gianfranco Balboni, Remo Guerrini, Géza Tóth, Severo Salvadori, Lawrence H. Lazarus, A. Borsodi

Research output: Contribution to journalArticle

3 Citations (Scopus)

Abstract

N,N(Me)2-Dimethyl-tyrosine-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid-OH (N,N(Me)2-Dmt-Tic-OH) is a very selective δ opioid dipeptide with elevated antagonist activity. We have radiolabelled this compound by catalytic tritiation of the N,N(Me)2-Dmt(3',5'-12)-Tic-OH precursor. The ligand labelled rat brain membranes with a K(d) value of 0.42 nM and a B(max) of 63.12 fmol/mg protein. The new tritiated ligand showed high affinity for the δ opioid receptor whereas its binding at μ and κ opioid receptors was weak. N,N(Me)2-Dmt-Tic-OH was able to inhibit the agonist-stimulated binding of the non-hydrolysable GTP analogue [35S]GTPγS, thus attenuating the activation of G proteins via opioid receptors. This simple opioid dipeptide in both normal and labelled form may serve as a useful tool to study δ opioid receptors in vitro and in vivo. (C) 2000 Lippincott Williams and Wilkins.

Original languageEnglish
Pages (from-to)2083-2086
Number of pages4
JournalNeuroReport
Volume11
Issue number10
Publication statusPublished - Jul 14 2000

Fingerprint

Narcotic Antagonists
Dipeptides
Opioid Receptors
Opioid Analgesics
Ligands
Tics
Guanosine Triphosphate
GTP-Binding Proteins
Membranes
N,N(Me)2-dimethyl-tyrosine-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid-OH
Brain
Proteins

Keywords

  • [S]GTPγS binding
  • Antagonist
  • Delta opioid receptor
  • Peptide
  • Radioligand binding

ASJC Scopus subject areas

  • Neuroscience(all)

Cite this

Monory, K., Bryant, S. D., Kertész, I., Balboni, G., Guerrini, R., Tóth, G., ... Borsodi, A. (2000). Characterization of N,N(Me)2-Dmt-Tic-OH, a delta selective opioid dipeptide antagonist. NeuroReport, 11(10), 2083-2086.

Characterization of N,N(Me)2-Dmt-Tic-OH, a delta selective opioid dipeptide antagonist. / Monory, Krisztina; Bryant, Sharon D.; Kertész, István; Balboni, Gianfranco; Guerrini, Remo; Tóth, Géza; Salvadori, Severo; Lazarus, Lawrence H.; Borsodi, A.

In: NeuroReport, Vol. 11, No. 10, 14.07.2000, p. 2083-2086.

Research output: Contribution to journalArticle

Monory, K, Bryant, SD, Kertész, I, Balboni, G, Guerrini, R, Tóth, G, Salvadori, S, Lazarus, LH & Borsodi, A 2000, 'Characterization of N,N(Me)2-Dmt-Tic-OH, a delta selective opioid dipeptide antagonist', NeuroReport, vol. 11, no. 10, pp. 2083-2086.
Monory K, Bryant SD, Kertész I, Balboni G, Guerrini R, Tóth G et al. Characterization of N,N(Me)2-Dmt-Tic-OH, a delta selective opioid dipeptide antagonist. NeuroReport. 2000 Jul 14;11(10):2083-2086.
Monory, Krisztina ; Bryant, Sharon D. ; Kertész, István ; Balboni, Gianfranco ; Guerrini, Remo ; Tóth, Géza ; Salvadori, Severo ; Lazarus, Lawrence H. ; Borsodi, A. / Characterization of N,N(Me)2-Dmt-Tic-OH, a delta selective opioid dipeptide antagonist. In: NeuroReport. 2000 ; Vol. 11, No. 10. pp. 2083-2086.
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