A new potential affinity label for the opiate receptor

M. Szücs, Katalin Di Gleria, Kálmán Medzihradszky

Research output: Contribution to journalArticle

9 Citations (Scopus)

Abstract

D-Ala2-Leu5-enkephalin (DALA) was elongated with the methyl ester of melphalan (Mel), a nitrogen mustard on the C-terminus. The new derivative, DALA-Mel-OMe might be a potential affinity label of the opiate receptor. The compound shows high affinity in displacement experiments with an IC50 of 10 nM and 100 nM against 3H-D-Ala2-Leu5-enkephalin and 3H-naloxone, respectively. 10-100 μM of DALA-Mel-OMe causes a significant inhibition of 3H-naloxone binding, which effect can't be reversed by extensive washes. This irreversible blockade is significantly but only partially protected by high concentrations of naloxone and Leu-enkephalin. Our results suggest that DALA-Mel-OMe binds irreversibly to the opiate receptor, but nonspecific labelling also occurs.

Original languageEnglish
Pages (from-to)435-438
Number of pages4
JournalLife Sciences
Volume33
Issue numberSUPPL. 1
DOIs
Publication statusPublished - 1983

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Affinity Labels
Enkephalins
Opioid Receptors
Melphalan
Naloxone
Leucine Enkephalin
Mechlorethamine
Labeling
Inhibitory Concentration 50
Esters
Derivatives
Experiments

ASJC Scopus subject areas

  • Pharmacology

Cite this

A new potential affinity label for the opiate receptor. / Szücs, M.; Gleria, Katalin Di; Medzihradszky, Kálmán.

In: Life Sciences, Vol. 33, No. SUPPL. 1, 1983, p. 435-438.

Research output: Contribution to journalArticle

Szücs, M, Gleria, KD & Medzihradszky, K 1983, 'A new potential affinity label for the opiate receptor', Life Sciences, vol. 33, no. SUPPL. 1, pp. 435-438. https://doi.org/10.1016/0024-3205(83)90535-0
Szücs, M. ; Gleria, Katalin Di ; Medzihradszky, Kálmán. / A new potential affinity label for the opiate receptor. In: Life Sciences. 1983 ; Vol. 33, No. SUPPL. 1. pp. 435-438.
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