OPIOID RECEPTOR LABELING WITH THE CHLOROMETHYL KETONE DERIVATIVE OF [H-3] TYR-D-ALA-GLY-(ME)PHE-GLY-OL (DAMGO) .1. BINDING-PROPERTIES OF H-3 TYR-D-ALA-GLY-(ME)PHE CHLOROMETHYL KETONE

OKTEM, HÜSEYİN; VARGA, E; HEPP, J; MEDZIHRADZKY, K; LAJTHA, A; BORSODI, A

doi:10.1016/0024-3205(91)90213-u

OPIOID RECEPTOR LABELING WITH THE CHLOROMETHYL KETONE DERIVATIVE OF [H-3] TYR-D-ALA-GLY-(ME)PHE-GLY-OL (DAMGO) .1. BINDING-PROPERTIES OF H-3 TYR-D-ALA-GLY-(ME)PHE CHLOROMETHYL KETONE

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OKTEM H. A., VARGA E., HEPP J., MEDZIHRADZKY K., LAJTHA A., BORSODI A.

LIFE SCIENCES, vol.48, no.18, pp.1757-1762, 1991 (SCI-Expanded)

Publication Type: Article / Article
Volume: 48 Issue: 18
Publication Date: 1991
Doi Number: 10.1016/0024-3205(91)90213-u
Journal Name: LIFE SCIENCES
Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus
Page Numbers: pp.1757-1762
Middle East Technical University Affiliated: Yes

Abstract

We prepared a tritiated chloromethyl ketone derivative of Tyr-D-Ala-Gly(Me)Phe-Gly-ol H-3-D-Ala-Gly-(Me)Phe-chloromethyl ketone, and studied its binding characteristics in rat brain membranes. A significant portion (about 70%) of the binding becomes wash-resistant after 60 min of incubation. The binding of the ligand is highly stereospecific and mu-opioid receptor selective. These characteristics of the ligand, together with its high specific radioactivity (57 Ci/mmol) makes it a good candidate for biochemical characterization and covalent labeling of mu opioid receptors.