Oktem H A, Varga E, Hepp J, Medzihradzky K, Lajtha A, Borsodi A
Institute of Biochemistry, Biological Research Center, Hungarian Academy of Sciences, Szeged.
Life Sci. 1991;48(18):1757-62. doi: 10.1016/0024-3205(91)90213-u.
We prepared a tritiated chloromethyl ketone derivative of Tyr-D-Ala-Gly(Me)Phe-Gly-ol 3H-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.
