Opioid receptor labeling with the chloromethyl ketone derivative of (3)H-Tyr-D-Ala-Gly-(ME)Phe-Gly-Ol (Damgo) I: Binding properties of 3H-Tyr-D-Ala-Gly-(Me)Phe chloromethyl ketone

Date

1991-01-01

Author

Öktem, Hüseyin Avni
VARGA, E
HEPP, J
MEDZIHRADZKY, K
LAJTHA, A
BORSODI, A

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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.

URI

https://hdl.handle.net/11511/107876

Journal

LIFE SCIENCES

DOI

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

Collections

Department of Biology, Article

Citation Formats

H. A. Öktem, E. VARGA, J. HEPP, K. MEDZIHRADZKY, A. LAJTHA, and A. BORSODI, “Opioid receptor labeling with the chloromethyl ketone derivative of (3)H-Tyr-D-Ala-Gly-(ME)Phe-Gly-Ol (Damgo) I: Binding properties of 3H-Tyr-D-Ala-Gly-(Me)Phe chloromethyl ketone,” LIFE SCIENCES, vol. 48, no. 18, pp. 1757–1762, 1991, Accessed: 00, 2024. [Online]. Available: https://hdl.handle.net/11511/107876.