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

H. A. Oktem, E. Varga, J. Hepp, K. Medzihradzky, A. Lajtha, A. Borsodi

Research output: Contribution to journalArticle

5 Citations (Scopus)

Abstract

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.

Original languageEnglish
Pages (from-to)1757-1762
Number of pages6
JournalLife Sciences
Volume48
Issue number18
DOIs
Publication statusPublished - 1991

Fingerprint

mu Opioid Receptor
Opioid Receptors
Ketones
Labeling
alanylglycine
Ligands
Derivatives
Radioactivity
Rats
Brain
Membranes
tyrosyl-alanyl-glycyl-phenylalanine

ASJC Scopus subject areas

  • Pharmacology

Cite this

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. / Oktem, H. A.; Varga, E.; Hepp, J.; Medzihradzky, K.; Lajtha, A.; Borsodi, A.

In: Life Sciences, Vol. 48, No. 18, 1991, p. 1757-1762.

Research output: Contribution to journalArticle

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AU - Borsodi, A.

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