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.
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.
Oktem
H A
HA
Institute of Biochemistry, Biological Research Center, Hungarian Academy of Sciences, Szeged.
Varga
E
E
Hepp
J
J
Medzihradzky
K
K
Lajtha
A
A
Borsodi
A
A
D000590:Amino Acid Chloromethyl Ketones / Q000378:metabolism*; D000818:Animals; D001921:Brain / Q000378:metabolism*; D002462:Cell Membrane / Q000378:metabolism; D007700:Kinetics; D009294:Narcotics / Q000494:pharmacology; D051381:Rats; D011919:Rats, Inbred Strains; D011957:Receptors, Opioid / Q000187:drug effects / Q000378:metabolism*; D017450:Receptors, Opioid, mu; D014316:Tritium
D000590:Amino Acid Chloromethyl Ketones; D009294:Narcotics; D011957:Receptors, Opioid; D017450:Receptors, Opioid, mu; D014316:Tritium; C052900:tyrosyl-alanyl-glycyl-N(alpha)-methylphenylalanine chloromethyl ketone