Belcheva M, Csanady G, Szucs M, Varga E, Wollemann M, Medzihradszky K
Institute of Biochemistry, Biological Research Center, Hungarian Academy of Sciences, Szeged.
Neuropeptides. 1988 Oct;12(3):149-54. doi: 10.1016/0143-4179(88)90046-7.
The diazomethyl ketone derivative of D-Ala2-Leu-enkephalin and Leu-enkephalin were synthesized. Replacement of the C-terminal carboxyl group with CO-CHN2 resulted in a potency decrease, the new compounds display micromolar affinities to 3H-naloxone and 3H-DALE binding sites. Photolysis of the ligands bound to rat brain membranes resulted in an approximately 30% irreversible loss of the receptors. Photoinactivation was prevented by the opiate antagonist, naloxone, thus providing that the ligands are specific photoaffinity probes of the opioid receptors.
