A potent peptide affinity reagent for the opiate receptor.
The synthesis and characterization of a novel enkephalin analogue, Tyr-D-Ala-Gly-Phe-Leu-chloromethyl ketone, is described. The biological potency of the compound in various assays has been determined to be very high. The compound is an alkylating affinity reagent and irreversibly inactivates a defined population of enkephalin receptors in rat brain membrane preparations, as well as irreversibly inhibiting electrically stimulated contractions in the mouse vas deferens tissue preparation.
D000345:Affinity Labels; D000590:Amino Acid Chloromethyl Ketones / Q000138:chemical synthesis / Q000494:pharmacology*; D000818:Animals; D001667:Binding, Competitive; D001681:Biological Assay; D001921:Brain / Q000378:metabolism*; D002462:Cell Membrane / Q000378:metabolism; D004723:Endorphins / Q000494:pharmacology*; D004745:Enkephalins / Q000138:chemical synthesis / Q000494:pharmacology*; D007700:Kinetics; D008297:Male; D008722:Methods; D051379:Mice; D051381:Rats; D011957:Receptors, Opioid / Q000187:drug effects / Q000378:metabolism*
D000345:Affinity Labels; D000590:Amino Acid Chloromethyl Ketones; D004723:Endorphins; D004745:Enkephalins; D011957:Receptors, Opioid; C028557:tyrosyl-alanyl-glycyl-phenylalanyl-leucine chloromethyl ketone