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Photolabile opioid derivatives of 2 d alanine 5 leucine enkephalin and their interactions with the opiate receptor


Journal of Biological Chemistry 258(18): 10934-10937
Photolabile opioid derivatives of 2 d alanine 5 leucine enkephalin and their interactions with the opiate receptor
Photolabile derivatives of D-Ala2-Leu5-enkephalin were prepared by synthetic procedures in which a 2-nitro-4-azidophenyl group is linked to the terminal carboxyl group of the enkephalin by means of an ethylenediamine or ethylenediamine .beta.-alanine spacer. These peptides bind to opiate receptors with nanomolar affinities and inhibit electrically stimulated contractions of the mouse vas deferens and adenylate cyclase activity of [mouse] NG108-15 neuroblastoma .times. glioma hybrid cell membranes. Both inhibitions are reversed by the opiate antagonist naloxone. Photolysis of the ligands bound to rat brain membranes results in the loss of approximately 50% of the receptor sites. This decrease in receptor number is blocked by naloxone and requires light. A photolabile [3H]enkephalin derivative labels an equivalent number of sites under similar irradiation conditions.

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Accession: 006110922



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Photolabile opioid derivatives of D-Ala2-Leu5-enkephalin and their interactions with the opiate receptor. Journal of Biological Chemistry 258(18): 10934-7, 1983

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