| Autor: |
Zioudrou, C, Varoucha, D, Loukas, S, Nicolaou, N, Streaty, R A, Klee, W A |
| Zdroj: |
Journal of Biological Chemistry; September 1983, Vol. 258 Issue: 18 p10934-10937, 4p |
| Abstrakt: |
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 NG108-15 neuroblastoma x 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. |
| Databáze: |
Supplemental Index |
| Externí odkaz: |
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