δ and μ opiate receptor probes: fluorescent enkephalins with high receptor affinity and specificity
- 12 November 1985
- journal article
- Published by Wiley in FEBS Letters
- Vol. 193 (1) , 35-38
- https://doi.org/10.1016/0014-5793(85)80074-0
Abstract
The fluorescent amino acid, L‐1‐pyrenylalanine (Pya) was incorporated into [D‐Ala2,Leu5]enkephalin and its methyl ester at position 4 or 5. Pya‐enkephalins showed strong fluorescent intensity and displayed high binding affinity for opiate receptors. Pya4‐enkephalins showed high specificity for the μ receptors, while Pya5‐enkephalins showed high specificity and selectivity for the δ receptors. Particularly, [D‐Ala2,Pya5]enkephalin was as potent as the most utilized δ‐specific ligand of [D‐Ala2,D‐Leu5]enkephalin (DADLE), and yet its δ‐selectivity was about 5‐times greater than that of DADLE. Thus, Pya‐enkephalins per se can be utilized as a fluorescent probe or tracer for the opiate receptor‐binding assays.Keywords
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