The use of [3H]‐[d‐Pen2,d‐Pen5]enkephalin as a highly selective ligand for the δ‐binding site
Open Access
- 1 April 1985
- journal article
- research article
- Published by Wiley in British Journal of Pharmacology
- Vol. 84 (4) , 927-932
- https://doi.org/10.1111/j.1476-5381.1985.tb17387.x
Abstract
The characteristics of the binding of [3H]‐[d‐Pen2,d‐Pen5]enkephalin were determined in homogenates of guinea‐pig and rat brain. In the guinea‐pig, the maximum binding capacity for [3H]‐[d‐Pen2,d‐Pen5]enkephalin was 4.19 pmol g−1 and the KD 1.61 nm. In the rat, the corresponding values were 2.47 pmol g−1 and 5.42 nm. In both species, the maximum binding capacity and the affinity were not altered when μ‐binding was suppressed with [d‐Ala2, MePhe4, Gly‐ol5]enkephalin. The μ‐agonists, [d‐Ala2, MePhe4, Gly‐ol5]enkephalin and morphine, displaced a small portion of the binding of [3H]‐[d‐Pen2,d‐Pen5]enkephalin with high affinities.This publication has 7 references indexed in Scilit:
- Selectivities of opioid peptide analogues as agonists and antagonists at the δ‐receptorBritish Journal of Pharmacology, 1984
- Bis-penicillamine enkephalins possess highly improved specificity toward delta opioid receptors.Proceedings of the National Academy of Sciences, 1983
- SPECTRUM OF THE μ‐, δ‐ AND κ‐BINDING SITES IN HOMOGENATES OF RAT BRAINBritish Journal of Pharmacology, 1982
- The binding spectrum of narcotic analgesic drugs with different agonist and antagonist propertiesNaunyn-Schmiedebergs Archiv für experimentelle Pathologie und Pharmakologie, 1982
- COMPARISON OF THE BINDING CHARACTERISTICS OF TRITIATED OPIATES AND OPIOID PEPTIDESBritish Journal of Pharmacology, 1980
- Relationship between the inhibition constant (KI) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reactionBiochemical Pharmacology, 1973