Article
Radioligand-dependent discrepancy in agonist affinities enhanced by mutations in the kappa-opioid receptor.
Molecular pharmacology - 1 Oct 1996
Hjorth S A, Thirstrup K, Schwartz T W
Abstract excerpt
A series of kappa/mu receptor chimeras and a number of kappa receptors substituted in the second transmembrane segment (TM-II) were investigated using as radioligands, respectively, the kappa-selective agonist [3H]C1977 and the nonselective opioid antagonist [3H]diprenorphine (DIP). All of the receptor constructs bound [3H]DIP with similar and high affinity, whereas the apparent affinity of the nonpeptide agonist...
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