Kappa-opioid receptors are differentially labeled by arylacetamides and benzomorphans.
Kappa-opioid receptors are differentially labeled by arylacetamides and benzomorphans.
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Kappa-阿片受体由芳基乙酰胺和苯并吗啡进行差异标记。
DOI：
10.1016/j.ejphar.2003.11.078
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发表时间：
2004
影响因子：
5
通讯作者：
Bidlack,JeanM
中科院分区：
文献类型：
--
作者：
Rusovici,DanielaE;Negus,SStevens;Mello,NancyK;Bidlack,JeanM
Using Chinese Hamster Ovary cell membranes that stably expressed the human κ-opioid receptor, we investigated the hypothesis that κ1- and κ2-opioid receptors, historically defined by their phrmacological selectivity for either arylacetamides or benzomorphans are, in fact, different affinity states or binding sites on the same κ-opioid receptors. Receptor binding studies showed that GTPγS potently inhibited [3H](5α,7α,8β)-(+)-N-methyl-N-(7-[1-pyrrolidinyl]-1-oxaspiro [4.5]dec-8-yl)-benzeneacetamide (U69,593) binding, compared to virtually no inhibition of [3H]bremazocine binding. Saturation binding experiments showed a three-fold decrease in [3H]U69,593 affinity in the presence of GTPγS, but GTPγS had no effect on [3H]bremazocine affinity. The κ-opioid receptor antagonist nor-binaltorphimine had a four-fold higher affinity for [3H]U69,593-labeled receptors than for [3H]bremazocine-labeled receptors. Functional selectivity studies, measuring the stimulation of [35S]GTPγS agonist-induced binding, showed a significantly higher U69,593-induced G protein-receptor activation in comparison to the stimulation observed with bremazocine. These results suggest that pharmacologically defined 1κ-opioid receptor subtypes may be different affinity states of the same receptor.
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期刊：
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