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Activation profiles of opioid ligands in HEK cells expressing δ opioid receptors

Overview of attention for article published in BMC Neuroscience, November 2002
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Title
Activation profiles of opioid ligands in HEK cells expressing δ opioid receptors
Published in
BMC Neuroscience, November 2002
DOI 10.1186/1471-2202-3-19
Pubmed ID
Authors

Parham Gharagozlou, Hasan Demirci, J David Clark, Jelveh Lameh

Abstract

The aim of the present study was to characterize the activation profiles of 15 opioid ligands in transfected human embryonic kidney cells expressing only delta opioid receptors. Activation profiles of most of these ligands at delta opioid receptors had not been previously characterized in vitro. Receptor activation was assessed by measuring the inhibition of forskolin-stimulated cAMP production. Naltrexone and nalorphine were classified as antagonists at delta opioid receptor. The other ligands studied were agonists at delta opioid receptors and demonstrated IC50 values of 0.1 nM to 2 microM, maximal inhibition of 39-77% and receptor binding affinities of 0.5 to 243 nM. The rank order of efficacy of the ligands tested was metazocine = xorphanol > or = fentanyl = SKF 10047 = etorphine = hydromorphone = butorphanol = lofentanil > WIN 44,441 = Nalbuphine = cyclazocine > or = met-enkephalin > morphine = dezocine. For the first time these data describe and compare the function and relative efficacy of several ligands at delta opioid receptors. The data produced from this study can lead to elucidation of the complete activation profiles of several opioid ligands, leading to clarification of the mechanisms involved in physiological effects of these ligands at delta opioid receptors. Furthermore, these data can be used as a basis for novel use of existing opioid ligands based on their pharmacology at delta opioid receptors.

Mendeley readers

Mendeley readers

The data shown below were compiled from readership statistics for 32 Mendeley readers of this research output. Click here to see the associated Mendeley record.

Geographical breakdown

Country Count As %
United Kingdom 1 3%
Germany 1 3%
Unknown 30 94%

Demographic breakdown

Readers by professional status Count As %
Student > Ph. D. Student 5 16%
Student > Bachelor 4 13%
Other 4 13%
Researcher 4 13%
Student > Doctoral Student 2 6%
Other 5 16%
Unknown 8 25%
Readers by discipline Count As %
Pharmacology, Toxicology and Pharmaceutical Science 10 31%
Medicine and Dentistry 4 13%
Biochemistry, Genetics and Molecular Biology 3 9%
Agricultural and Biological Sciences 2 6%
Neuroscience 2 6%
Other 2 6%
Unknown 9 28%
Attention Score in Context

Attention Score in Context

This research output has an Altmetric Attention Score of 3. This is our high-level measure of the quality and quantity of online attention that it has received. This Attention Score, as well as the ranking and number of research outputs shown below, was calculated when the research output was last mentioned on 15 December 2023.
All research outputs
#8,535,684
of 25,374,917 outputs
Outputs from BMC Neuroscience
#395
of 1,294 outputs
Outputs of similar age
#32,931
of 135,085 outputs
Outputs of similar age from BMC Neuroscience
#3
of 4 outputs
Altmetric has tracked 25,374,917 research outputs across all sources so far. This one is in the 43rd percentile – i.e., 43% of other outputs scored the same or lower than it.
So far Altmetric has tracked 1,294 research outputs from this source. They receive a mean Attention Score of 4.7. This one has gotten more attention than average, scoring higher than 60% of its peers.
Older research outputs will score higher simply because they've had more time to accumulate mentions. To account for age we can compare this Altmetric Attention Score to the 135,085 tracked outputs that were published within six weeks on either side of this one in any source. This one is in the 16th percentile – i.e., 16% of its contemporaries scored the same or lower than it.
We're also able to compare this research output to 4 others from the same source and published within six weeks on either side of this one.