| Title |
8-Cyclopentyl-1,3-dipropylxanthine (DPCPX) — a selective high affinity antagonist radioligand for A1 adenosine receptors
|
|---|---|
| Published in |
Naunyn-Schmiedeberg's Archives of Pharmacology, August 1987
|
| DOI | 10.1007/bf00165806 |
| Pubmed ID | |
| Authors |
Martin J. Lohse, Karl-Norbert Klotz, Jutta Lindenborn-Fotinos, Martin Reddington, Ulrich Schwabe, Ray A. Olsson |
| Abstract |
The properties of 8-cyclopentyl-1,3-dipropylxanthine (DPCPX) as an antagonist ligand for A1 adenosine receptors were examined and compared with other radioligands for this receptor. DPCPX competitively antagonized both the inhibition of adenylate cyclase activity via A1 adenosine receptors and the stimulation via A2 adenosine receptors. The Ki-values of this antagonism were 0.45 nM at the A1 receptor of rat fat cells, and 330 nM at the A2 receptor of human platelets, giving a more than 700-fold A1-selectivity. A similar A1-selectivity was determined in radioligand binding studies. Even at high concentrations, DPCPX did not significantly inhibit the soluble cAMP-phosphodiesterase activity of human platelets. [3H]DPCPX (105 Ci/mmol) bound in a saturable manner with high affinity to A1 receptors in membranes of bovine brain and heart, and rat brain and fat cells (KD-values 50-190 pM). Its nonspecific binding was about 1% of total at KD, except in bovine myocardial membranes (about 10%). Binding studies with bovine myocardial membranes allowed the analysis of both the high and low agonist affinity states of this receptor in a tissue with low receptor density. The binding properties of [3H]DPCPX appear superior to those of other agonist and antagonist radioligands for the A1 receptor. |
Mendeley readers
The data shown below were compiled from readership statistics for 103 Mendeley readers of this research output. Click here to see the associated Mendeley record.
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| United Kingdom | 1 | <1% |
| Germany | 1 | <1% |
| France | 1 | <1% |
| Unknown | 100 | 97% |
Demographic breakdown
| Readers by professional status | Count | As % |
|---|---|---|
| Student > Bachelor | 19 | 18% |
| Student > Ph. D. Student | 12 | 12% |
| Researcher | 7 | 7% |
| Professor > Associate Professor | 5 | 5% |
| Student > Master | 5 | 5% |
| Other | 6 | 6% |
| Unknown | 49 | 48% |
| Readers by discipline | Count | As % |
|---|---|---|
| Pharmacology, Toxicology and Pharmaceutical Science | 15 | 15% |
| Chemistry | 11 | 11% |
| Biochemistry, Genetics and Molecular Biology | 7 | 7% |
| Agricultural and Biological Sciences | 7 | 7% |
| Neuroscience | 5 | 5% |
| Other | 9 | 9% |
| Unknown | 49 | 48% |
Attention Score in Context
This research output has an Altmetric Attention Score of 9. 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 01 August 2017.
All research outputs
#3,272,356
of 22,788,370 outputs
Outputs from Naunyn-Schmiedeberg's Archives of Pharmacology
#89
of 1,724 outputs
Outputs of similar age
#641
of 12,168 outputs
Outputs of similar age from Naunyn-Schmiedeberg's Archives of Pharmacology
#1
of 5 outputs
Altmetric has tracked 22,788,370 research outputs across all sources so far. Compared to these this one has done well and is in the 84th percentile: it's in the top 25% of all research outputs ever tracked by Altmetric.
So far Altmetric has tracked 1,724 research outputs from this source. They receive a mean Attention Score of 4.0. This one has done particularly well, scoring higher than 92% 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 12,168 tracked outputs that were published within six weeks on either side of this one in any source. This one has done particularly well, scoring higher than 90% of its contemporaries.
We're also able to compare this research output to 5 others from the same source and published within six weeks on either side of this one. This one has scored higher than all of them