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8-Cyclopentyl-1,3-dipropylxanthine (DPCPX) — a selective high affinity antagonist radioligand for A1 adenosine receptors
TLDR
The binding properties of 8-cyclopentyl-1,3-dipropylxanthine as an antagonist ligand for A1 adenosine receptors appeared superior to those of other agonist and antagonist radioligands for the A1 receptor.
Towards a revised nomenclature for P1 and P2 receptors.
Variations and increase in use of statins across Europe: data from administrative databases
TLDR
Data on statin use by total defined daily doses and then calculated doses per 1000 of the population covered (by the relevant data source) in 13 of the 15 European Union countries and in Norway for the year 2000 are collected.
Policies to Enhance Prescribing Efficiency in Europe: Findings and Future Implications
TLDR
The 4E methodology allows European countries to concisely capture the range of current demand-side measures and plan for the future knowing that initiatives can be additive to further enhance their prescribing efficiency.
Facilitation by adenosine of the action of insulin on the accumulation of adenosine 3':5'-monophosphate, lipolysis, and glucose oxidation in isolated fat cells.
The modulation of insulin action by adenosine has been studied in lipid and glucose metabolism of isolated rat fat cells. When 20000 cells per ml were incubated, insulin failed to antagonize the
Two affinity states of Ri adenosine receptors in brain membranes. Analysis of guanine nucleotide and temperature effects on radioligand binding.
TLDR
The data indicate that guanine nucleotides convert the Ri adenosine receptor from a high- to a low-agonist affinity state and that agonist binding shows thermodynamic differences from antagonist binding only when it is to the high-affinity state of the receptor.
Measurement of guanine nucleotide-binding protein activation by A1 adenosine receptor agonists in bovine brain membranes: stimulation of guanosine-5'-O-(3-[35S]thio)triphosphate binding.
TLDR
The inclusion of 100 mM NaCl as well as increasing GDP concentrations led to a parallel increase of Ki values and EC50 values, and both compounds induced a shift of A1 adenosine receptors from the high affinity state for agonists to the low affinity state.
Interaction of full and partial agonists of the A1 adenosine receptor with receptor/G protein complexes in rat brain membranes.
TLDR
The lower efficacy in stimulation of the binding of [35S]GTP[S] is probably the consequence of an impaired ability of the partial agonists to release GDP from the G protein, as was shown by an impaired release of prebound G protein activation from the membranes.
2-Chloro-N6-cyclopentyladenosine: a highly selective agonist at A1 adenosine receptors
TLDR
CCPA is an agonist at A1 adenosine receptors with a 4-foldHigher selectivity and 2-fold higher affinity than CPA, and a considerably higher selectivity than the standard A1 receptor agonist R-N6-phenylisopropyladenosine (R-PIA).
Comparison of national administrative and commercial databases to monitor expenditure and costs of statins across Europe
TLDR
Administrative databases can give useful utilisation data, which are broadly comparable with those from commercial sources, but cost data differ more, and the figures for each may be useful in different settings.
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