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Some 56 million years ago, a massive pulse of carbon dioxide into the atmosphere sent global temperatures soaring. In the oceans, carbonate sediments…
Adenosine is a modulator of many physiological and pathophysiological processes in the central nervous system (CNS). Blockade of the adenosine receptors A1ARs and A2AARs has shown beneficial neuroprotective effects in animal models and in clinical studies of Parkinsons’s disease (PD) and Alzheimer’s disease (AD). There is still no satisfactory multitarget drug approach which inhibits MAO-A and the two adenosine receptors A1ARs and A2AARs. This invention provides newly designed tricyclic xanthine derivatives which allow overcoming this problem. A variety of 69 derivatives were prepared and evaluated in radioligand binding studies at adenosine receptors and for their ability to inhibit monoamine oxidases. Potent dual-target-directed A1/A2A adenosine receptor antagonists were identified. Several compounds even showed triple-target inhibition.
The scientists recommend reconciling the rapid infrastructure development that is currently taking place in Mongolia with the needs of migratory species, such…
If Nina Mahmoudian has her way, the next generation of autonomous underwater vehicles (AUVs) will have a much better chance of getting it right.
The best estimates currently available suggest that 350,000 deaths in each year in Europe are due to so called 'out-of-hospital cardiac arrest' (OOH-CA).This…
Worldwide, major cities stand to gain around $800 billion per year of economic opportunity from 2030 by upgrading their public transportation networks. This is…