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" 4 The Adenosine A1 Receptor and its Ligands "
Peter G Nell Affiliation: Global Drug Discovery - Operations, Bayer HealthCare AG, Bayer Schering Pharma, Müllerstraße 178, 13353 Berlin, Germany
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BL
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784875
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b604889
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| Main Entry
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Peter G Nell Affiliation: Global Drug Discovery - Operations, Bayer HealthCare AG, Bayer Schering Pharma, Müllerstraße 178, 13353 Berlin, Germany
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| Title & Author
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4 The Adenosine A1 Receptor and its Ligands\ Peter G Nell Affiliation: Global Drug Discovery - Operations, Bayer HealthCare AG, Bayer Schering Pharma, Müllerstraße 178, 13353 Berlin, Germany
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9780444533005
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| Abstract
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This chapter discusses the adenosine A1 receptor and its ligands. The adenosine A1 receptor is a G-protein-coupled receptor of about 36 kDa with even transmembrane domain structure. Adenosine and adenosine A1 receptors are involved in the modulation of several physiological effects in heart, kidney, CNS, and lipid metabolism. Adenosine A1 receptor activation leads to: bradycardia, vasoconstriction, negative cardiac inotropy and dromotropy, and preconditioning in heart; decreased glomerular filtration rate, the inhibition of rennin release, antidiuresis, and the vasoconstriction of afferent arteries in the kidney; decreased transmitter release, decreased locomotor activity, sedation, and anti-convulsant effects in the CNS; and anti-lipolytic effects and an increase of insulin sensitivity in lipid metabolism. A large number of ligands for the adenosine receptors have been synthesized and evaluated for binding affinity to the A1 receptor. There is a broad spectrum of therapeutic opportunities for A1 agonists. This includes cardiovascular diseases, neuroprotection, and modulation of lipid metabolism. The major class of A1 agonistsis derived from adenosine and the structural requirements of these agonists for potency and selectivity is described in the chapter.
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Barbara Albrecht-Küpper Affiliation: Global Drug Discovery - Department of Cardiology Research, Bayer HealthCare AG, Bayer Schering Pharma, Aprather Weg 18a, 42096 Wuppertal, Germany
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Peter G Nell Affiliation: Global Drug Discovery - Operations, Bayer HealthCare AG, Bayer Schering Pharma, Müllerstraße 178, 13353 Berlin, Germany
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