%0 Journal Article %1 Klotz2000 %A Klotz, K. N. %D 2000 %J Naunyn Schmiedebergs Arch Pharmacol %K Animals Assay Humans Ligands P1/analysis/*drug Purinergic Radioligand Relationship Structure-Activity Xanthine/pharmacology effects/physiology Receptor %N 4-5 %P 382-91 %T Adenosine receptors and their ligands %U http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&dopt=Citation&list_uids=11111832 %V 362 %X The regulatory actions of adenosine are mediated via four subtypes of G protein-coupled receptors distinguished as A1, A2A, A2B and A3 receptors. Their presence on basically every cell makes them an interesting target for the pharmacological intervention in many pathophysiological situations. A large number of ligands have been synthesized over the last two decades and provide agonists and antagonists that are more or less selective for the known receptor subtypes. In addition, many radioligands are available in tritiated or radioiodinated form. The comparative pharmacological characterization of all four human adenosine receptor subtypes revealed that some of the compounds thought to be selective from data in other species have unexpected potencies at human receptors. As a result, compounds that exhibit high affinity to only one subtype are an exception. Although the selection of ligands is immense, it is less than satisfying for most subtypes of adenosine receptors.

@article{Klotz2000, abstract = {The regulatory actions of adenosine are mediated via four subtypes of G protein-coupled receptors distinguished as A1, A2A, A2B and A3 receptors. Their presence on basically every cell makes them an interesting target for the pharmacological intervention in many pathophysiological situations. A large number of ligands have been synthesized over the last two decades and provide agonists and antagonists that are more or less selective for the known receptor subtypes. In addition, many radioligands are available in tritiated or radioiodinated form. The comparative pharmacological characterization of all four human adenosine receptor subtypes revealed that some of the compounds thought to be selective from data in other species have unexpected potencies at human receptors. As a result, compounds that exhibit high affinity to only one subtype are an exception. Although the selection of ligands is immense, it is less than satisfying for most subtypes of adenosine receptors.}, added-at = {2010-12-14T18:12:02.000+0100}, author = {Klotz, K. N.}, biburl = {https://www.bibsonomy.org/bibtex/2c023037212c5f6a7624a94583f74a8a8/pharmawuerz}, endnotereftype = {Journal Article}, interhash = {0e334b4e883e5659d89fed6291d57833}, intrahash = {c023037212c5f6a7624a94583f74a8a8}, issn = {0028-1298 (Print) 0028-1298 (Linking)}, journal = {Naunyn Schmiedebergs Arch Pharmacol}, keywords = {Animals Assay Humans Ligands P1/analysis/*drug Purinergic Radioligand Relationship Structure-Activity Xanthine/pharmacology effects/physiology Receptor}, month = Nov, note = {Klotz, K N Research Support, Non-U.S. Gov't Review Germany Naunyn-Schmiedeberg's archives of pharmacology Naunyn Schmiedebergs Arch Pharmacol. 2000 Nov;362(4-5):382-91.}, number = {4-5}, pages = {382-91}, shorttitle = {Adenosine receptors and their ligands}, timestamp = {2010-12-14T18:20:04.000+0100}, title = {Adenosine receptors and their ligands}, url = {http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&dopt=Citation&list_uids=11111832}, volume = 362, year = 2000 }