Adenosine Receptor Agonists
Adenosine is a purine nucleoside that binds to adenosine cell surface receptors, which are widely expressed in heart and blood vessel cells as well as in the brain, kidney and adipose tissue. There are 4 subtypes of P1 (adenosine) G protein-coupled receptors (GPCR), named A1, A2A, A2B, and A3, which...
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| Format: | Article |
| Language: | English |
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Barcaray International
2019-01-01
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| Series: | International Cardiovascular Forum Journal |
| Subjects: | |
| Online Access: | https://icfjournal.org/index.php/icfj/article/view/613/pdf |
| _version_ | 1811285669471846400 |
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| author | Markus Wallner Piotr Ponikowski |
| author_facet | Markus Wallner Piotr Ponikowski |
| author_sort | Markus Wallner |
| collection | DOAJ |
| description | Adenosine is a purine nucleoside that binds to adenosine cell surface receptors, which are widely expressed in heart and blood vessel cells as well as in the brain, kidney and adipose tissue. There are 4 subtypes of P1 (adenosine) G protein-coupled receptors (GPCR), named A1, A2A, A2B, and A3, which mediate a variety of cardioprotective and regenerative effects. In the heart, these effects are predominantly mediated through A1 receptors (A1R), which are expressed in atrial and ventricular cardiomyocytes and smooth muscle cells. Pre-clinical studies have reported multiple potential benefits achievable by modulation of adenyl cyclase with beneficial effects in a variety of pre-clinical models of cardiovascular disease including chronic heart failure (HF). A1R blockade (e.g. rolofylline) was however not successful in the PROTECT trial, where 2033 patients with acute HF and renal dysfunction were randomized to rolofylline or placebo, showed no benefit on renal function, symptoms, rehospitalization, or mortality. Following this attention turned to partial adenosine agonists, capadenoson and neladenoson bialanate hydrochloride, which has two phase II studies underway, PANACHE (HFpEF) and PANTHEON (HFrEF). |
| first_indexed | 2024-04-13T02:47:34Z |
| format | Article |
| id | doaj.art-4e66a13b5ee34ad5b7a9129c2d63e57f |
| institution | Directory Open Access Journal |
| issn | 2410-2636 2409-3424 |
| language | English |
| last_indexed | 2024-04-13T02:47:34Z |
| publishDate | 2019-01-01 |
| publisher | Barcaray International |
| record_format | Article |
| series | International Cardiovascular Forum Journal |
| spelling | doaj.art-4e66a13b5ee34ad5b7a9129c2d63e57f2022-12-22T03:05:57ZengBarcaray InternationalInternational Cardiovascular Forum Journal2410-26362409-34242019-01-01181114https://doi.org/10.17987/icfj.v18i0.613Adenosine Receptor AgonistsMarkus Wallner0Piotr Ponikowski1Division of Cardiology Medical University of Graz, AustriaHead of the Department of Heart Diseases, Wroclaw Medical University and Head of the Cardiology Department at the Center for Heart Diseases at 4th Military Hospital, Wroclaw, PolandAdenosine is a purine nucleoside that binds to adenosine cell surface receptors, which are widely expressed in heart and blood vessel cells as well as in the brain, kidney and adipose tissue. There are 4 subtypes of P1 (adenosine) G protein-coupled receptors (GPCR), named A1, A2A, A2B, and A3, which mediate a variety of cardioprotective and regenerative effects. In the heart, these effects are predominantly mediated through A1 receptors (A1R), which are expressed in atrial and ventricular cardiomyocytes and smooth muscle cells. Pre-clinical studies have reported multiple potential benefits achievable by modulation of adenyl cyclase with beneficial effects in a variety of pre-clinical models of cardiovascular disease including chronic heart failure (HF). A1R blockade (e.g. rolofylline) was however not successful in the PROTECT trial, where 2033 patients with acute HF and renal dysfunction were randomized to rolofylline or placebo, showed no benefit on renal function, symptoms, rehospitalization, or mortality. Following this attention turned to partial adenosine agonists, capadenoson and neladenoson bialanate hydrochloride, which has two phase II studies underway, PANACHE (HFpEF) and PANTHEON (HFrEF).https://icfjournal.org/index.php/icfj/article/view/613/pdfheart failureadenosine receptor agonists |
| spellingShingle | Markus Wallner Piotr Ponikowski Adenosine Receptor Agonists International Cardiovascular Forum Journal heart failure adenosine receptor agonists |
| title | Adenosine Receptor Agonists |
| title_full | Adenosine Receptor Agonists |
| title_fullStr | Adenosine Receptor Agonists |
| title_full_unstemmed | Adenosine Receptor Agonists |
| title_short | Adenosine Receptor Agonists |
| title_sort | adenosine receptor agonists |
| topic | heart failure adenosine receptor agonists |
| url | https://icfjournal.org/index.php/icfj/article/view/613/pdf |
| work_keys_str_mv | AT markuswallner adenosinereceptoragonists AT piotrponikowski adenosinereceptoragonists |