Cardiac adrenergic receptor effects of carvedilol (original) (raw)
Journal Article
,
Division of Cardiology, The Temple Hoyne Buell Heart Research Laboratories, University of Colorado Health Sciences Center, U.S.A.
Search for other works by this author on:
,
Division of Cardiology, The Temple Hoyne Buell Heart Research Laboratories, University of Colorado Health Sciences Center, U.S.A.
Search for other works by this author on:
,
Division of Cardiology, The Temple Hoyne Buell Heart Research Laboratories, University of Colorado Health Sciences Center, U.S.A.
Search for other works by this author on:
,
Division of Cardiology, The Temple Hoyne Buell Heart Research Laboratories, University of Colorado Health Sciences Center, U.S.A.
Search for other works by this author on:
,
Division of Cardiology, The Temple Hoyne Buell Heart Research Laboratories, University of Colorado Health Sciences Center, U.S.A.
Search for other works by this author on:
,
Division of Cardiology, The Temple Hoyne Buell Heart Research Laboratories, University of Colorado Health Sciences Center, U.S.A.
Search for other works by this author on:
,
Division of Cardiology, The Temple Hoyne Buell Heart Research Laboratories, University of Colorado Health Sciences Center, U.S.A.
Search for other works by this author on:
,
Division of Cardiology, The Temple Hoyne Buell Heart Research Laboratories, University of Colorado Health Sciences Center, U.S.A.
Search for other works by this author on:
,
Division of Cardiology, The Temple Hoyne Buell Heart Research Laboratories, University of Colorado Health Sciences Center, U.S.A.
Search for other works by this author on:
Division of Cardiology, The Temple Hoyne Buell Heart Research Laboratories, University of Colorado Health Sciences Center, U.S.A.
Correspondence: Michael R. Bristow, MD, PhD, University of Colorado, Health Sciences Center, Cardiology, B-139, 4200 East Ninth Avenue, Denver, Colorado 80262, U.S A.
Search for other works by this author on:
PDF Cite
T. Yoshikawa, J. D. Port, K. Asano, P. Chidiak, M. Bouvier, D. Dutcher, R. L. Roden, W. Minobe, K. D. Tremmel, M. R. Bristow, Cardiac adrenergic receptor effects of carvedilol, European Heart Journal, Volume 17, Issue suppl_B, April 1996, Pages 8–16, https://doi.org/10.1093/eurheartj/17.suppl_B.8
Close
Navbar Search Filter Mobile Enter search term Search
Abstract
Carvedilol is an adrenoceptor antagonist which modulates the activity not only of β1 and β1 but also of α1 adrenergic receptors present on the cell surface membrane of the human cardiac myocyte. In the heart, carvedilol has approximately 7 times higher potency for 13, and 132 adrenoceptors, but in the doses 50–100 mg. day−1 used in clinical practice, it is essentially non-selective. In human myocardial preparations and in cultured heart cells, carvedilol has no intrinsic sympathomimetic activity but is able to identify high affinity agonist-binding receptors whose pharmaco logical signature is reduction in binding by incubation with guanine nucleotides (guanine nucleotide-modulatable binding). This property is more prominent for the human β2 than for the β1adrenoceptor. The property of gaunine nucleotide-modulatable binding for carvedilol and structurally related bucindolol correlates with their ability to directly down-regulate β1-like receptors present in cultured chick myocytes, and with a lack of reversal of down-regulation of cardiac β-receptors in patients with heart failure. Carvedilol does not exhibit high levels of inverse agonist activity, which may contribute to its good tolerability in subjects with heart failure.
These data indicate that carvedilol produces a high degree of adrenergic receptor blockade in the failing human heart, and does not re-sensitize the β-receptor pathway to stimulation by adrenergic agonists.
This content is only available as a PDF.
© 1996 1996 The European Society of Cardiology
Topic:
- cardiac myocytes
- myocardium
- carvedilol
- heart failure
- adrenergic agonists
- down-regulation
- guanine
- guanine nucleotides
- tissue membrane
- nucleotides
- adrenergic receptor
- sympathomimetics
- heart
- agonists
- antagonists
- bucindolol
- muscle cells
- affinity
- drug inverse agonism
Advertisement intended for healthcare professionals
Citations
Views
Altmetric
Metrics
Total Views 1,062
49 Pageviews
1,013 PDF Downloads
Since 12/1/2016
| Month: | Total Views: |
|---|---|
| December 2016 | 2 |
| February 2017 | 4 |
| March 2017 | 3 |
| June 2017 | 6 |
| July 2017 | 4 |
| August 2017 | 1 |
| September 2017 | 5 |
| October 2017 | 8 |
| December 2017 | 8 |
| January 2018 | 6 |
| February 2018 | 21 |
| March 2018 | 12 |
| April 2018 | 5 |
| May 2018 | 4 |
| June 2018 | 9 |
| July 2018 | 3 |
| August 2018 | 3 |
| September 2018 | 5 |
| October 2018 | 6 |
| November 2018 | 9 |
| December 2018 | 10 |
| January 2019 | 6 |
| February 2019 | 18 |
| March 2019 | 11 |
| April 2019 | 17 |
| May 2019 | 13 |
| June 2019 | 9 |
| July 2019 | 22 |
| August 2019 | 20 |
| September 2019 | 36 |
| October 2019 | 23 |
| November 2019 | 42 |
| December 2019 | 12 |
| January 2020 | 13 |
| February 2020 | 25 |
| March 2020 | 24 |
| April 2020 | 24 |
| May 2020 | 11 |
| June 2020 | 12 |
| July 2020 | 10 |
| August 2020 | 13 |
| September 2020 | 7 |
| October 2020 | 11 |
| November 2020 | 5 |
| December 2020 | 10 |
| January 2021 | 6 |
| February 2021 | 11 |
| March 2021 | 13 |
| April 2021 | 12 |
| May 2021 | 13 |
| June 2021 | 7 |
| July 2021 | 6 |
| August 2021 | 3 |
| September 2021 | 15 |
| October 2021 | 8 |
| November 2021 | 14 |
| December 2021 | 17 |
| January 2022 | 17 |
| February 2022 | 22 |
| March 2022 | 12 |
| April 2022 | 23 |
| May 2022 | 16 |
| June 2022 | 6 |
| July 2022 | 10 |
| August 2022 | 5 |
| September 2022 | 21 |
| October 2022 | 15 |
| November 2022 | 24 |
| December 2022 | 16 |
| January 2023 | 6 |
| February 2023 | 13 |
| March 2023 | 16 |
| April 2023 | 1 |
| May 2023 | 10 |
| June 2023 | 4 |
| July 2023 | 6 |
| August 2023 | 9 |
| September 2023 | 8 |
| October 2023 | 9 |
| November 2023 | 9 |
| December 2023 | 15 |
| January 2024 | 6 |
| February 2024 | 13 |
| March 2024 | 9 |
| April 2024 | 12 |
| May 2024 | 9 |
| June 2024 | 10 |
| July 2024 | 15 |
| August 2024 | 17 |
| September 2024 | 14 |
| October 2024 | 9 |
| November 2024 | 2 |
Citations
132 Web of Science
×
Email alerts
Related articles in PubMed
Citing articles via
More from Oxford Academic
Advertisement intended for healthcare professionals