| Are there functional β₃-adrenoceptors in the human heart? | |
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MedLine Citation:
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PMID: 20735409 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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β₃-Adrenoceptor mRNA is expressed in the human heart, but corresponding receptor protein has not yet consistently been demonstrated. Furthermore, their physiological role remains highly controversial. For example, in human atria these receptors apparently do not promote cAMP formation. Evidence presented in this issue of the BJP suggests that a previously reported β₃-adrenoceptor-mediated stimulation of Ca(2+) channels at room temperature is absent at physiological temperatures, and that β₃-adrenoceptors have no effect on atrial contraction. Drugs classified as β₃-adrenoceptor agonists cause contraction in human atria but in most cases this involves β₁- and/or β₂-adrenoceptors. In contrast, in human ventricles β₃-adrenoceptor agonists can exhibit negative inotropic effects, potentially involving Pertussis toxin-sensitive G-proteins and activation of a NO synthase. However, firmer pharmacological evidence is required that these effects indeed occur via β₃-adrenoceptors. Whether the expected future use of β₃-adrenoceptor agonists in the treatment of urinary bladder dysfunction is associated with adverse events related to cardiac function remains to be determined from clinical studies. |
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Authors:
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Martin C Michel; Sian E Harding; Richard A Bond |
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Publication Detail:
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Type: Comment; Journal Article; Review |
Journal Detail:
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Title: British journal of pharmacology Volume: 162 ISSN: 1476-5381 ISO Abbreviation: Br. J. Pharmacol. Publication Date: 2011 Feb |
Date Detail:
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Created Date: 2011-01-21 Completed Date: 2011-05-11 Revised Date: 2012-02-01 |
Medline Journal Info:
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Nlm Unique ID: 7502536 Medline TA: Br J Pharmacol Country: England |
Other Details:
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Languages: eng Pagination: 817-22 Citation Subset: IM |
Copyright Information:
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© 2011 The Authors. British Journal of Pharmacology © 2011 The British Pharmacological Society. |
Affiliation:
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Department of Pharmacology & Pharmacotherapy, University of Amsterdam, Amsterdam, The Netherlands. m.c.michel@amc.nl |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Adrenergic beta-3 Receptor Agonists
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pharmacology Adrenergic beta-3 Receptor Antagonists / pharmacology Calcium Channels, L-Type / metabolism Heart / drug effects Humans Myocardial Contraction / drug effects Myocardium / metabolism* Receptors, Adrenergic, beta-3 / metabolism* |
| Chemical | |
Reg. No./Substance:
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0/Adrenergic beta-3 Receptor Agonists; 0/Adrenergic beta-3 Receptor Antagonists; 0/Calcium Channels, L-Type; 0/Receptors, Adrenergic, beta-3 |
| Comments/Corrections | |
Comment On:
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Br J Pharmacol. 2011 Feb;162(4):823-39
[PMID:
20726983
]
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From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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