ArticleBritish journal of pharmacology2005
Positron emission tomography using 18F-labelled endothelin-1 reveals prevention of binding to cardiac receptors owing to tissue-specific clearance by ET B receptors in vivo.
Article in British journal of pharmacology, 2005. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 papers, 1 of them a synthesis that pooled it.
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Who cites it
21 citing papers in PubMed, 1 synthesis or guideline pooled it, 65 citations in OpenAlex.
- The Role of Endothelin in the Pathophysiology of Migraine-a Systematic Review.Current pain and headache reports · 2018Pooled it
- Selective endothelin-1 receptor type A inhibition in subjects undergoing cardiac surgery with preexisting left ventricular dysfunction: Influence on early postoperative hemodynamics.The Journal of thoracic and cardiovascular surgery · 2010Trial
- ET-1 as a Sex-Specific Mechanism Impacting Age-Related Changes in Vascular Function.Frontiers in aging · 2021Review
- Intravascular Endothelin-1 does not trigger or increase susceptibility to Spreading Depolarizations.The journal of headache and pain · 2020Article
- Distortion of KPharmacology research & perspectives · 2017Article
- The heart as an extravascular target of endothelin-1 in particulate matter-induced cardiac dysfunction.Pharmacology & therapeutics · 2016Review
- Endothelin.Pharmacological reviews · 2016Review
- Endothelin receptors and their antagonists.Seminars in nephrology · 2015Review
- MicroRNA regulation of endothelin-1 mRNA in renal collecting duct cells.Life sciences · 2014Article
- Modulation of endothelin receptors in the failing right ventricle of the heart and vasculature of the lung in human pulmonary arterial hypertension.Life sciences · 2014Article
- Tissue-specific and time-dependent regulation of the endothelin axis by the circadian clock protein Per1.Life sciences · 2014Article
- Adaptive regulation of endothelin receptor type-A and type-B in vascular smooth muscle cells during pregnancy in rats.Journal of cellular physiology · 2014Article
- Molecular imaging of the pulmonary circulation in health and disease.Clinical and translational imaging · 2014Review
- Endothelin antagonism and its role in the treatment of hypertension.Current hypertension reports · 2013Review
- Endothelin-2, the forgotten isoform: emerging role in the cardiovascular system, ovarian development, immunology and cancer.British journal of pharmacology · 2013Review
- Themed section: Imaging in pharmacology.British journal of pharmacology · 2010Article
- Positron emission tomography of [18F]-big endothelin-1 reveals renal excretion but tissue-specific conversion to [18F]-endothelin-1 in lung and liver.British journal of pharmacology · 2010Article
- Endothelin receptors and pain.The journal of pain · 2009Review
- Activation of ETB receptors regulates the abundance of ET-1 mRNA in vascular endothelial cells.British journal of pharmacology · 2008Article
- The endothelin system as a therapeutic target in cardiovascular disease: great expectations or bleak house?British journal of pharmacology · 2008Review
Corrections and comments
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Authors and funding
8 authors at 2 institutions in 1 country.
Funding
Abstract
Our aim was to synthesise an (18)F analogue of endothelin-1 (ET-1), to dynamically image ET receptors in vivo by positron emission tomography (PET) and to elucidate the function of the ET(B) subtype as a clearing receptor in organs expressing high densities including kidney and lung.[(18)F]-ET-1 was characterised in vitro and bound with a single subnanomolar affinity (K(D)=0.43+/-0.05 nM, B(max)=27.8+/-2.1 fmol mg(-1) protein) to human left ventricle (n=4). The in vivo distribution of [(18)F]-ET-1 in anaesthetised rats was measured using a dedicated small animal PET scanner (microPET) and ex vivo analysis. Dynamic PET data demonstrated that high levels of radioligand accumulated rapidly in the lung, kidney and liver, consistent with receptor binding. The in vivo distribution correlated with the anatomical localisation of receptors detected in vitro using [(125)I]-ET-1. However, the receptor density visualised in the heart was unexpectedly low compared with that predicted from the in vitro measurements.[(18)F]-ET-1 binding in lungs could not be displaced by the ET(B) selective antagonist BQ788, in agreement with the proposed internalisation of ET-1 by ET(B) receptors. In contrast, infusion of BQ788 prior to injecting [(18)F]-ET-1 significantly reduce the amount of radioligand visualised in the ET(B) rich lung and kidney by 85% (P< 0.05, n=3) and 55% (P<0.05, n=3), respectively. Under conditions of ET(B) receptor blockade, the heart could be visualised by microPET imaging.These results suggest that clearance by ET(B) receptors in the lung and kidney prevents binding of ET-1 to receptors in the heart.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.