ArticleBritish journal of pharmacology2001
[125I-His(9)]-ghrelin, a novel radioligand for localizing GHS orphan receptors in human and rat tissue: up-regulation of receptors with athersclerosis.
Article in British journal of pharmacology, 2001. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 39 papers.
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Who cites it
39 citing papers in PubMed, 190 citations in OpenAlex.
- Acute peripheral metabolic effects of intraarterial ghrelin infusion in healthy young men.The Journal of clinical endocrinology and metabolism · 2011Trial
- The Orally Available Ghrelin Receptor-Agonist AC01 Improves Systolic Function in HFrEF Mice and Nonhuman Primates.JACC. Basic to translational science · 2026Article
- Obesity-Induced PVAT Dysfunction and Atherosclerosis Development: The Role of GHSR-1a in Increased Macrophage Infiltration and Adipocytokine Secretion.Journal of cardiovascular development and disease · 2025Article
- Effects of Weight Loss on Endothelium and Vascular Homeostasis: Impact on Cardiovascular Risk.Biomedicines · 2025Review
- N-Terminal Pro-Brain Natriuretic Peptide Correlates with Ghrelin and Acyl-Ghrelin in Pre-Dialysis Chronic Kidney Disease.International journal of molecular sciences · 2024Observational
- Ghrelin is essential for lowering blood pressure during torpor.Frontiers in endocrinology · 2024Article
- Effect of Ghrelin on the Cardiovascular System.Biology · 2022Review
- Regional Differences in the Ghrelin-Growth Hormone Secretagogue Receptor Signalling System in Human Heart Disease.CJC open · 2021Article
- Acylated Ghrelin as a Multi-Targeted Therapy for Alzheimer's and Parkinson's Disease.Frontiers in neuroscience · 2020Review
- Physiological significance of ghrelin in the cardiovascular system.Proceedings of the Japan Academy. Series B, Physical and biological sciences · 2019Review
- Less Exploited GPCRs in Precision Medicine: Targets for Molecular Imaging and Theranostics.Molecules (Basel, Switzerland) · 2018Review
- The CD36-PPARγ Pathway in Metabolic Disorders.International journal of molecular sciences · 2018Review
- Exploring the Behavioral and Metabolic Phenotype Generated by Re-Introduction of the Ghrelin Receptor in the Ventral Tegmental Area.International journal of molecular sciences · 2017Article
- Development of Fluorinated Non-Peptidic Ghrelin Receptor Ligands for Potential Use in Molecular Imaging.International journal of molecular sciences · 2017Article
- Ghrelin-Induced Enhancement of Vasopressin and Oxytocin Secretion in Rat Neurohypophyseal Cell Cultures.Journal of molecular neuroscience : MN · 2016Article
- Ghrelin inhibits AngII -induced expression of TNF-α, IL-8, MCP-1 in human umbilical vein endothelial cells.International journal of clinical and experimental medicine · 2015Article
- The Concise Guide to PHARMACOLOGY 2013/14: G protein-coupled receptors.British journal of pharmacology · 2013Article
- Effect of ghrelin on inflammatory response in lung contusion.The Kaohsiung journal of medical sciences · 2013Article
- AMPK activity is down-regulated in endothelial cells of GHS-R(-/-) mice.International journal of clinical and experimental pathology · 2013Article
- A role of ghrelin in canine mammary carcinoma cells proliferation, apoptosis and migration.BMC veterinary research · 2012Article
Corrections and comments
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Authors and funding
3 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
1. Ghrelin is the recently identified endogenous ligand for the cloned growth hormone secretagogue receptor (GHS-R). We have characterized for the first time the binding of human [125I-His(9)]-ghrelin to normal human and rat tissue and demonstrated expression of this 'orphan' receptor that has previously been predicted to exist from mRNA. Furthermore, we have discovered that [125I-His(9)]-ghrelin density is significantly increased in atherosclerosis. 2. [125I-His(9)]-Ghrelin bound to non-diseased human heart (left ventricle) with an association rate constant (k(obs)) of 0.16+/-0.004 min(-1), a dissociation rate constant of 0.068+/-0.0005 min(-1) (kinetically derived K(D) of 0.1 nM; n=5 individuals+/-s.e.mean), a K(D) of 0.43+/-0.08 nM and B(max) of 7.8+/-0.9 fmol mg(-1) protein (n=6 individual+/-s.e.mean). 3. Specific [125I-His(9)]-ghrelin binding was to the human vasculature including aorta, coronary, pulmonary, arcuate arteries in the kidney and saphenous veins. In rat tissues, binding sites were also localized to the vasculature in peripheral tissues as well as the granular layer of the cerebellum in the CNS. 4. [125I-His(9)]-Ghrelin binding was significantly up-regulated (3 - 4 fold) in both atherosclerotic coronary arteries and saphenous vein grafts with advanced intimal thickening, compared with normal vessels (P<0.05). 5. Our results suggest that the native receptor for [125I-His(9)]-ghrelin may be widely distributed in the human cardiovascular system. Furthermore, changes in the density of this proposed ghrelin receptor implicates this new transmitter system in the development of atherosclerosis and may therefore represent a novel therapeutic target in the treatment of cardiovascular disease.
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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.