ArticleBritish journal of pharmacology2001
[(125)I]-(Pyr(1))Apelin-13 is a novel radioligand for localizing the APJ orphan receptor in human and rat tissues with evidence for a vasoconstrictor role in man.
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 66 papers.
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Who cites it
66 citing papers in PubMed, 213 citations in OpenAlex.
- The exerkine apelin reverses age-associated sarcopenia.Nature medicine · 2018Trial
- The relationship between apelin and cardiac parameters in patients on peritoneal dialysis: is there a new cardiac marker?BMC nephrology · 2014Trial
- International Union of Basic and Clinical Pharmacology. CXXI. Apelin receptor pharmacology in the human cardiovascular system and emerging clinical applications.Pharmacological reviews · 2026Review
- Metabolically stable apelin analogs: development and functional role in water balance and cardiovascular function.Clinical science (London, England : 1979) · 2025Review
- Evaluating Apelin as a Potential Biomarker in Major Depressive Disorder: Its Correlation with Clinical Symptomatology.International journal of molecular sciences · 2024Article
- Microparticle Mediated Delivery of Apelin Improves Heart Function in Post Myocardial Infarction Mice.Circulation research · 2024Article
- Apelin and Copeptin Levels in Patients With Chronic SIAD Treated With Empagliflozin.Journal of the Endocrine Society · 2024Article
- ELABELA/APJ Axis Prevents Diabetic Glomerular Endothelial Injury by Regulating AMPK/NLRP3 Pathway.Inflammation · 2023Article
- Intravenous administration of apeling-13 induces a depressor response by releasing an unidentified substance.Biochemical and biophysical research communications · 2023Article
- APJ as Promising Therapeutic Target of Peptide Analogues in Myocardial Infarction- and Hypertension-Induced Heart Failure.Pharmaceutics · 2023Review
- Chronic Effects of Apelin on Cardiovascular Regulation and Angiotensin II-Induced Hypertension.Pharmaceuticals (Basel, Switzerland) · 2023Article
- Expanding the apelin receptor pharmacological toolbox using novel fluorescent ligands.Frontiers in endocrinology · 2023Article
- The therapeutic potential of apelin in kidney disease.Nature reviews. Nephrology · 2021Review
- Identification of 6-Hydroxypyrimidin-4(1ACS medicinal chemistry letters · 2021Article
- In Vitro and In Vivo Evaluation of a Small-Molecule APJ (Apelin Receptor) Agonist, BMS-986224, as a Potential Treatment for Heart Failure.Circulation. Heart failure · 2021Article
- Apelin and Vasopressin: The Yin and Yang of Water Balance.Frontiers in endocrinology · 2021Review
- Apelin Does Not Impair Coronary Artery Relaxation Mediated by Nitric Oxide-Induced Activation of BKFrontiers in pharmacology · 2021Article
- Article
- Apelin inhibits an endothelium-derived hyperpolarizing factor-like pathway in rat cerebral arteries.Peptides · 2020Article
- Increased apelin receptor gene expression in the subfornical organ of spontaneously hypertensive rats.PloS one · 2020Article
6 more citing papers are in PubMed but not listed here.
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Authors and funding
4 authors at 3 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
1. We have determined the binding characteristics of [(125)I]-(Pyr(1))Apelin-13, a putative ligand for the APJ orphan receptor in human cardiovascular and rat tissue and investigated the functional properties of (Pyr(1))Apelin-13 in human saphenous vein. 2. The binding of [(125)I]-(Pyr(1))Apelin-13 to sections of human heart tissue was time dependent and rapid at 23 degrees C. Data were fitted to a single site model with an association rate constant (k(obs)) of 0.115 min(-1). [(125)I]-(Pyr(1))Apelin-13 also dissociated from a single site with a dissociation rate constant of 0.0105 min(-1). 3. In saturation binding experiments [(125)I]-(Pyr(1))Apelin-13 bound to human left ventricle with a K(D) value of 0.35+/-0.08 nM, B(max) of 4.3+/-0.9 fmol mg(-1) protein with a Hill slope of 0.97+/-0.04 and to the right atria with a K(D) of 0.33+/-0.09 nM, B(max) of 3.1+/-0.6 fmol mg(-1) protein and a Hill slope of 0.93+/-0.05. 4. [(125)I]-(Pyr(1))Apelin-13 binding sites were localized using autoradiography to human cardiovascular tissue, including coronary artery, aorta and saphenous vein grafts. In rat tissue a high density of receptors were localized to the molecular layer of the rat cerebellum, rat lung, rat heart and low levels in the rat kidney cortex. 2. (Pyr(1))Apelin-13 potently contracted human saphenous vein with a pD(2) value of 8.4+/-0.2 (n=8). The maximum response elicited by the peptide was 22.6+/-6% of 100 mM KCl. 6. We provide the first evidence of APJ receptor expression, relative densities and functional properties of (Pyr(1))Apelin-13 in human cardiovascular tissue.
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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.