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[125I]‐(Pyr1)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
Open accessAbstract
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. The binding of [125 I]‐(Pyr 1)Apelin‐13 to sections of human heart tissue was time dependent and rapid at 23°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. In saturation binding experiments [125 I]‐(Pyr 1)Apelin‐13 bound to human left ventricle with a KD value of 0.35±0.08 n M, 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 KD of 0.33±0.09 n M, B max of 3.1±0.6 fmol mg−1 protein and a Hill slope of 0.93±0.05. [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. (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 m M KCl. We provide the first evidence of APJ receptor expression, relative densities and functional properties of (Pyr 1)Apelin‐13 in human cardiovascular tissue. British Journal of Pharmacology (2001) 132, 1255–1260; doi:10.1038/sj.bjp.0703939
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Cited by
Ishida, J., Hashimoto, T., Hashimoto, Y., Nishiwaki, S., Iguchi, T., Harada, S., Sugaya, T., Matsuzaki, H., Yamamoto, R., Shiota, N., et al. (2004) · Journal of Biological Chemistry · doi:10.1074/jbc.m404149200 · Cited by 411
The exerkine apelin reverses age-associated sarcopenia
Vinel, C., Lukjanenko, L., Batut, A., Deleruyelle, S., Pradère, J.-P., Le Gonidec, S., Dortignac, A., Geoffre, N., Pereira, O., Karaz, S., et al. (2018) · Nature Medicine · doi:10.1038/s41591-018-0131-6 · Cited by 398
The apelin receptor APJ: journey from an orphan to a multifaceted regulator of homeostasis
O'Carroll, A.-M., Lolait, S. J., Harris, L. E., & Pope, G. R. (2013) · Journal of Endocrinology · doi:10.1530/joe-13-0227 · Cited by 344
Vascular Effects of Apelin In Vivo in Man
Japp, A. G., Cruden, N. L., Amer, D. A. B., Li, V. K. Y., Goudie, E. B., Johnston, N. R., Sharma, S., Neilson, I., Webb, D. J., Megson, I. L., et al. (2008) · Journal of the American College of Cardiology · doi:10.1016/j.jacc.2008.06.013 · Cited by 326
Maguire, J. J., Kleinz, M. J., Pitkin, S. L., & Davenport, A. P. (2009) · Hypertension · doi:10.1161/hypertensionaha.109.134619 · Cited by 323
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Metadata
- Authors
- Katugampola, S. D., Maguire, J. J., Matthewson, S. R., & Davenport, A. P.
- Venue
- British Journal of Pharmacology
- Publisher
- Wiley
- Published
- 2001-03
- Volume
- 132
- Issue
- 6
- Pages
- 1255-1260
- ISSN
- 0007-1188 (ISSN-L)
- 1476-5381
- OpenAlex
- W2069333438
- Cited by
- 216
- References
- 0
- FWCI
- 4.99
- Type
- journal article
- Language
- en
- Open access
- green
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- Katugampola, S. D., Maguire, J. J., Matthewson, S. R., & Davenport, A. P. (2001). [125I]‐(Pyr1)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. British Journal of Pharmacology. https://doi.org/10.1038/sj.bjp.0703939
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