Binding of [3H] SR 49059, a potent nonpeptide vasopressin V1a antagonist, to rat and human liver membranes
Abstract
The new potent and selective nonpeptide vasopressin V1a antagonist, SR 49059, was tritiated and used for the characterization of rat and human liver AVP V1a receptors. Binding of [3H] SR 49059 was time-dependent, reversible and saturable. A single class of high affinity binding sites was identified with Kd values of 0.63 +/- 0.13 and 2.95 +/- 0.64 nM, in rat and human liver membranes, respectively. The maximal binding capacity (Bmax) was about 7 times higher in rat than in human liver preparations. The relative potencies of several AVP/oxytocin agonists or antagonists to inhibit [3H] SR 49059 binding confirmed that this ligand labeled a homogeneous population of sites with the expected AVP V1a profile. Furthermore, [3H] SR 49059 or unlabeled SR 49059 displayed only slight species differences between rat and human V1a receptors, whereas OPC-21268, another nonpeptide V1a antagonist, exhibited a high species-related potency with more than 500 fold higher affinity for rat than for human liver V1a receptors. Thus, [3H] SR 49059 is the first nonpeptide AVP V1a ligand reported having highly specific activity, stability, specificity and affinity. This makes it a suitable probe for labeling AVP V1a receptors in rat and also in human tissues.
Integrity signals
Registry
Cites
Statistics
Claims the paper makes
Claims other papers make about this one
Each is checked against this paper’s own text: does it say what the citing paper says it does?
Vasopressin transiently increases glycemia in healthy humans.
“A causal link between vasopressin and glucose homeostasis is plausible because vasopressin induces gluconeogenesis in the rat liver and transiently increases glycemia in healthy humans and because vasopressin receptors are expressed in hepatocytes and pancreatic islets (2–9).”
From Low Water Intake and Risk for New-Onset Hyperglycemia (2011) · cites this paper as [7]
A causal link between vasopressin and glucose homeostasis is plausible.
“A causal link between vasopressin and glucose homeostasis is plausible because vasopressin induces gluconeogenesis in the rat liver and transiently increases glycemia in healthy humans and because vasopressin receptors are expressed in hepatocytes and pancreatic islets (2–9).”
From Low Water Intake and Risk for New-Onset Hyperglycemia (2011) · cites this paper as [7]
Vasopressin receptors are expressed in hepatocytes and pancreatic islets.
“A causal link between vasopressin and glucose homeostasis is plausible because vasopressin induces gluconeogenesis in the rat liver and transiently increases glycemia in healthy humans and because vasopressin receptors are expressed in hepatocytes and pancreatic islets (2–9).”
From Low Water Intake and Risk for New-Onset Hyperglycemia (2011) · cites this paper as [7]
Vasopressin induces gluconeogenesis in the rat liver.
“A causal link between vasopressin and glucose homeostasis is plausible because vasopressin induces gluconeogenesis in the rat liver and transiently increases glycemia in healthy humans and because vasopressin receptors are expressed in hepatocytes and pancreatic islets (2–9).”
From Low Water Intake and Risk for New-Onset Hyperglycemia (2011) · cites this paper as [7]
Cites
Still being checked.
Cited by
Sorted by citations
Gal, C. S., Lacour, C., Valette, G., Garcia, G., Foulon, L., Galindo, G., Bankir, L., Pouzet, B., Guillon, G., Barberis, C., et al. (1996) · Journal of Clinical Investigation · doi:10.1172/jci119098 · Cited by 249 · see citing works
Self-citationVasopressin: a novel target for the prevention and retardation of kidney disease?
Bankir, L., Bouby, N., & Ritz, E. (2013) · Nature Reviews Nephrology · doi:10.1038/nrneph.2013.22 · Cited by 214 · see citing works
Low Water Intake and Risk for New-Onset Hyperglycemia
Roussel, R., Fezeu, L., Bouby, N., Balkau, B., Lantieri, O., Alhenc-Gelas, F., Marre, M., Bankir, L., & for the D.E.S.I.R. Study Group (2011) · Diabetes Care · doi:10.2337/dc11-0652 · Cited by 165 · see citing works
Bardoux, P., Martin, H., Ahloulay, M., Schmitt, F., Bouby, N., Trinh-Trang-Tan, M.-M., & Bankir, L. (1999) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.96.18.10397 · Cited by 138 · see citing works
Molecular neurobiology and pharmacology of the Vasopressin/Oxytocin receptor family
Burbach, J. P. H., Burbach, H., Adan, R. A. H., Lolait, S. J., van Leeuwen, F. W., Mezey, É., Palkovits, M., & Barberis, C. (1995) · Cellular and Molecular Neurobiology · doi:10.1007/bf02071318 · Cited by 118 · see citing works
Neurohypophyseal hormones manipulation modulate social and anxiety-related behavior in zebrafish
Braida, D., Donzelli, A., Martucci, R., Capurro, V., Busnelli, M., Chini, B., & Sala, M. (2011) · Psychopharmacology · doi:10.1007/s00213-011-2482-2 · Cited by 116 · see citing works
SR120819A, an orally‐active and selective neuropeptide Y Y1 receptor antagonist
Gal, C. S., Valette, G., Rouby, P.-E., Pellet, A., Oury-Donat, F., Brossard, G., Lespy, L., Marty, E., Neliat, G., COINTET, P. D., et al. (1995) · FEBS Letters · doi:10.1016/0014-5793(95)00230-7 · Cited by 113 · see citing works
Self-citationTribollet, E., Raufaste, D., Maffrand, J., & Gal, C. S. (1999) · Neuroendocrinology · doi:10.1159/000054409 · Cited by 66 · see citing works
Self-citationArginine vasopressin receptor 1a is a therapeutic target for castration-resistant prostate cancer
Zhao, N., Peacock, S. O., Lo, C. H., Heidman, L. M., Rice, M. A., Fahrenholtz, C. D., Greene, A. M., Magani, F., Copello, V. A., Martinez, M. J., et al. (2019) · Science Translational Medicine · doi:10.1126/scitranslmed.aaw4636 · Cited by 64 · see citing works
Molecular pharmacology of V1a vasopressin receptors
Howl, J., & Wheatley, M. (1995) · General Pharmacology The Vascular System · doi:10.1016/0306-3623(95)00016-t · Cited by 58 · see citing works
Structural modifications of glycopeptide antibiotics
Malabarba, A., Nicas, T. I., & Thompson, R. C. (1997) · Medicinal Research Reviews · doi:10.1002/(sici)1098-1128(199701)17:1 · Cited by 140 · see citing works
Chapter 1.4 Vasopressin binding sites in the central nervous system: Distribution and regulation
Tribollet, E., Arsenijévic, Y., & Barberis, C. (1999) · Progress in brain research · doi:10.1016/s0079-6123(08)61561-7 · Cited by 37 · see citing works
Autoradiographic localization of vasopressin V1a receptors in the rat kidney using [3H]-SR 49059
Gal, C. S., Raufaste, D., Marty, E., Garcia, C., Maffrand, J., & Fur, G. L. (1996) · Kidney International · doi:10.1038/ki.1996.341 · Cited by 36 · see citing works
Self-citationGal, C. S.-L., Raufaste, D., Derick, S., Blankenstein, J., Allen, J., Pouzet, B., Pascal, M., Wagnon, J., & Ventura, M. A. (2007) · American Journal of Physiology-Regulatory, Integrative and Comparative Physiology · doi:10.1152/ajpregu.00062.2007 · Cited by 35 · see citing works
Self-citationHowl, J., & Wheatley, M. (1996) · Biochemical Journal · doi:10.1042/bj3170577 · Cited by 34 · see citing works
Failure is an option: learning from unsuccessful proof-of-concept trials
Schäfer, S., & Kolkhof, P. (2008) · Drug Discovery Today · doi:10.1016/j.drudis.2008.03.026 · Cited by 31 · see citing works
Binding properties of a selective tritiated vasopressin V2 receptor antagonist, [3H]-SR 121463
Gal, C. S., Raufaste, D., Double-Cazanave, E., Guillon, G., Garcia, C., Pascal, M., & Maffrand, J. P. (2000) · Kidney International · doi:10.1046/j.1523-1755.2000.00322.x · Cited by 25 · see citing works
Self-citationBax, W. A., der Graaf, P. H. V., Stam, W. B., Bos, E., Nisato, D., & Saxena, P. R. (1995) · European Journal of Pharmacology · doi:10.1016/0014-2999(95)00503-d · Cited by 25 · see citing works
Stam, W. B., der Graaf, P. H. V., & Saxena, P. R. (1998) · British Journal of Pharmacology · doi:10.1038/sj.bjp.0702149 · Cited by 23 · see citing works
Hyponatremia and Cancer: From Bedside to Benchside
Fibbi, B., Marroncini, G., Naldi, L., Anceschi, C., Errico, A., Norello, D., & Peri, A. (2023) · Cancers · doi:10.3390/cancers15041197 · Cited by 21 · see citing works
Braida, D., Donzelli, A., Martucci, R., Ponzoni, L., Pauletti, A., & Sala, M. (2012) · Peptides · doi:10.1016/j.peptides.2012.07.013 · Cited by 19 · see citing works
Bossmar, T., Rasmussen, T., & Åkerlund, M. (1996) · Acta Obstetricia Et Gynecologica Scandinavica · doi:10.3109/00016349609054663 · Cited by 13 · see citing works
Kerckhoven, R. V., Lankhuizen, I. M., van Veghel, R., Saxena, P. R., & Schoemaker, R. G. (2002) · European Journal of Pharmacology · doi:10.1016/s0014-2999(02)01972-6 · Cited by 11 · see citing works
Vasopressin and oxytocin receptors (version 2019.4) in the IUPHAR/BPS Guide to Pharmacology Database
Bichet, D. G., Bouvier, M., Chini, B., Gimpl, G., Guillon, G., Kimura, T., Knepper, M. A., Lolait, S. J., Manning, M., Mouillac, B., et al. (2019) · IUPHAR/BPS Guide to Pharmacology CITE · doi:10.2218/gtopdb/f66/2019.4 · Cited by 8 · see citing works
Recent discovery and development of non-peptide vasopressin V2receptor agonists
Kondo, K. (2002) · Expert Opinion on Therapeutic Patents · doi:10.1517/13543776.12.8.1249 · Cited by 6 · see citing works
Pharmacological characterization of a vasopressin V1 receptor in the isolated human gastric artery
Calò, G., Rizzi, A., Traina, L., & Regoli, D. C. (1996) · Life Sciences · doi:10.1016/s0024-3205(96)00635-2 · Cited by 6 · see citing works
Lankhuizen, I. M., van Veghel, R., Saxena, P. R., & Schoemaker, R. G. (2001) · European Journal of Pharmacology · doi:10.1016/s0014-2999(01)01092-5 · Cited by 5 · see citing works
Lankhuizen, I. M., van Veghel, R., Saxena, P. R., & Schoemaker, R. G. (2000) · Journal of Cardiovascular Pharmacology · doi:10.1097/00005344-200007000-00005 · Cited by 5 · see citing works
Grélot, L., Girod, V., Dapzol, J., Maffrand, J. P., & Gal, C. S. (2001) · Fundamental and Clinical Pharmacology · doi:10.1046/j.1472-8206.2001.00027.x · Cited by 3 · see citing works
Self-citationSR 120819A or the first Generation of orally active Y1-receptor antagonists
Gal, C. S. (1997) · Elsevier eBooks · doi:10.1016/b978-012304990-2/50009-3 · Cited by 3 · see citing works
Vasopressin and oxytocin receptors in GtoPdb v.2023.1
Bichet, D. G., Bouvier, M., Chini, B., Gimpl, G., Guillon, G., Kimura, T., Knepper, M. A., Lolait, S. J., Manning, M., Mouillac, B., et al. (2023) · IUPHAR/BPS Guide to Pharmacology CITE · doi:10.2218/gtopdb/f66/2023.1 · Cited by 2 · see citing works
Naldi, L., Fibbi, B., Marroncini, G., Norello, D., & Peri, A. (2025) · Best Practice & Research Clinical Endocrinology & Metabolism · doi:10.1016/j.beem.2025.102066 · Cited by 1 · see citing works
Vogel, H. G. (2007) · Springer eBooks · doi:10.1007/978-3-540-70995-4_15 · Cited by 1 · see citing works
(1995) · British Journal of Pharmacology · doi:10.1111/j.1476-5381.1995.tb16306.x · Cited by 1 · see citing works
Discovery of Nonpeptide Vasopressin V2 Receptor Antagonists
Kondo, K., & Ogawa, H. (2012) · doi:10.1002/9783527651085.ch8
Sandow, J. (2015) · Springer eBooks · doi:10.1007/978-3-319-05392-9_82
Autoradiographic localization of vasopressin Via receptors in the rat kidney using (3HJ-SR 49059
Gal, C. S., Raufaste, D., Marty, E., & Garcia, C. (1996)
Self-citationVogel, H. G., Vogel, W. H., Schölkens, B. A., Sandow, J., Müller, G. A., & Vogel, W. F. (2002) · Springer eBooks · doi:10.1007/3-540-29837-1_15
(1996) · British Journal of Pharmacology · doi:10.1111/j.1476-5381.1996.tb17246.x
Barberis, C. (2007) · xPharm: The Comprehensive Pharmacology Reference · doi:10.1016/b978-008055232-3.62671-6
- Authors
- Serradeillegal, C., Raufaste, D., Marty, E., Garcia, C., Maffrand, J. P., & Lefur, G.
- Affiliations
- Sanofi (France) (FR)
- Venue
- Biochemical and Biophysical Research Communications
- Publisher
- Elsevier BV
- Published
- 1994-02
- Volume
- 199
- Issue
- 1
- Pages
- 353-360
- ISSN
- 0006-291X (ISSN-L)
- OpenAlex
- W1995247367
- Cited by
- 40
- References
- 0
- Citations by year
- 2025: 1 · 2023: 2 · 2019: 2 · 2015: 1 · 2013: 1 · 2012: 2
- FWCI
- 9.17
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Biochemical and Biophysical Research Communications (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Social Sciences › Psychology › Social Psychology › Neuroendocrine regulation and behavior
- Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Neuropeptides and Animal Physiology
- Health Sciences › Medicine › Surgery › Cardiovascular, Neuropeptides, and Oxidative Stress Research
- Keywords
- vasopressin V1a receptor, non-peptide antagonists, radioligand binding, liver membranes, receptor binding affinity, species differences, OPC-21268, oxytocin receptor
- MeSH terms
- Animals, Arginine Vasopressin, Binding, Competitive, Cell Membrane, Humans, Indoles, Kinetics, Liver, Male, Pyrrolidines, Rats, Sprague-Dawley, Receptors, Vasopressin, Rats
About these checks
Registry, retraction, Cites and statistics results are computed, not judged, with one exception: a printed reference that no index lists is read once by a model before it counts as a citation error. Claims are extracted by a model and kept only when their quote appears verbatim in the text; each cited source is then checked, with a model’s help, for whether it says what the claim relies on. Those verdicts can be wrong — read the claim’s quote and the cited source before relying on one.
Statistics and arithmetic are recomputed, not judged.
Confidence bands are shown only for fields calibrated on our annotated test set. None is calibrated yet, so no band is shown.
What counts as a claim ›How we measure confidence ›How we check this ›
Are you an author, or do you see a problem with this page? Request a review
