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5. Biological characterization of rodent and human vasopressin [V.sub.1b] receptors using SSR-149415, a nonpeptide [V.sub.1b] receptor ligand

Author

Gal, Claudine Serradeil-Le, Raufaste, Daniele, Derick, Sylvain, Blankenstein, Jorg, Allen, John, Pouzet, Brigitte, Pascal, Marc, Wagnon, Jean, and Ventura, Maria Angeles

Subjects
Vasopressin -- Identification and classification, Rodents -- Physiological aspects, Rodents -- Comparative analysis, Human beings -- Physiological aspects, Human beings -- Comparative analysis, Man -- Physiological aspects, Man -- Comparative analysis, Ligands (Biochemistry) -- Usage, Biological sciences
Abstract

[[sup.3]H]SSR--149415 is the first tritiated nonpeptide vasopressin [V.sub.1b] receptor ([V.sub.1b]R) antagonist ligand. It was used for studying rodent (mouse, rat, hamster) and human [V.sub.1b]R from native or recombinant origin. Moreover, a close comparison between the human and the mouse [V.sub.1b]R was performed using SSR-149415/[[3.sup.H]]SSR-149415 in binding and functional studies in vitro. [[sup]H]SSR-149415 binding was time-dependent, reversible, and saturable. Scatchard plot analysis gave a single class of high-affinity binding sites with apparent equilibrium dissociation constant ([K.sub.d]) ~1 nM and maximum binding density ([B.sub.max]) values from 7,000 to 300,000 sites/cell according to the cell line. In competition experiments, [[sup.3]H]SSR-149415 binding was stereospecific and dose-dependently displaced by reference peptide and nonpeptide arginine vasopressin (AVP)/OT ligands following a [V.sub.1b] rank order of affinity: SSR-149415 = AVP > dCha > dPen > dPal > dDavp > SSR126768A > SR-49059 > SSR-149424 > OT > SR-121463B. Species differences between human, rat, mouse, and hamster [V.sub.lb]R were observed. Autoradiography studies with [[sup.3]H]SSR-149415 on rat and human pituitary showed intense specific labeling confined to cortico-troph cells and absence of labeling in the other tissues examined. SSR-149415 potently and stereospecifically antagonized the AVP-induced inositol phosphate production and intracellular [Ca.sup.2+] increase ([EC.sub.50] from 1.83 to 3.05 nM) in recombinant cell lines expressing either the mouse or the human [V.ub.1b]R. AVP ([10.sup.-7] M) exposure of AtT20 cells expressing mouse or human EGFP-tagged [V.sub.1b]R induced their rapid internalization. Preincubation with [10.sup.-6] M SSR-149415 counteracted the internalization process. Moreover, recycling of internalized receptors was observed upon [10.sup.-6] M SSR-149415 treatment. Thus SSR-149415/[[sup.3]H]SSR-149415 are unique tools for studying animal and human [V.sub1b]R. vasopressin; [V.sub.1b] receptor; rat; hamster; mouse; human

Published
2007

10. Development of new biosensors to detect ciguatoxins

Author

Yken, Helene, Derick, Sylvain, Gironde, Camille, Darius, Hélène Taiana, Furger, Christophe, Laurent, Dominique, François, Jean-Marie, Chinain, Mireille, ProdInra, Archive Ouverte, Priority environmental contaminants in seafood: safety assessment, impact and public perception - 311820 - INCOMING, Laboratoire d'Ingénierie des Systèmes Biologiques et des Procédés (LISBP), Institut National de la Recherche Agronomique (INRA)-Institut National des Sciences Appliquées - Toulouse (INSA Toulouse), Institut National des Sciences Appliquées (INSA)-Université Fédérale Toulouse Midi-Pyrénées-Institut National des Sciences Appliquées (INSA)-Université Fédérale Toulouse Midi-Pyrénées-Centre National de la Recherche Scientifique (CNRS), Équipe Micro et nanosystèmes HyperFréquences Fluidiques (LAAS-MH2F), Laboratoire d'analyse et d'architecture des systèmes (LAAS), Université Toulouse Capitole (UT Capitole), Université Fédérale Toulouse Midi-Pyrénées-Université Fédérale Toulouse Midi-Pyrénées-Institut National des Sciences Appliquées - Toulouse (INSA Toulouse), Institut National des Sciences Appliquées (INSA)-Université Fédérale Toulouse Midi-Pyrénées-Institut National des Sciences Appliquées (INSA)-Université Toulouse - Jean Jaurès (UT2J)-Université Toulouse III - Paul Sabatier (UT3), Université Fédérale Toulouse Midi-Pyrénées-Centre National de la Recherche Scientifique (CNRS)-Institut National Polytechnique (Toulouse) (Toulouse INP), Université Fédérale Toulouse Midi-Pyrénées-Université Toulouse Capitole (UT Capitole), Université Fédérale Toulouse Midi-Pyrénées, LED Engineering Development, Institut Louis Malardé [Papeete] (ILM), Institut de Recherche pour le Développement (IRD), Pharmacochimie et Biologie pour le Développement (PHARMA-DEV), Institut de Recherche pour le Développement (IRD)-Institut de Chimie de Toulouse (ICT-FR 2599), Institut de Recherche pour le Développement (IRD)-Université Toulouse III - Paul Sabatier (UT3), Université Fédérale Toulouse Midi-Pyrénées-Université Fédérale Toulouse Midi-Pyrénées-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS)-Institut National Polytechnique (Toulouse) (Toulouse INP), Université Fédérale Toulouse Midi-Pyrénées-Institut de Recherche pour le Développement (IRD)-Université Toulouse III - Paul Sabatier (UT3), 'OcéaSafe', PEPs CNRS, 2016., European Project: 311820, Institut National des Sciences Appliquées (INSA)-Institut National des Sciences Appliquées (INSA)-Centre National de la Recherche Scientifique (CNRS), LAAS-2I, Institut National Polytechnique (Toulouse) (Toulouse INP), Institut National des Sciences Appliquées (INSA)-Institut National des Sciences Appliquées (INSA)-Université Toulouse III - Paul Sabatier (UT3), Université Fédérale Toulouse Midi-Pyrénées-Centre National de la Recherche Scientifique (CNRS)-Université Toulouse 1 Capitole (UT1)-Université Toulouse - Jean Jaurès (UT2J)-Institut National Polytechnique (Toulouse) (Toulouse INP), Université Fédérale Toulouse Midi-Pyrénées-Centre National de la Recherche Scientifique (CNRS)-Université Toulouse 1 Capitole (UT1)-Université Toulouse - Jean Jaurès (UT2J), Méiose et reproduction : génétique moléculaire, physiologie, pathologies, applications (MRGMPPA), Institut National de la Recherche Agronomique (INRA)-Université Paris-Sud - Paris 11 (UP11)-Université Nice Sophia Antipolis (... - 2019) (UNS), COMUE Université Côte d'Azur (2015 - 2019) (COMUE UCA)-COMUE Université Côte d'Azur (2015 - 2019) (COMUE UCA)-Assistance publique - Hôpitaux de Paris (AP-HP) (AP-HP)-Université Paris Descartes - Paris 5 (UPD5)-Institut National de la Santé et de la Recherche Médicale (INSERM)-Centre National de la Recherche Scientifique (CNRS), Université Toulouse III - Paul Sabatier (UT3), Institut de Recherche pour le Développement (IRD [Polynésie]), Université Fédérale Toulouse Midi-Pyrénées-Université Fédérale Toulouse Midi-Pyrénées-Centre National de la Recherche Scientifique (CNRS)-Institut National Polytechnique (Toulouse) (Toulouse INP), Centre National de la Recherche Scientifique (CNRS)-Institut National des Sciences Appliquées - Toulouse (INSA Toulouse), Institut National des Sciences Appliquées (INSA)-Institut National des Sciences Appliquées (INSA)-Institut National de la Recherche Agronomique (INRA), Université Toulouse - Jean Jaurès (UT2J)-Université Toulouse 1 Capitole (UT1), Université Fédérale Toulouse Midi-Pyrénées-Université Fédérale Toulouse Midi-Pyrénées-Centre National de la Recherche Scientifique (CNRS)-Université Toulouse III - Paul Sabatier (UT3), Université Fédérale Toulouse Midi-Pyrénées-Institut National des Sciences Appliquées - Toulouse (INSA Toulouse), Institut National des Sciences Appliquées (INSA)-Institut National des Sciences Appliquées (INSA)-Institut National Polytechnique (Toulouse) (Toulouse INP), Université Fédérale Toulouse Midi-Pyrénées-Université Toulouse - Jean Jaurès (UT2J)-Université Toulouse 1 Capitole (UT1), Université Fédérale Toulouse Midi-Pyrénées-Université Fédérale Toulouse Midi-Pyrénées-Centre National de la Recherche Scientifique (CNRS)-Institut de Recherche pour le Développement (IRD)-Université Toulouse III - Paul Sabatier (UT3), Université Fédérale Toulouse Midi-Pyrénées-Institut de Chimie du CNRS (INC)-Institut National Polytechnique (Toulouse) (Toulouse INP), Université Fédérale Toulouse Midi-Pyrénées-Institut de Chimie du CNRS (INC), Université Fédérale Toulouse Midi-Pyrénées-Université Fédérale Toulouse Midi-Pyrénées-Institut de Recherche pour le Développement (IRD)-Université Toulouse III - Paul Sabatier (UT3), Université Fédérale Toulouse Midi-Pyrénées-Centre National de la Recherche Scientifique (CNRS), Université Fédérale Toulouse Midi-Pyrénées-Université Fédérale Toulouse Midi-Pyrénées-Institut de Chimie de Toulouse (ICT-FR 2599), Université Fédérale Toulouse Midi-Pyrénées-Centre National de la Recherche Scientifique (CNRS)-Institut de Recherche pour le Développement (IRD)-Institut de Chimie du CNRS (INC)-Institut de Recherche pour le Développement (IRD), Institut National des Sciences Appliquées (INSA)-Université de Toulouse (UT)-Institut National des Sciences Appliquées (INSA)-Université de Toulouse (UT)-Centre National de la Recherche Scientifique (CNRS), Université de Toulouse (UT)-Université de Toulouse (UT)-Institut National des Sciences Appliquées - Toulouse (INSA Toulouse), Institut National des Sciences Appliquées (INSA)-Université de Toulouse (UT)-Institut National des Sciences Appliquées (INSA)-Université Toulouse - Jean Jaurès (UT2J), Université de Toulouse (UT)-Université Toulouse III - Paul Sabatier (UT3), Université de Toulouse (UT)-Centre National de la Recherche Scientifique (CNRS)-Institut National Polytechnique (Toulouse) (Toulouse INP), Université de Toulouse (UT)-Université Toulouse Capitole (UT Capitole), Université de Toulouse (UT), Institut de Recherche pour le Développement (IRD)-Institut de Chimie de Toulouse (ICT), Université de Toulouse (UT)-Université de Toulouse (UT)-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS)-Institut National Polytechnique (Toulouse) (Toulouse INP), and Université de Toulouse (UT)-Institut de Recherche pour le Développement (IRD)-Université Toulouse III - Paul Sabatier (UT3)

Subjects
[SDV.BIO]Life Sciences [q-bio]/Biotechnology, [SPI.GPROC] Engineering Sciences [physics]/Chemical and Process Engineering, [SDV]Life Sciences [q-bio], [SDE.MCG]Environmental Sciences/Global Changes, sensory neuron, Biotechnologies, yeast, brewer s, Ciguatoxins, intoxication, saccharomyces cerevisiae, [SPI.GPROC]Engineering Sciences [physics]/Chemical and Process Engineering, 14. Life underwater, biosenseur, Génie des procédés, micro-algue, CIguatera, biosensors, [SDV.BIO] Life Sciences [q-bio]/Biotechnology, poisoning, Detection, Process Engineering, environment, marine toxins, [SDV.TOX]Life Sciences [q-bio]/Toxicology, [SDE]Environmental Sciences, fruit de mer, neurone sensoriel, [SDV.AEN]Life Sciences [q-bio]/Food and Nutrition
Abstract

International audience; Ciguatoxins are lipid-soluble polyether compounds produced by dinoflagellates from the genus Gambierdiscus spp.. Ciguatoxins are mostly found in tropical and subtropical zones; however, within the last decade, they have been identified in fishes caught in European waters, notably in Madeira (1) and Canary Islands (2), while Gambierdiscus spp. have also been found both in the NE Atlantic Ocean (3) and in the Mediterranean Sea (4). These toxins bind to Voltage Gated Sodium Channels at the surface of human sensory neurons where they remain, causing Ciguatera Fish Poisoning with a variety of gastrointestinal, cardiovascular and neurological symptoms (paresthesia, ataxia, cold allodynia), including persistent neurological effects. Ciguatera is the major cause of food poisonings by seafood worldwide, with an estimated 50 000 to 500 000 victims per year. However, there is so far no simple and quick way of detecting these toxins in contaminated samples. Currently, only heavy and expensive laboratory methods are available to detect them: LC-MS/MS, receptor-binding assays by competition with radiolabeled compounds, and neuroblastoma cell-based assays performed on mammalian neurons (5). We have started to engineer biosensors based on the detection of a transcriptional signal in the yeast model Saccharomyces cerevisiae. This unicellular eukaryotic model is well-known and easy to genetically modify, grows fast and presents a very good conservation of signaling pathways with higher eukaryotes. We present a series of genetically modified yeast strains which allow us to follow the activation of specific signaling pathways responding linearly to ciguatoxin exposure. This pre-exploratory project received a seed-funding by CNRS (PEPs project, Océasafe). References : 1 Otero et al., Anal. Chem. 2010, 82, 6032 2 Nuñez et al., 2012. Euro Surveill. 17, 20188 3 Fraga et Rodriguez, 2014 Protist 165, 839 4 Aligizaki et Nikolaidis, 2008. J. Biol. Res. Thessalon 9, 75. 5 Caillaud et al., 2010 Mar. Drugs. 8, 1838

Published
2017
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16. Position 4 analogues of [deamino-Cys1] arginine vasopressin exhibit striking species differences for human and rat V2/V1b receptor selectivity

Author

Guillon, Gilles, primary, Pena, Ana, additional, Murat, Brigitte, additional, Derick, Sylvain, additional, Trueba, Miguel, additional, Ventura, Maria A., additional, Szeto, Hazel H., additional, Wo, Nga, additional, Stoev, Stoytcho, additional, Cheng, Ling Ling, additional, and Manning, Maurice, additional

Published
2006
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18. Comparative cytotoxicity induced by bulk and nanoparticulated ZnO in the fish and human hepatoma cell lines PLHC-1 and Hep G2.

Author

Fernández-Cruz, Maria Luisa, Lammel, Tobias, Connolly, Mona, Conde, Estefania, Barrado, Ana Isabel, Derick, Sylvain, Perez, Yolanda, Fernandez, Marta, Furger, Christophe, and Navas, Jose Maria

Subjects
NANOPARTICLES analysis, HEPATOCELLULAR carcinoma, CELL lines, TOXICITY testing, BIOCHEMICAL mechanism of action, LIVER tumors, CELL culture, PREVENTION, PHYSIOLOGY
Abstract

The increasing presence of ZnO nanoparticles (NPs) in consumer products may be having a dramatic impact in aquatic environments. The evaluation of ZnO NP toxicity represents a great challenge. This study aimed at evaluating the cytotoxic effect of micro- and nanosized ZnO in a fish and a mammalian hepatoma cell line. A detailed characterisation of the particles in exposure media showed that ZnO NPs formed large aggregates. ZnO cytotoxicity was evaluated with a battery of in vitro assays including LUCS, a new approach based on DNA alteration measurements. In fish cells, ZnO NP aggregates contributed substantially to the cytotoxic effects whereas toxicity in the human cells appeared to be mainly produced by the dissolved fraction. ROS production did not contribute to the observed cytotoxicity. This work also showed that measuring concentrations of NPs is essential to understand the mechanisms underlying their toxicity. [ABSTRACT FROM AUTHOR]

Published
2013
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19. Biological characterization of rodent and human vasopressin V1b receptors using SSR-149415, a nonpeptide V1b receptor ligand.

Author

Serradeil-Le Gal, Claudine, Raufaste, Danièle, Derick, Sylvain, Blankenstein, Jörg, Allen, John, Pouzet, Brigitte, Pascal, Marc, Wagnon, Jean, and Ventura, Maria Angeles

Subjects
VASOPRESSIN, LABORATORY rodents, LIGANDS (Biochemistry), BINDING sites, ARGININE
Abstract

[³H]SSR-1494 15 is the first tritiated nonpeptide vasopressin V1b receptor (V1bR) antagonist Iigand. It was used for studying rodent (mouse, rat, hamster) and human V1bR from native or recombinant origin. Moreover, a close comparison between the human and the mouse V1bR was performed using SSR-149415/[³H]SSR-149415 in binding and functional studies in vitro. [³H]SSR-149415 binding was time-dependent, reversible, and saturable. Scatchard plot analysis gave a single class of high-affinity binding sites with apparent equilibrium dissociation constant (Kd) ~1 nM and maximum binding density (Bmax) values from 7,000 to 300,000 sites/cell according to the cell line. In competition experiments, [³H]SSR-149415 binding was stereospecific and dose-dependently displaced by reference peptide and nonpeptide arginine vasopressin (AVP)/OT ligands following a V1b rank order of affinity: SSR-149415 = AVP > dCha > dPen > dPal > dDavp > SSR-126768A > SR-49059 > SSR-149424 > OT > SR-121463B. Species differences between human, rat, mouse, and hamster V1bR were observed. Autoradiography studies with [³H]SSR-149415 on rat and human pituitary showed intense specific labeling confined to corticotroph cells and absence of labeling in the other tissues examined. SSR-149415 potently and stereospecifically antagonized the AVP-induced inositol phosphate production and intracellular Ca2+ increase (EC50 from 1.83 to 3.05 nM) in recombinant cell lines expressing either the mouse or the human V1bR. AVP (10-7 M) exposure of AtT20 cells expressing mouse or human EGFP-tagged V1bR induced their rapid internalization. Preincubation with 10-6 M SSR-149415 counteracted the internalization process. Moreover, recycling of internalized receptors was observed upon 10-6 M SSR-149415 treatment. Thus SSR-149415/[³H]SSR-149415 are unique tools for studying animal and human V1bR. [ABSTRACT FROM AUTHOR]

Published
2007
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20. Position 4 analogues of [deamino-Cys1] arginine vasopressin exhibit striking species differences for human and rat V2/V1b receptor selectivity.

Author

Guillon, Gilles, Pena, Ana, Murat, Brigitte, Derick, Sylvain, Trueba, Miguel, Ventura, Maria A., Szeto, Hazel H., Wo, Nga, Stoev, Stoytcho, Cheng, Ling Ling, and Manning, Maurice

Abstract

Copyright of Journal of Peptide Science is the property of Wiley-Blackwell and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

Published
2006
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22. Functional and pharmacological characterization of the first specific agonist and antagonist for the V1b receptor in mammals.

Author

Serradeil-Le Gal C, Derick S, Brossard G, Manning M, Simiand J, Gaillard R, Griebel G, and Guillon G

Subjects
Animals, Humans, Antidiuretic Hormone Receptor Antagonists, Arginine Vasopressin analogs & derivatives, Arginine Vasopressin pharmacology, Indoles pharmacology, Pyrrolidines pharmacology, Receptors, Vasopressin agonists
Abstract

By activating three distinct vasopressin receptor isoforms called V1a-R, V1b-R (V3-R) and V2-R, vasopressin (VP) mediates a wide number of biological effects in mammals and may be involved in several pathological states. Up to now only specific V1a and V2 receptor agonists and antagonists have been successfully designed. The role of the V1b-R still remains partially unknown, due to the lack of selective V1b-R ligands and orally-active molecules, which are crucial tools for investigating the central and peripheral functions or pathological disorders associated with this receptor. In this review, we report the biological and pharmacological properties of the first two specific V1b-R ligands: d[Cha4] AVP, a high affinity V1b-R agonist and SSR149415, a potent orally-active V1b-R antagonist with good selectivity with respect to other VP/OT receptor isoforms and able to control ACTH secretion in vitro and in vivo. Indeed, these molecules constitute invaluable tools for exploring the central and peripheral roles of VP mediated via V1b receptors. Interestingly, SSR149415 displays potent anxiolytic and antidepressant-like activities, indicating that this new class of drugs has a promising therapeutical potential in the treatment of stress-related disorders, anxiety and depression.

Published
2003
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