Neurotensin is an antagonist of the human neurotensin NT2 receptor expressed in Chinese hamster ovary cells

European Journal of Pharmacology

Volumn 360, Issue 2-3, 1998, Pages 265-272

  Vita, Natalio ^a   Oury Donat, Florence ^a   Chalon, Pascale ^a   Guillemot, Marie ^a   Kaghad, Mourad ^a   Bachy, André ^a   Thurneyssen, Olivier ^a   Garcia, Stéphanie ^a   Poinot Chazel, Caroline ^a   Casellas, Pierre ^a   Keane, Peter ^a   Le Fur, Gérard ^a   Maffrand, Jean P ^a   Soubrie, Philippe ^a   Caput, Daniel ^a   Ferrara, Pascual ^a  

^a SANOFI   (France)

Author keywords

G protein; Levocabastine; Neurotensin; Receptor; SR142948A; SR48692

Indexed keywords

2 [5 (2,6 DIMETHOXYPHENYL) 1 [4 [N (3 DIMETHYLAMINOPROPYL) N METHYLCARBAMOYL] 2 ISOPROPYLPHENYL] 1H PYRAZOL 3 YLCARBONYLAMINO]ADAMANTANE 2 CARBOXYLIC ACID; 2 [[1 (7 CHLORO 4 QUINOLINYL) 5 (2,6 DIMETHOXYPHENYL) 3 PYRAZOLYL]CARBONYLAMINO] 2 ADAMANTANECARBOXYLIC ACID; ARACHIDONIC ACID; CALCIUM ION; HISTAMINE H1 RECEPTOR ANTAGONIST; INOSITOL PHOSPHATE; LEVOCABASTINE; LIGAND; MITOGEN ACTIVATED PROTEIN KINASE; NEUROMEDIN N; NEUROTENSIN; NEUROTENSIN RECEPTOR; RECEPTOR SUBTYPE; UNCLASSIFIED DRUG; XENIN;

ARTICLE; CALCIUM MOBILIZATION; CHO CELL; CONCENTRATION RESPONSE; CONTROLLED STUDY; DNA LIBRARY; ENZYME ACTIVITY; FEMALE; HUMAN CELL; MOLECULAR CLONING; NONHUMAN; PRIORITY JOURNAL; PROTEIN EXPRESSION; RECEPTOR BINDING; SECOND MESSENGER; SIGNAL TRANSDUCTION;

AMINO ACID SEQUENCE; ANIMALS; CHO CELLS; CLONING, MOLECULAR; CRICETINAE; DNA, COMPLEMENTARY; HUMANS; MOLECULAR SEQUENCE DATA; NEUROTENSIN; RECEPTORS, NEUROTENSIN; RECOMBINANT PROTEINS; RNA, MESSENGER; SEQUENCE HOMOLOGY, AMINO ACID; SIGNAL TRANSDUCTION; TISSUE DISTRIBUTION;

EID: 18144433363     PISSN: 00142999     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0014-2999(98)00678-5     Document Type: Article

References (27)

1. Amar S., Kitabgi P., Vincent J.P. Activation of phosphatidylinositol turnover by neurotensin receptors in the human colonic adenocarcinoma cell line HT29. FEBS Lett. 201:1986;31-36.
2. Aviv H., Leder P. Purification of biologically active globin messenger RNA by chromatography on oligothymidylic acid-cellulose. Proc. Natl. Acad. Sci. USA. 69:1972;1408-1411.
3. Botto J.-M., Guillemare E., Vincent J.P., Mazella J. Effects of SR48692 on neurotensin-induced calcium-activated chloride currents in the Xenopus oocyte expression system: agonist-like activity on the levocabastine-sensitive neurotensin receptor and absence of antagonist effect on the levocabastine insensitive neurotensin receptor. Neurosci. Lett. 223:1997;193-196.
4. Botto J.M., Chabry J., Sarret P., Vincent J.P., Mazella J. Stable expression of the mouse levocabastine-sensitive neurotensin receptor in HEK-293 cell line: binding properties, photoaffinity labelling and internalisation. Biochem. Biophys. Res. Commun. 243:1998;585-590.
5. Carraway R., Leeman S.E. The isolation of a new hypotensive peptide, neurotensin, from bovine hypothalami. J. Biol. Chem. 248:1973;6854-6861.
6. Carraway R., Ruane S.E., Kim H.R. Distribution and immunochemical characterisation of neurotensin-like material in representative vertebrates and invertebrates: apparent conservation of the COOH-terminal region during evolution. Peptides. 3:1982;115-123.
7. Chalon P., Vita N., Kaghad M., Guillemot M., Bonnin J., Delpech B., Le Fur G., Ferrara P., Caput D. Molecular cloning of a levocabastine-sensitive neurotensin binding site. FEBS Lett. 386:1996;91-94.
8. Chomczynski P., Sacchi N. Single-step method of RNA isolation by acid guanidinium thiocyanate-phenol-chloroform extraction. Anal. Biochem. 162:1987;156-159.
9. Donaldson C.J., Sutton S.W., Perrin M.H., Corrigan A.Z., Lewis K.A., Rivier J.E., Vaughan J.M., Vale W.W. Cloning and characterisation of human urocortin. Endocrinology. 137:1996;2167-2170.
10. Dubuc I., Costentin J., Terranova J.P., Barnouin M.C., Soubrie P., Le Fur G., Rostene W., Kitabgi P. The non-peptide neurotensin antagonist, SR48692 used as a tool to reveal putative neurotensin receptor subtypes. Br. J. Pharmacol. 112:1994;352-354.
11. 2+ indicators with greatly improved fluorescence properties. J. Biol. Chem. 260:1985;3440-3450.
12. Gully D., Canton M., Boigegrain R., Jeanjean F., Molimard J.C., Poncelet M., Gueudet Ch., Heaulme M., Leyris R., Brouard A., Pelaprat D., Labbé-Jullié C., Mazella J., Soubrié Ph., Maffrand J.P., Rostène W., Kitabgi P., Le Fur G. Biochemical and pharmacological profile of a potent and selective non-peptide antagonist of the neurotensin receptor. Proc. Natl. Acad. Sci. USA. 90:1992;65-69.
13. Gully D., Labeeuw B., Boigegrain R., Oury-Donat F., Bachy A., Poncelet M., Steinberg R., Suaud-Chagny M.F., Santucci V., Vita N., Pecceu F., Labbé-Juillé C., Kitabgi P., Soubrié P., Le Fur G., Maffrand J.P. Biochemical and pharmacological activities of SR142948A, a new potent neurotensin receptor antagonist. J. Pharmacol. Exp. Ther. 280:1997;802-812.
14. Kitabgi P., Checler F., Mazella J., Vincent J.P. Pharmacology and biochemistry of neurotensin receptors. Rev. Clin. Basic Pharmacol. 5:1985;397-486.
15. Mazella J., Botto J.-M., Guillemare E., Coppola T., Sarret P., Vincent J.P. Structure, functional expression, and cerebral localisation of the levocabastine-sensitive neurotensin/neuromedin n receptor from mouse brain. J. Neurosci. 16:1996;5613-5620.
16. Nemeroff C.B. Neurotensin: perchance and endogenous neuroleptic? Biol. Psychiatry. 15:1980;283-302.
17. Nouel D., Faure M.P., St. Pierre J.A., Alonso R., Quirion R., Beaudet A. Differential binding profile and internalisation process of neurotensin via neuronal and glial receptors. J. Neurosci. 17:1997;1795-1803.
18. Oury-Donat F., Thurneyssen O., Gonalons N., Forgez P., Gully D., Le Fur G., Soubrie P. Characterisation of the effect of SR48692 on inositol monophosphate, cyclic GMP and cyclic AMP responses linked to neurotensin receptor activation in neuronal and non-neuronal cells. Br. J. Pharmacol. 116:1995;1899-1905.
19. Perrin M., Donaldson C., Chen R.P., Blount A., Berggren T., Bilezikjian L., Sawchenko P., Vale W. Identification of a second corticotrophin-releasing factor receptor gene and characterisation of a cDNA expressed in heart. Proc. Natl. Acad. Sci. USA. 92:1995;2969-2973.
20. Poinot-Chazel C., Portier M., Bouaboula M., Vita N., Pecceu F., Gully D., Monroe J.G., Maffrand J.P., Le Fur G., Casellas P. Activation of mitogen-activated protein kinase couples neurotensin receptor stimulation to induction of the primary response gene krox-24. Biochem. J. 320:1996;145-151.
21. Sambrook, J., Fritsch, E., Maniatis, T., 1989. Cold Spring Harbor Laboratory Press, Cold Spring Harbor, NY.
22. Schotte A., Leysen J.E. Further characterisation of neurotensin binding in the rat brain: levocabastine-displaceable neurotensin binding sites are not histamine-H1 receptors. Biochem. Pharmacol. 38:1989;3891-3893.
23. 3H ]neurotensin binding site in rat brain Naunyn-Schimiedeberg's Arch. Pharmacol. 333:1986;400-405.
24. Tanaka K., Masu M., Nakanishi S. Structure and functional expression of the cloned rat neurotensin receptor. Neuron. 4:1990;847-854.
25. Vincent J.P. Neurotensin receptors: binding properties, transduction pathways, and structure. Cell. Mol. Neurobiol. 15:1995;501-512.
26. Vita N., Laurent P., Lefort S., Chalon P., Dumont X., Kaghad M., Gully D., Le Fur G., Ferrara P., Caput D. Cloning and expression of a complementary DNA encoding a high affinity human neurotensin receptor. FEBS Lett. 317:1993;139-142.
27. Zsurger N., Chabry J., Coquerel A., Vincent J.P. Ontogenesis and binding properties of high-affinity neurotensin receptors in human brain. Brain Res. 586:1992;303-310.