ST1936 stimulates cAMP, Ca2+, ERK1/2 and Fyn kinase through a full activation of cloned human 5-HT6 receptors

European Journal of Pharmacology

Volumn 661, Issue 1-3, 2011, Pages 8-14

  Riccioni, Teresa ^a   Bordi, Fabio ^a   Minetti, Patrizia ^a   Spadoni, Gilberto ^b   Yun, Hyung Mun ^c   Im, Bo Hye ^c,d   Tarzia, Giorgio ^b   Rhim, Hyewhon ^c,d   Borsini, Franco ^a  

^a Sigma Tau SpA   (Italy)

^b UNIVERSITY OF URBINO   (Italy)

^c Korea Institute of Science and Technology   (South Korea)

^d University of Science and Technology (UST)   (South Korea)

Author keywords

(Rat); 5 HT6 receptor; Biochemistry; cAMP; Fyn kinase; ST1936

Indexed keywords

ALPHA ADRENERGIC RECEPTOR; CALCIUM ION; CYCLIC AMP; MITOGEN ACTIVATED PROTEIN KINASE 1; MITOGEN ACTIVATED PROTEIN KINASE 3; N,N DIMETHYL 2 (5 CHLORO 2 METHYL 1H INDOL 3 YL)ETHYLAMINE; PROTEIN KINASE FYN; SEROTONIN 6 RECEPTOR; SEROTONIN AGONIST; SEROTONIN RECEPTOR AFFECTING AGENT; ST 1936; UNCLASSIFIED DRUG; WAY 181187;

ARTICLE; BINDING AFFINITY; BINDING SITE; CELL CLONE; CONCENTRATION RESPONSE; CONTROLLED STUDY; DRUG EFFECT; DRUG MECHANISM; DRUG RECEPTOR BINDING; DRUG SCREENING; DRUG STRUCTURE; DRUG SYNTHESIS; ENZYME ACTIVATION; ENZYME ACTIVITY; ENZYME PHOSPHORYLATION; ENZYME REGULATION; HUMAN; HUMAN CELL; PRIORITY JOURNAL; PROTEIN TARGETING; REGULATORY MECHANISM; SIGNAL TRANSDUCTION;

CALCIUM; CELL LINE, TUMOR; CLONING, MOLECULAR; CYCLIC AMP; ENZYME ACTIVATION; ETHYLAMINES; HUMANS; INDOLES; MITOGEN-ACTIVATED PROTEIN KINASE 1; MITOGEN-ACTIVATED PROTEIN KINASE 3; PHOSPHORYLATION; PROTEIN KINASES; PROTO-ONCOGENE PROTEINS C-FYN; RECEPTORS, SEROTONIN; SEROTONIN RECEPTOR AGONISTS; SIGNAL TRANSDUCTION; THIAZOLES; TRYPTAMINES;

EID: 79956222211     PISSN: 00142999     EISSN: 18790712     Source Type: Journal    
DOI: 10.1016/j.ejphar.2011.04.028     Document Type: Article

References (27)

1. S.J. Ballaz, H. Akil, and S.J. Watson Analysis of 5-HT6 and 5-HT7 receptor gene expression in rats showing differences in novelty-seeking behavior Neuroscience 147 2007 428 438 (Pubitemid 46907454)
2. 6 ligand, on rodent adenylate cyclase and forced swimming test. XXVIth CINP Congress. München (Germany) Int. J. Neuropsychopharmacol. 11 2008 123 124
3. G.V. Carr, L.E. Schechter, and I. Lucki Antidepressant and anxiolytic effects of selective 5-HT(6) receptor agonists in rats Psychopharmacology 213 2010 499 507
4. X. Codony, J. Burgueňo, M.J. Ramirez, and J.M. Vela 5-HT6 Receptor Signal Transduction: Second messenger systems F. Borsini, Pharmacology of 5-HT6 receptors. Part I Int. Rev. Neurobiol. 94 2010 89 110
5. D.S. Dupuis, C. Mannoury la Cour, C. Chaput, L. Verrièle, G. Lavielle, and M.J. Millan Actions of novel agonists, antagonists and antipsychotic agents at recombinant rat 5-HT6 receptors: a comparative study of coupling to Gαs Eur. J. Pharmacol. 588 2008 170 177
6. 6 receptor in cognitive function Neuropharmacology 55 2008 1015 1022
7. C. Gerard, M.P. Martres, K. Lefevre, M.C. Miquel, D. Verge, L. Lanfumey, E. Doucet, M. Hamon, and S. El Mestikawy Immuno-localization of serotonin 5-HT6 receptor-like material in the rat central nervous system Brain Res. 746 1997 207 219 (Pubitemid 27060349)
8. D.J. Heal, S.L. Smith, A. Fisas, X. Codony, and H. Buschmann Selective 5-HT6 receptor ligands: progress in the development of a novel pharmacological approach to the treatment of obesity and related metabolic disorders Pharmacol. Ther. 117 2008 207 231
9. 6 receptor assay for high-throughput screening of chemical ligands and binding proteins Comb. Chem. High Throughput Screen. 11 2008 316 324 (Pubitemid 351705494)
10. R. Kohen, L.A. Fashingbauber, D.E. Heidmann, C.R. Guthrie, and M.W. Hamblin Cloning of the mouse 5-HT6 serotonin receptor and mutagenesis studies of the third cytoplasmatic loop Brain Res. Mol. Brain Res. 90 2001 110 117 (Pubitemid 32537632)
11. A. Mancinelli Pharmacokinetics of 5-HT6 receptor ligands F. Borsini, Pharmacology of 5-HT6 receptors. Part I Int. Rev. Neurobiol. 94 2010 153 169
12. F.J. Monsma Jr., Y. Shen, R.P. Ward, M.W. Hamblin, and D.R. Sibley Cloning and expression of a novel serotonin receptor with affinity for tricyclic psychotropic drugs Mol. Pharmacol. 43 1993 320 327 (Pubitemid 23081986)
13. J.L. Plassat, N. Amlaiky, and R. Hen Molecular cloning of a mammalian serotonin receptor that activates adenylate cyclase Mol. Pharmacol. 44 1993 229 236 (Pubitemid 23252224)
14. C. Routledge, S.M. Bromidge, S.F. Moss, G.W. Price, W. Hirst, H. Newman, G. Riley, T. Gager, T. Stean, N. Upton, S.E. Clarke, A.M. Brown, and D.N. Middlemiss Characterization of SB-271046: a potent, selective and orally active 5-HT(6) receptor antagonist Br. J. Pharmacol. 130 2000 1606 1612 (Pubitemid 30611938)
15. M. Ruat, E. Traiffort, J.M. Arrang, J. Tardivel-Lacombe, J. Diaz, R. Leurs, and J.C. Schwartz A novel rat serotonin (5-HT6) receptor: molecular cloning, localization and stimulation of cAMP accumulation Biochem. Biophys. Res. Commun. 193 1993 268 276 (Pubitemid 23199942)
16. N.V. Ruiz, and G.O. Olsina Patents F. Borsini, Pharmacology of 5-HT6 receptors. Part I Int. Rev. Neurobiol. 94 2010 36 66
17. L.E. Schechter, Q. Lin, D.L. Smith, G. Zhang, Q. Shan, B. Platt, M.R. Brandt, L.A. Dawson, D. Cole, R. Bernotas, A. Robichaud, S. Rosenzweig-Lipson, and C.E. Beyer Neuropharmacological profile of novel and selective 5-HT6 receptor agonists: WAY-181187 and WAY-208466 Neuropsychopharmacology 33 2008 1323 1335 (Pubitemid 351521711)
18. K. Semba, M. Nishizawa, N. Miyajima, M.C. Yoshida, J. Sukegawa, Y. Yamanashi, M. Sasaki, T. Yamamoto, and K. Toyoshima Yes-related protooncogene, syn, belongs to the protein-tyrosine kinase family Proc. Natl. Acad. Sci. U. S. A. 83 1986 5459 5463 (Pubitemid 16001242)
19. S.K. Shirazi, and J.G. Wood The protein tyrosine kinase, fyn, in Alzheimer's disease pathology Neuroreport 4 1993 435 437 (Pubitemid 23116742)
20. P. Svenningsson, E.T. Tzavara, H. Qi, R. Carruthers, J.M. Witkin, G.G. Nomikons, and P. Greengard Biochemical and behavioural evidence for antidepressant-like effects of 5-HT6 receptor stimulation J. Neurosci. 27 2007 4201 4209 (Pubitemid 46597167)
21. A. Szczepankiewicz, J.K. Rybakowski, M. Skibinska, M. Dmitrzak-Weglarz, A. Leszczynska-Rodziewicz, M. Wilkosc, and J. Hauser FYN kinase gene: another glutamatergic gene associated with bipolar disorder? Neuropsychobiology 59 2009 178 183
22. S.M. Thomas, and J.S. Brugge Cellular functions regulated by src family kinases Cell Dev. Biol. 13 1997 513 609 (Pubitemid 28034534)
23. V. Valentini, R. Frau, F. Bordi, F. Borsini, and G. Di Chiara A microdialysis study of ST1936, a novel 5-HT6 receptor agonist Neuropharmacology 60 2011 602 608
24. R.P. Ward, M.W. Hamblin, J.E. Lachowicz, B.J. Hoffman, D.R. Sibley, and D.M. Dorsa Localization of serotonin subtype 6 receptor messenger RNA in the rat brain by in situ hybridization histochemistry Neuroscience 64 1995 1105 1111
25. A. Wesolowska, and A. Nikiforuk Effects of the brain-penetrant and selective 5-HT6 receptor antagonists SB-3999885 in animal models of anxiety and depression Neuropharmacology 52 2007 1274 1283 (Pubitemid 46527703)
26. A. Wesolowska, A. Nikiforuk, and K. Stachowicz Anxiolytic-like and antidepressant-like effect produced by the selective 5-HT6 receptor antagonist SB-258585 after the intrahippocampal administration to rats Behav. Pharmacol. 18 2007 439 446 (Pubitemid 47356370)
27. H.M. Yun, S. Kim, H.J. Kim, E. Kostenis, J.I. Kim, J.Y. Seong, J.H. Baik, and H. Rhim The novel cellular mechanism of human 5-HT6 receptor through an interaction with Fyn J. Biol. Chem. 282 2007 5496 5505 (Pubitemid 47093777)