Characterization of SB-271046: A potent, selective and orally active 5-HT6 receptor antagonist

British Journal of Pharmacology

Volumn 130, Issue 7, 2000, Pages 1606-1612

  Routledge, Carol ^a   Bromidge, Steven M ^a   Moss, Stephen F ^a   Price, Gary W ^a   Hirst, Warren ^a   Newman, Helen ^a   Riley, Graham ^a   Gager, Tracey ^a   Stean, Tania ^a   Upton, Neil ^a   Clarke, Stephen E ^a   Brown, Anthony M ^a   Middlemiss, Derek N ^a  

^a GLAXOSMITHKLINE   (United Kingdom)

Author keywords

Adenylyl cyclase; Pharmacokinetics; Rat maximal electroshock seizure threshold (MEST) test; SB 258585; SB 271046

Indexed keywords

4 AMINO N [2,6 BIS(METHYLAMINO) 4 PYRIMIDINYL]BENZENESULFONAMIDE; 5 CHLORO N (4 METHOXY 3 PIPERAZIN 1 YLPHENYL) 3 METHYL 2 BENZOTHIOPHENESULFONAMIDE; ADENYLATE CYCLASE; SB 258510; SEROTONIN 6 RECEPTOR; SEROTONIN ANTAGONIST;

ANIMAL EXPERIMENT; ANTICONVULSANT ACTIVITY; ARTICLE; HELA CELL; HUMAN; HUMAN CELL; NONHUMAN; PRIORITY JOURNAL; RAT; SEIZURE THRESHOLD;

ADENYLATE CYCLASE; ADMINISTRATION, ORAL; ANIMALS; BINDING, COMPETITIVE; BRAIN; COGNITION; DISEASE MODELS, ANIMAL; ELECTRIC STIMULATION; HELA CELLS; HUMANS; MALE; RADIOLIGAND ASSAY; RATS; RATS, SPRAGUE-DAWLEY; RECEPTORS, SEROTONIN; RECOMBINANT PROTEINS; SEIZURES; SEROTONIN ANTAGONISTS; SULFONAMIDES; THIOPHENES; TRANSFECTION;

EID: 0033854822     PISSN: 00071188     EISSN: None     Source Type: Journal    
DOI: 10.1038/sj.bjp.0703457     Document Type: Article

References (28)

1. 6 receptor antagonist, Ro 04-6790, in rats. Br. J. Pharmacol., 126, 1537-1542.
2. 6 antisense oligonucleotide i.c.v. affects rat performance in the water maze and feeding. British Association for Psychopharmacology Meeting, Cambridge, 13-17th July 1997, P255.
3. 6 receptors stably expressed in HEK293 cells. Neuropharmacol., 36, 713-720.
4. 6 receptors in nigro-striatal function in rodents. Br. J. Pharmacol., 125, 1562-1566.
5. 6 receptor in the rat brain: a study using antisense oligonucleotides. J. Pharmacol. Exp. Ther., 274, 173-180.
6. BOWEN, W.P. & JERMAN, J.C. (1995). Nonlinear regression using spreadsheets. Trends in Pharmacol. Sci., 16, 413-417.
7. 6 Receptor Antagonist. J. Med. Chem., 42, 202-205.
8. 50) of an enzymatic reaction. Biochem. Pharmacol., 92, 881-894.
9. 1A receptor antagonist. Behav. Brain Res., 73, 337-353.
10. 1B receptor inverse agonist 1′-methyl-5[[2′-methyl-4′-(5-methyl-1,2,4-oxadiazol-3-yl)biphenyl-4-yl]carbonyl-2,3,6,7-tetrahydrospiro[furo[2,3-F]indole-3,4′-piperidine] (SB-224289) potently blocks terminal 5-HT autoreceptor function both in vitro and in vivo. J. Med. Chem., 41, 1218-1235.
11. HIRST, W.D., MINTON, J.A.L., BROMIDGE, S.M., MOSS, S.F., LATTER, A.J., RILEY, G., ROUTLEDGE, C., MIDDLEMISS, D.N. & PRICE, G.W. Characterisation of [1251] SB-258585 binding to human recombinant and native 5-HT receptors in rat, pig and human brain tissue. Br. J. Pharmacol., (In Press).
12. KIMBALL, A.W., BURNETT, W.T. & DOHERTY, D.G. (1957). Chemical protection against ionising radiation I. Sampling methods of screening compounds in radiation protection studies in mice. Radiation Res., 7, 1-12.
13. 6 serotonin receptor. J. Neurochem., 66, 47-56.
14. LITCHFIELD, J.T. & WILCOXON, F. (1949). A simplified method of evaluating dose-effect experiments. J. Pharmacol. Exp. Ther., 96, 99-113.
15. MONSMA, JR. F.J., SHEN, Y., WARD, R.P., HAMBLIN, M.W. & SIBLEY, D.R. (1993). Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol., 43, 320-327.
16. 6 antagonist SB-271046. Br. J. Pharmacol., 127, 22P.
17. ROTH, B.L., CRAIGO, S.C., CHOUDHARY, M.S., ULUER, A., MONSMA, F.J., SHEN, Y., MELTZER, H.Y. & SIBLEY, D.R. (1994). Binding of typical and atypical antipsychotic agents to 5-hydroxytryptamine-6 and 5-hydroxytryptamine-7 receptors. J. Pharmacol. Exp. Ther., 268, 1403-1410.
18. 6 receptor antagonist. Br. J. Pharmacol., 127, 21P.
19. 6) receptor: molecular cloning, localization and stimulation of cAMP accumulation. Biochem. Biophys. Res. Comm., 193, 268-276.
20. SALOMON, Y. (1979). Adenylate cyclase assay. Adv. Cyclic. Nuc. Res., 10, 35-55.
21. SCHOEFFTER, P. & WAEBER, C. (1994). 5-Hydroxytryptamine receptors with a 5-HT6 receptor-like profile stimulating adenylyl cyclase activity in pig caudate membranes. Naunyn Schmiedebergs Arch. Pharmacol., 350, 356-360.
22. 6 receptors. Br. J. Pharmacol., 124, 556-562.
23. 6 receptor antagonist SB-271046-A in the rat maximal electroshock seizure threshold test. Br. J. Pharmacol., 127, 131P.
24. UPTON, N., BLACKBURN, T.P., CAMPBELL, C.A., COOPER, D., EVANS, M.L., HERDON, H.J., KING, P.D., RAY, A.M., STEAN, T.O., CHAN, W.N., EVANS, J.M. & THOMPSON, M. (1997). Profile of SB-204269, a mechanistically novel anticonvulsant drug, in rat models of focal and generalised epileptic seizures. Br. J. Pharmacol., 121, 1679-1686.
25. 3 receptor antagonist, attenuates the increased seizure susceptibility observed during diazepam-induced withdrawal in mice. Br. J. Pharmacol., 108, 254P.
26. 2B receptors in regulating generalised seizure threshold in rodents. Eur. J. Pharmacol., 359, 33-40.
27. YAU, J.L.W., NOBLE, J., WIDDOWSON, J. & SECKL, J.R. (1997). Impact of adrenalectomy on 5-HT6 and 5-HT7 receptor gene expression in the rat hippocampus. Mol. Brain Res., 45, 182-186.
28. 6 receptor subtype in the rat brain. Life Sci., 62, 1473-1477.