Characterization of [125I]-SB-258585 binding to human recombinant and native 5-HT6 receptors in rat, pig and human brain tissue

British Journal of Pharmacology

Volumn 130, Issue 7, 2000, Pages 1597-1605

  Hirst, Warren D ^a   Minton, Jayne A L ^a   Bromidge, Steven M ^a   Moss, Stephen F ^a   Latter, Alison J ^a   Riley, Graham ^a   Routledge, Carol ^a   Middlemiss, Derek N ^a   Price, Gary W ^a  

^a GLAXOSMITHKLINE   (United Kingdom)

Author keywords

Radioligand binding; SB 258585; SB 271046

Indexed keywords

4 AMINO N [2,6 BIS(METHYLAMINO) 4 PYRIMIDINYL]BENZENESULFONAMIDE; 5 CARBAMOYLTRYPTAMINE; 5 CHLORO N (4 METHOXY 3 PIPERAZIN 1 YLPHENYL) 3 METHYL 2 BENZOTHIOPHENESULFONAMIDE; 5 METHOXYTRYPTAMINE; AMITRIPTYLINE; CLOZAPINE; IODINE 125; METITEPINE; MIANSERIN; RADIOPHARMACEUTICAL AGENT; RITANSERIN; SB 214111; SB 258585; SEROTONIN; SEROTONIN 6 RECEPTOR; SEROTONIN AGONIST; LYSERGIDE; PIPERAZINE DERIVATIVE; RADIOACTIVE IODINE; RECOMBINANT PROTEIN; SEROTONIN ANTAGONIST; SEROTONIN RECEPTOR; SULFONAMIDE; TRITIUM;

ANIMAL TISSUE; ARTICLE; CORPUS STRIATUM; DRUG POTENCY; DRUG RECEPTOR BINDING; HUMAN; HUMAN TISSUE; NONHUMAN; PRIORITY JOURNAL; PUTAMEN; RAT; RECEPTOR AFFINITY; SWINE; ANIMAL; BINDING COMPETITION; BRAIN; CAUDATE NUCLEUS; CELL MEMBRANE; CYTOLOGY; DRUG ANTAGONISM; DRUG EFFECT; HELA CELL; METABOLISM; RADIOASSAY; SPRAGUE DAWLEY RAT;

ANIMALS; BINDING, COMPETITIVE; BRAIN; CAUDATE NUCLEUS; CELL MEMBRANE; CORPUS STRIATUM; HELA CELLS; HUMANS; IODINE RADIOISOTOPES; LYSERGIC ACID DIETHYLAMIDE; PIPERAZINES; PUTAMEN; RADIOLIGAND ASSAY; RATS; RATS, SPRAGUE-DAWLEY; RECEPTORS, SEROTONIN; RECOMBINANT PROTEINS; SEROTONIN ANTAGONISTS; SULFONAMIDES; SWINE; TRITIUM;

EID: 0033624158     PISSN: 00071188     EISSN: None     Source Type: Journal    
DOI: 10.1038/sj.bjp.0703458     Document Type: Article

References (44)

1. 1 receptor subtype coupled to the inhibition of adenylate cyclase. Proc. Natl. Acad. Sci. USA., 90, 408-412.
2. 6 receptor antagonist, Ro 04-6790, in rats. Br. J. Pharmacol., 126, 1537-1542.
3. 6 receptors stably expressed in HEK293 cells. Neuropharmacol., 36, 713-720.
4. 3H]Ro 63-0563 labels 5-hydroxytryptamine receptor binding sites in rat and porcine striatum. Mol. Pharmacol., 54, 577-583.
5. 2C receptors. Br. J. Pharmacol., 115, 622-628.
6. 6 receptors in nigro-striatal function in rodents. Br. J. Pharmacol., 125, 1562-1566.
7. 6 receptor in the rat brain: a study using antisense oligonucleotides. J. Pharmacol. Exp. Ther., 274, 173-180.
8. 3 dopamine receptors: GppNHp shifts are explained by the presence of more than one binding site in each clone. Br. J. Pharmacol., 108, 277P.
9. BOWEN, W.P. & JERMAN, J.C. (1995). Nonlinear regression using spreadsheets. Trends in Pharmacol. Sci., 16, 413-417.
10. 6 receptor antagonist. J. Med. Chem., 42, 202-205.
11. 4 receptors. Br. J. Pharmacol., 110, 10P.
12. 50) of an enzymatic reaction. Biochem. Pharmacol., 92, 881-894.
13. CONNER, D.A. & MANSOUR, T.E. (1990). Serotonin receptor-mediated activation of adenylate cyclase in the neuroblastoma NCB 20: a novel 5-hydroxytryptamine receptor. Mol. Pharmacol., 37, 742-751.
14. 6 receptor mRNA in the central nervous system of control or 5,7-dihydroxytryptamine-treated rats. Synapse, 23, 164-173.
15. 6 receptor-like material in the rat central nervous system. Brain Res., 746, 207-219.
16. 6 serotonin receptors may reflect psychoactive profile. Mol. Med., 1, 398-406.
17. 3H]PAT. Nature, 305, 140-142.
18. HAMBLIN, M.W. & METCALF, M.A. (1991). Primary structure and functional characterization of a human 5-HT1D-type serotonin receptor. Mol. Pharmacol., 40, 143-148.
19. 3H-5 hydroxytryptamine binding site subtype in bovine brain membranes. J. Neurosci., 7, 894-903.
20. 6 receptors. Br. J. Pharmacol., 127, 23P.
21. HOYER, D., CLARKE, D.E., FOZARD, J.R., HARTIG, P.R., MARTIN, G.R., MYLECHARANE, E.J., SAXENA, P.R. & HUMPHREY, P.P. (1994). International Union of Pharmacology classification of receptors for 5-hydroxytryptamine (Serotonin). Pharmacol. Rev., 46, 157-203.
22. HOYER, D. & MARTIN, G.R. (1996). Classification and nomeclature of 5-HT receptors: A comment on current issues. Behav. Brain Res., 73, 263-268.
23. 6 serotonin receptor. J. Neurochem., 66, 47-56.
24. KURSAR, J.D., NELSON, D.L., WAINSCOTT, D.B., COHEN, M.L. & BAEZ, M. (1992). Molecular cloning, functional expression, and pharmacological characterization of a novel serotonin receptor (5-hydroxytryptamine2F) from rat stomach fundus. Mol. Pharmacol., 42, 549-557.
25. McPHERSON, G.A. (1997). KELL: A collection of radioligand binding analysis programs. Cambridge, UK: Biosoft.
26. 6 receptors in native tissues. Br. J. Pharmacol., 128, 157P.
27. MONSMA, F.J., JR., 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.
28. MUNSON, P.J. & RODBARD, D. (1980). Ligand: A versatile computerized approach for characterization of ligand-binding systems. Anal. Biochem., 107, 220-239.
29. 6 receptor variant produced by alternative splicing. Mol. Brain Res., 64, 255-263.
30. 125I]SB-258585. Br. J. Pharmacol., 128, 156P.
31. 6 antagonist SB-271046. Br. J. Pharmacol., 127, 22P.
32. 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.
33. 6 receptor antagonist. Br. J. Pharmacol., 127, 21P.
34. 6) receptor: molecular cloning, localization and stimulation of cAMP accumulation. Biochem. Biophys. Res. Comm., 193, 268-276.
35. 6 receptor-like profile stimulating adenylyl cyclase activity in pig caudate membranes. Naunyn Schmiedebergs Arch. Pharmacol., 350, 356-360.
36. 6 receptors positively coupled to adenylyl cyclase in striatal neurones in culture. Neuroreport, 5, 2553-2557.
37. 6 receptors. Br. J. Pharmacol., 124, 556-562.
38. 2 receptor. Eur. J. Pharmacol., 225, 331-337.
39. TESTA, R., GUARNERI, M., IBBA, M., STRADA, G., POGGESI, E., TADDEI, C., SIMONAZZI, I. & LEONARDI, A. (1993). Characterisation of α1-adrenoceptor subtypes in prostate and prostatic urethra of rat, rabbit, dog and man. Eur. J. Pharmacol., 249, 307-315.
40. 7 receptors in guinea-pig brain. Br. J. Pharmacol., 115, 107-116.
41. UNSWORTH, C.D. & MOLINOFF, P.B. (1994). Characterization of a 5-hydroxytryptamine receptor in mouse neuroblastoma N18TG2 cells. J. Pharmacol. Exp. Ther., 269, 246-255.
42. WARD, R.P., HAMBLIN, M.W., LACHOWICZ, J.E., HOFFMAN, B.J., SIBLEY, D.R. & DORSA, D.M. (1995). Localization of serotonin subtype 6 receptor messenger RNA in the rat brain by in situ hybridization histochemistry. Neuroscience, 64, 1105-1111.
43. 2A receptor. Pharmacol. Comun., 5, 109-116.
44. 6 receptor subtype in the rat brain. Life Sci., 62, 1473-1477.