Effects of mutations at conserved TM II residues on ligand binding and activation of mouse 5-HT6 receptor

European Journal of Pharmacology

Volumn 534, Issue 1-3, 2006, Pages 77-82

  Zhang, Jiaping ^a   Shen, Chun Pyn ^a   Xiao, Jing C ^a   Lanza, Thomas J ^a   Lin, Linus S ^a   Francis, Barbara E ^a   Fong, Tung M ^a   Chen, Richard Z ^a  

^a MERCK RESEARCH LABORATORIES   (United States)

Author keywords

Mouse 5 HT6 receptor; Site directed mutagenesis

Indexed keywords

ADENYLATE CYCLASE; ASPARTIC ACID; CYCLIC AMP; G PROTEIN COUPLED RECEPTOR; MEMBRANE PROTEIN; SB 258585; SEROTONIN; SEROTONIN 6 RECEPTOR; SEROTONIN ANTAGONIST; UNCLASSIFIED DRUG;

ANIMAL CELL; ARTICLE; CELL STRAIN HEK293; CONTROLLED STUDY; DRUG BINDING; GENETIC TRANSFECTION; HUMAN; HUMAN CELL; LIGAND BINDING; MOUSE; MUTATION; NONHUMAN; NORTHERN BLOTTING; PRIORITY JOURNAL; RADIOASSAY; SITE DIRECTED MUTAGENESIS;

AMINO ACID SEQUENCE; AMINO ACID SUBSTITUTION; ANIMALS; CELL LINE; CYCLIC AMP; HUMANS; LIGANDS; MICE; MOLECULAR SEQUENCE DATA; MUTAGENESIS, SITE-DIRECTED; PIPERAZINES; PROTEIN STRUCTURE, TERTIARY; RECEPTORS, SEROTONIN; SEROTONIN; SEROTONIN AGONISTS; SEROTONIN ANTAGONISTS; SULFONAMIDES; TRANSFECTION;

EID: 33644980063     PISSN: 00142999     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.ejphar.2006.01.049     Document Type: Article

References (30)

1. F.G. Boess, F.J. Monsma, V. Meyer, C. Zwingelstein, and A.J. Sleight Interaction of tryptamine and ergoline compounds with threonine 196 in the ligand binding site of the 5-hydroxytryptamine6 receptor Mol. Pharmacol. 52 1997 515 523
2. 6 receptor J. Neurochem. 71 1998 2169 2177
3. 6 receptor in the rat brain: a study using antisense oligonucleotides J. Pharmacol. Exp. Ther. 274 1995 173 180
4. B.P. Ceresa, and L.E. Limbird Mutation of an aspartate residue highly conserved among G-protein-coupled receptors results in nonreciprocal disruption of alpha 2-adrenergic receptor-G-protein interactions. A negative charge at amino acid residue 79 forecasts alpha 2A-adrenergic receptor sensitivity to allosteric modulation by monovalent cations and fully effective receptor/G-protein coupling J. Biol. Chem. 269 1994 29557 29564
5. P.K. Chanda, M.C. Minchin, A.R. Davis, L. Greenberg, Y. Reilly, W.H. McGregor, R. Bhat, M.D. Lubeck, S. Mizutani, and P.P. Hung Identification of residues important for ligand binding to the human 5-hydroxytryptamine1A serotonin receptor Mol. Pharmacol. 43 1993 516 520
6. L.A. Dawson, H.Q. Nguyen, and P. Li The 5-HT(6) receptor antagonist SB-271046 selectively enhances excitatory neurotransmission in the rat frontal cortex and hippocampus Neuropsychopharmacology 25 2001 662 668
7. 125I]SB-258585 Synapse 45 2002 191 199
8. T.M. Fong Overview of mutagenesis studies J. Wess Structure-Function Analysis of G Protein-Coupled Receptors 1999 Wiley and Son New York, NY 1 20
9. 6 receptors Neuropsychopharmacology 21 1999 68S 76S
10. 125I]-SB-258585 binding to human recombinant and native 5-HT(6) receptors in rat, pig and human brain tissue Br. J. Pharmacol. 130 2000 1597 1605
11. W.D. Hirst, B. Abrahamsen, F.E. Blaney, A.R. Calver, L. Aloj, G.W. Price, and A.D. Medhurst Differences in the central nervous system distribution and pharmacology of the mouse 5-hydroxytryptamine-6 receptor compared with rat and human receptors investigated by radioligand binding, site-directed mutagenesis, and molecular modeling Mol. Pharmacol. 64 2003 1295 1308
12. R.R. Huang, H. Yu, C.D. Strader, and T.M. Fong Interaction of substance P with the second and seventh transmembrane domains of the neurokinin-1 receptor Biochemistry 33 1994 3007 3013
13. R.R. Huang, P.P. Vicario, C.D. Strader, and T.M. Fong Identification of residues involved in ligand binding to the neurokinin-2 receptor Biochemistry 34 1995 10048 10055
14. 6 serotonin receptor J. Neurochem. 66 1996 47 56
15. K. Kristiansen Molecular mechanisms of ligand binding, signaling, and regulation within the superfamily of G-protein-coupled receptors: molecular modeling and mutagenesis approaches to receptor structure and function Pharmacol. Ther. 103 2004 21 80
16. T. Mirzadegan, G. Benko, S. Filipek, and K. Palczewski Sequence analyses of G-protein-coupled receptors: similarities to rhodopsin Biochemistry 42 2003 2759 2767
17. 2 receptor affinity for drugs and inhibition of adenylyl cyclase Mol. Pharmacol. 39 1991 733 739
18. K. Palczewski, T. Kumasaka, T. Hori, C.A. Behnke, H. Motoshima, B.A. Fox, I. Le Trong, D.C. Teller, T. Okada, R.E. Stenkamp, M. Yamamoto, and M. Miyano Crystal structure of rhodopsin: a G protein-coupled receptor Science 289 2000 739 745
19. 6 receptors Bioorg. Med. Chem. Lett. 14 2004 4569 4573
20. 6 receptor antagonist J. Med. Chem. 46 2003 1273 1276
21. 125I]SB-258585 Brain Res. 934 2002 49 57
22. 6 receptor antagonists enhance retention of a water maze task in the rat Psychopharmacology (Berlin) 158 2001 114 119
23. 6) receptor: molecular cloning, localization and stimulation of cAMP accumulation Biochem. Biophys. Res. Commun. 193 1993 268 276
24. 2A receptor J. Biol. Chem. 270 1995 16683 16688
25. 6 expression in the rat: functional studies using antisense oligonucleotides Behav. Brain Res. 73 1996 245 248
26. T.O. Stean, W.D. Hirst, D.R. Thomas, G.W. Price, D. Rogers, G. Riley, S.M. Bromidge, H.T. Serafinowska, D.R. Smith, S. Bartlett, N. Deeks, M. Duxon, and N. Upton Pharmacological profile of SB-357134: a potent, selective, brain penetrant, and orally active 5-HT(6) receptor antagonist Pharmacol. Biochem. Behav. 71 2002 645 654
27. C.D. Strader, I.S. Sigal, M.R. Candelore, E. Rands, W.S. Hill, and R.A. Dixon Conserved aspartic acid residues 79 and 113 of the beta-adrenergic receptor have different roles in receptor function J. Biol. Chem. 263 1988 10267 10271
28. 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
29. 6 receptors in retention of spatial learning in the Morris water maze Neuropharmacology 41 2001 210 219
30. 6 receptors Curr. Drug Targets CNS Neurol. Disord. 3 2004 59 79