The ligand-binding site of buspirone analogues at the 5-HT(1A) receptor

Journal of Pharmacy and Pharmacology

Volumn 49, Issue 7, 1997, Pages 698-705

  Sylte, Ingebrigt ^a   Chilmonczyk, Zdzislaw ^b   Dahl, Svein G ^a   Cybulski, Jacek ^b   Edvardsen, Øyvind ^a  

^a UNIVERSITY OF TROMSØ   (Norway)

^b INDUSTRIAL CHEMISTRY RESEARCH INSTITUTE   (Poland)

Author keywords

[No Author keywords available]

Indexed keywords

BUSPIRONE; RHODOPSIN; SEROTONIN 1A RECEPTOR;

AMINO TERMINAL SEQUENCE; ARTICLE; BINDING AFFINITY; CARBOXY TERMINAL SEQUENCE; HYDROGEN BOND; LIGAND BINDING; MOLECULAR DYNAMICS; MOLECULAR INTERACTION; MOLECULAR MODEL; RECEPTOR BINDING; SIMULATION; STEREOSPECIFICITY;

EID: 0030764518     PISSN: 00223573     EISSN: None     Source Type: Journal    
DOI: 10.1111/j.2042-7158.1997.tb06095.x     Document Type: Article

References (32)

1. Anukanth, A., Khorana, H. G. (1994) Structure and function of rhodopsin. Requirements of a specific structure for the intradiscal domain. J. Biol. Chem. 269: 19738-19744
2. Baldwin, J. M. (1993) The probable arrangement of the helices in G protein-coupled receptors. EMBO J. 12: 1693-1703
3. Baldwin, J. M. (1994) Structure and function of receptors coupled to G proteins. Curr. Opin. Cell Biol. 6: 180-190
4. 1A receptor pharmacophore. J. Mol. Model. 1: 188-195
5. 1a serotonin receptors. Mol. Pharmacol. 43: 516-520
6. 1A receptor. 1. The molecular structure of buspirone and its two analogues. J. Med. Chem. 38: 1701-1710
7. Donnelly, D., Findlay, J. B. C., Blundell, T. L. (1994) The evolution and structure of aminergic G protein-coupled receptors. Receptors and Channels 2: 61-78
8. Ferenczy, G. F., Morris, G. M. (1989) The active site of cytochrome P-450 nifedipine oxidase: a model building study. J. Mol. Graphics 7: 206-211
9. Goa, K. L., Ward, A. (1986) Buspirone: a preliminary review of its pharmacological properties and therapeutic efficacy as an anxiolytic. Drugs 32: 114-129
10. 1A receptors. Mol. Pharmacol. 41: 695-698
11. Henderson, R., Baldwin, J. M., Ceska, T. A., Zemlin, F., Beckman, E., Downing, K. H. (1990) Model for the structure of bacteriorhodopsin based on high-resolution electron cryo-microscopy. J. Mol. Biol. 213: 899-929
12. 1A receptor. J. Med. Chem. 31: 1087-1093
13. 1A receptor agonists and definition of a steric model of this site. Eur. J. Med. Chem. 24: 31-37
14. 1A receptor: a site-directed mutation study. FEBS Lett. 312: 259-262
15. Hoyer, D., Clarke, D. E., Fozard, J. R., Hartig, P. R., Martin, G. R., Mylecharane, E. J., Saxena, P. R., Humphrey, P. A. (1994) VII. International Union of Pharmacology classification of receptors for 5-hydroxytryptamine (serotonin). Pharmacol. Rev. 46: 157-203
16. 2 dopamine receptors. Endocrine J. 2: 7-23
17. 1A receptor ligands. J. Med. Chem. 38: 1942-1954
18. Min, K. C., Zvyaga, T. A., Cypess, A. M., Sakmar, T. P. (1993) Characterization of mutant rhodopsin responsible for autosomal dominant retinitis pigmentosa. Mutations on the cytoplasmic surface affect transducin activation. J. Biol. Chem. 268: 9400-9404
19. Peroutka, S. J. (1995) Serotonin receptors. Their evolution and clinical relevance. CNS Drugs 4 (Suppl. 1): 18-28
20. Schertler, G. F. X., Villa, C., Henderson, R. (1993) Projection structure of rhodopsin. Nature 362: 770-772
21. Schwartz, T. W. (1994) Locating ligand-binding sites in 7TM receptors by protein engineering. Curr. Opin. Biotech. 5: 434-444
22. 2A receptors. J. Biol. Chem. 270: 16683-16688
23. Singh, U. C., Kollman, P. A. (1984) An approach to computing electrostatic charges for molecules. J. Comput. Chem. 5: 129-145
24. 1A receptor interactions. Protein Eng. 9: 149-160
25. 1A receptor-related anxiolytics. Trends Pharmacol. Sci. 8: 432-437
26. Unger, V. M., Schertler, G. F. X. (1995) Low resolution structure of bovine rhodopsin determined by electron cryo-microscopy. Biophys. J. 68: 1776-1786
27. van Rhee, A. M., Jacobson, K. A. (1996) Molecular architecture of G protein-coupled receptors. Drug. Dev. Res. 37: 1-38
28. Weiner, S. J., Kollman, P. A., Case, D. A., Singh, U. C., Ohio, C., Alagona, G., Profeta Jr, S., Weiner, P. (1984) A new force field for molecular mechanical simulation of nucleic acids and proteins. J. Am. Chem. Soc. 106: 765-784
29. Weiner, S. J., Kollmann, P. A., Nguyen, D. T., Case, D. A. (1986) An all-atom force field for simulation of proteins and nucleic acids. J. Comput. Chem. 7: 230-252
30. Wess, J., Nanavati, S., Vogel, Z., Maggio, R. (1993) Functional role of proline and tryptophan residues highly conserved among G protein-coupled receptors studied by mutational analysis of the m3 muscarinic receptor. EMBO J. 12: 331-338
31. 1A agonists measured with the forced swim test. Psychopharmacology 101: 497-504
32. Zhou, W., Flanagan, C., Ballesteros, J. A., Konvicka, K., Davidson, J. S., Weinstein, H., Millar, R. P., Sealfon, S. C. (1994) Replacement of lysine-181 by aspartic acid in the third trans-membrane region of endothelin type B receptor reduces its affinity to endothelin peptides and sarafotoxin 6c without affecting G protein coupling. Mol. Pharmacol. 45: 165-170