Ligand conformation has a definitive effect on 5-HT 1A and serotonin reuptake affinity

Bioorganic and Medicinal Chemistry Letters

Volumn 14, Issue 17, 2004, Pages 4467-4470

  Boy, Kenneth M ^a   Dee, Michael ^a   Yevich, Joseph ^a   Torrente, John ^a   Gao, Qi ^a   Iben, Lawrence ^a   Stark, Arlene ^a   Mattson, Ronald J ^a  

^a BRISTOL MYERS SQUIBB   (United States)

Author keywords

5 HT 1A; Depression; Serotonin; SSRI

Indexed keywords

SEROTONIN 1A ANTAGONIST; SEROTONIN UPTAKE INHIBITOR;

ARTICLE; BINDING AFFINITY; DRUG DESIGN; DRUG POTENCY; DRUG SYNTHESIS; LIGAND BINDING;

LIGANDS; MOLECULAR CONFORMATION; RECEPTOR, SEROTONIN, 5-HT1A; SEROTONIN; SEROTONIN UPTAKE INHIBITORS;

EID: 3843139591     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2004.06.050     Document Type: Article

References (16)

1. World Health Organization WHO Fact Sheet Number 265 2001 The World Health Organization Geneva, Switzerland
2. M.E. Thase J. Clin. Psychiatry 64 Suppl. 13 2003 18 25
3. M. Fava J. Clin. Psychiatry 64 Suppl. 13 2003 26 29
4. S.M. Stahl, and M.M. Grady J. Clin. Psychiatry 64 Suppl. 13 2003 13 17
5. A.F. Schatzberg J. Clin. Psychiatry 64 Suppl. 13 2003 30 37
6. P. Blier, R. Bergeron, and C. de Montigny Neuropsychopharmacology 16 1997 333 338
7. P. Blier, and R. Bergeron J. Clin. Psychopharmacol. 15 1995 217 222
8. R.J. Mattson, J.D. Catt, C.P. Sloan, Q. Gao, R.B. Carter, A. Gentile, C.D. Mahle, F.F. Matos, R. McGovern, C.P. VanderMaelen, and F.D. Yocca Bioorg. Med. Chem. Lett. 13 2003 285 288
9. R.J. Mattson, C.P. Sloan, C.C. Lockhart, J.D. Catt, Q. Gao, and S. Huang J. Org. Chem. 64 1999 8004 8007
10. Crystallographic data has been deposited with the Cambridge Crystallographic Data Centre as supplementary publication number CCDC 241821. Copies of the data can be obtained, free of charge, via the Internet at http://www.ccdc.cam.ac.uk
11. d concentration. Each experiment was carried out from 1 to 6 times. Standard errors were typically within 20% of the mean value
12. C.D. Mahle, H.L. Wiener, F.D. Yocca, and S. Maayani J. Pharmacol. Exp. Ther. 263 1992 1275
13. R.B. Rothman, S. Jayanthi, X. Wang, C.M. Dersch, J.L. Cadet, T. Prisinzano, K.C. Rice, and M.H. Baumann Synapse 50 2003 233 239
14. Poss, M. A.; Tortolani, D. R.; Mattson, R. J.; Yevich, J. P. U.S. Patent 6,225,324, example 11
15. F.D. Yocca, L. Iben, and E. Meller Mol. Pharmacol. 41 1992 1066 1072
16. J.M. Zgombick, S.G. Beck, C.D. Mahle, B. Craddock-Royal, and S. Maayani Mol. Pharmacol. 35 1989 484 494