Experimental solubility profiling of marketed CNS drugs, exploring solubility limit of CNS discovery candidate

Bioorganic and Medicinal Chemistry Letters

Volumn 20, Issue 24, 2010, Pages 7312-7316

  Alelyunas, Yun W ^a   Empfield, James R ^a   McCarthy, Dennis ^a   Spreen, Russell C ^a   Bui, Khanh ^a   Pelosi Kilby, Luciana ^a   Shen, Cindy ^a  

^a ASTRAZENECA   (United Kingdom)

Author keywords

CNS; Lipophilicity; Solubility; Toxicity

Indexed keywords

ALPIDEM; ALPRAZOLAM; AMFEBUTAMONE; AMISULPRIDE; AMPHETAMINE; ANIRACETAM; ATOMOXETINE; BROMAZEPAM; BUPIVACAINE; BUSPIRONE; BUTORPHANOL; CARBAMAZEPINE; CENTRAL NERVOUS SYSTEM AGENTS; CITALOPRAM; CLOMIPRAMINE; CLONAZEPAM; CLORAZEPATE; CLOZAPINE; DEXFENFLURAMINE; DEXTROPROPOXYPHENE; DIAZEPAM; DIHYDROERGOTAMINE; DOLASETRON MESILATE; DONEPEZIL; METACLAZEPAM; NEFAZODONE; PERGOLIDE; QUAZEPAM; UNINDEXED DRUG; ZIPRASIDONE;

ARTICLE; DRUG SOLUBILITY; MOLECULAR WEIGHT; PH MEASUREMENT;

CENTRAL NERVOUS SYSTEM AGENTS; DRUG EVALUATION, PRECLINICAL; HYDROGEN-ION CONCENTRATION; PHARMACEUTICAL PREPARATIONS; SOLUBILITY;

EID: 78449313272     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2010.10.068     Document Type: Article

References (44)

1. I. Kola, and J. Landis Nat. Rev. Drug Discov. 3 2004 711
2. Aaron, S. http://money.cnn.com/2007/08/10/news/companies/wyeth/index.htm, accessed 2010, August.
3. Aaron, S. http://money.cnn.com/2007/06/29/news/companies/acomplia/index. htm, accessed 2010, August.
4. S.D. Garad Am. Pharm. Rev. 7 2004 80
5. Humphreys, A. MedAdNews, 2001, May.
6. P.D. Leeson, and A.M. Davis J. Med. Chem. 47 2004 6338
7. Humphreys, A.; Mayer, R. MedAdNews, 2005, May.
8. Y.W. Alelyunas, R. Liu, L. Pelosi-Kilby, and C. Shen Eur. J. Pharm. Sci. 37 2009 172
9. A. Berson, V. Descatoire, A. Sutton, D. Fau, B. Maulny, N. Vadrot, G. Feldmann, B. Berthon, T. Tordjmann, and D. Pessayre J. Pharmacol. Exp. Ther. 299 2001 793
10. http://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/2007/ucm108877. htm, accessed 2010, August.
11. http://en.wikipedia.org/wiki/Nefazodone#cite-note-pi-1, accessed 2010, August.
12. www.moleculardevices.com/pages/instruments/px-herg-screening.html, accessed 2010, August.
13. J.S. Silvestre, and J.R. Prous Methods Find Exp. Clin. Pharmacol. 29 2007 457
14. M. Recanatini, E. Poluzzi, M. Masetti, A. Cavalli, and F. De Ponti Med. Res. Rev. 25 2005 133
15. http://www.fda.gov/Safety/MedWatch/SafetyInformation/ SafetyAlertsforHumanMedicalProducts/ucm170899.htm, accessed 2010, August.
16. http://www.fda.gov/Drugs/DrugSafety/ PostmarketDrugSafetyInformationforPatientsandProviders/ucm151088.htm, accessed 2010, August.
17. N. Jain, and S.H. Yalkowsky J. Pharm. Sci. 90 2001 234
18. F. Yoshida, and J.G. Topliss J. Med. Chem. 43 2000 2575
19. K. Yamazaki, and M. Kanaoka J. Pharm. Sci. 93 2004 1480
20. R.P. Austin, P. Barton, S.L. Cockroft, M.C. Wenlock, and R.J. Riley Drug Metab. Dispos. 30 2002 1497
21. R.P. Austin, P. Barton, S. Mohmed, and R.J. Riley Drug Metab. Dispos. 33 2005 419
22. J.D. Hughes, J. Blagg, D.A. Price, S. Bailey, G.A. DeCrescenzo, R.V. Devraj, E. Ellsworth, Y.M. Fobian, M.E. Gibbs, R.W. Gilles, N. Greene, E. Huang, T. Krieger-Burke, J. Loesel, T. Wager, L. Whiteley, and Y. Zhang Bioorg. Med. Chem. Lett. 18 2008 4872
23. K.A. Radcliffe, and W.W. Campbell Curr. Neurol. Neurosci. Rep. 8 2008 66
24. M. Ishigami, T. Honda, W. Takasaki, T. Ikeda, T. Komai, K. Ito, and Y.A. Sugiyama Drug Metab. Dispos. 29 2001 282
25. http://www.fda.gov/medwAtch/SAFETY/2001/Baycol2.htm, accessed 2010, August.
26. L. Stryer Biochemistry 1981 Freeman and Company p 110
27. N. Jain, G. Yang, S.G. Machatha, and S.H. Yalkowsky Int. J. Pharm. 319 2006 169
28. B. Puschner, R.H. Poppenga, L.J. Lowenstine, M.S. Filigenzi, and P.A. Pesavento J. Vet. Diagn. Invest. 19 2007 616
29. U.S. Patent 20040018236.
30. http://www.drugbank.ca, accessed 2010, October.
31. J.C. Shah, and M. Maniarb J. Control. Release 23 1993 261
32. D. Gondaliya, and K. Pundarikakshudu AAPS PharmSciTech. 4 2003 article 3
33. S.D. Roy, and G.L. Flynn Pharm. Res. 6 1989 147
34. L. Fouriea, J.C. Breytenbach, J.D. Plessisa, C. Goosena, H. Swarta, and J. Hadgraftb Int. J. Pharm. 279 2004 59
35. K.A. Levis, M.E. Lane, and O.I. Corrigan Int. J. Pharm. 253 2003 49
36. G. Puglisi, C.A. Ventura, M. Fresta, M.A. Vandelli, and G. Cavallaro J. Inclusion Phenom. Macrocyclic Chem. 24 1996 193
37. R. Mashru, V. Sutariya, M. Sankalia, and J. Sankalia J. Pharm. Pharm. Sci. 8 2005 54
38. Troy, D. B. Remington the Science and Practice of Pharmacy; Lippincott Williams & Wilkins, 2006; p 1505.
39. S.W. Larsen, J. Østergaard, S.V. Poulsen, B. Schulz, and C. Larsen Eur. J. Pharm. Sci. 31 2007 172
40. R. Andersin J. Pharm. Biomed. Anal. 9 1991 451
41. US Patent 20100086589.
42. S. Mutalik, H.S. Parekh, N.M. Davies, and N. Udupa Drug Delivery 16 2009 82
43. M.M. Forsberga, M. Huotaria, J. Savolainenb, and P.T. Männistöa Eur. J. Pharm. Sci. 24 2005 503
44. R.S. Plumb, W.B. Potts, P.D. Rainville, P.G. Alden, D.H. Shave, G. Baynham, and J.R. Mazzeo Rapid Commun. Mass Spectrom. 22 2008 2139