Substituted tetraazaacenaphthylenes as potent CRF1 receptor antagonists for the treatment of depression and anxiety

Bioorganic and Medicinal Chemistry Letters

Volumn 15, Issue 16, 2005, Pages 3713-3716

  St Denis, Y ^a   Di Fabio, R ^a   Bernasconi, G ^a   Castiglioni, E ^a   Contini, S ^a   Donati, D ^a   Fazzolari, E ^a   Gentile, G ^a   Ghirlanda, D ^a   Marchionni, C ^a   Messina, F ^a,b   Micheli, F ^a,b   Pavone, F ^a   Pasquarello, A ^a   Sabbatini, F M ^a   Zampori, M G ^a,c   Arban, R ^a   Vitulli, G ^a  

^a GSK   (Italy)

^b NERVIANO MEDICAL SCIENCES   (Italy)

^c PFIZER GLOBAL RESEARCH AND DEVELOPMENT   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

CORTICOTROPIN RELEASING FACTOR ANTAGONIST; NAPHTHYL GROUP;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANXIETY DISORDER; ARTICLE; BINDING AFFINITY; CONTROLLED STUDY; DEPRESSION; DRUG BIOAVAILABILITY; DRUG POTENCY; DRUG RECEPTOR BINDING; DRUG SYNTHESIS; NONHUMAN; PLASMA CLEARANCE; RAT; STRUCTURE ACTIVITY RELATION; SUBSTITUTION REACTION; TRANQUILIZING ACTIVITY; VOCALIZATION;

ACENAPHTHENES; ANIMALS; ANXIETY; DEPRESSION; DISEASE MODELS, ANIMAL; DRUG EVALUATION, PRECLINICAL; MOLECULAR STRUCTURE; RATS; RATS, WISTAR; RECEPTORS, CORTICOTROPIN-RELEASING HORMONE; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 22844432255     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2005.05.040     Document Type: Article

References (14)

1. J. Fawcett, and R.L. Barkin J. Clin. Psychiat. 58 1997 32
2. C.L. DeVane J. Clin. Psychiat. 61 2000 4
3. W. Wale, J. Spiess, C. Rivier, and J. Rivier Science 213 1981 1394
4. For some recent reviews and opinions on the subject, see P.J. Gilligan, and Y.-W. Li Curr. Opin. Drug Discov. Dev. 7 2004 487
5. E.P. Zorilla, and G.F. Koob Expert Opin. Investig. Drugs 13 2004 799
6. D.W. Schulz, R.S. Mansbach, J. Sprouse, J.P. Braselton, J. Collins, M. Corman, A. Dunaiskis, S. Faraci, A.W. Schmidt, T. Seeger, P. Seymour, F.D. Tingley III, E.N. Winston, Y.L. Chen, and J. Heym Proc. Natl. Acad. Sci. USA 93 1996 10477
7. L. He, P.J. Gilligan, R. Zaczek, L.W. Fitzgerald, J. McElroy, H.S. Shen, J.A. Saye, N.H. Kalin, S. Shelton, D. Christ, G. Trainor, and P. Hartig J. Med. Chem. 43 2000 449
8. J. Saunders, and J. Williams Prog. Med. Chem. 41 2003 195
9. Di Fabio, R.; Micheli, F.; Pasquarello, A.; St-Denis, Y. WO 02/087573 A1, 2002.
10. Di Fabio, R.; Gentile, G.; Haddach, M.; St-Denis, Y.; Williams, J.P. WO 02/094826, 2002.
11. Chen, Y.L. WO 95/33750 A1, 1995.
12. Chen, Y.L. US 5962479 A, 1999.
13. Daicel CHIRALPAK AD; mobile phase: n-hexane/isopropyl alcohol 9:1; flow rate: 6.5 mL/min; detector type: diode array detector (DAD) (225 nm, 292 nm)
14. Rat pups between 9 and 11 days postnatal emit ultrasonic vocalization in response to separation from their mother and littermates. This behavior can reflect a state of distress. This test has been originally proposed by Gardner (J. Pharmacol. Methods, 1985, 14, 181) as a sensitive test for anxiolytic drugs. Benzodiazepines, buspirone, CRF1 antagonists, fluovoxamine, and tianeptine have been reported to be active in this test