Advances toward new antidepressants beyond SSRIs: 1-Aryloxy-3- piperidinylpropan-2-ols with dual 5-HT1A receptor antagonism/SSRI activities. Part 3

Bioorganic and Medicinal Chemistry Letters

Volumn 13, Issue 22, 2003, Pages 3939-3942

  Takeuchi, Kumiko ^a   Kohn, Todd J ^a   Honigschmidt, Nicholas A ^a   Rocco, Vincent P ^a   Spinazze, Patrick G ^a   Atkinson, Steven T ^a   Hertel, Larry W ^a   Nelson, David L ^a   Wainscott, D Bradley ^a   Ahmad, Laura J ^a   Shaw, Janice ^a   Threlkeld, Penny G ^a   Wong, David T ^a  

^a ELI LILLY AND COMPANY   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ANTIDEPRESSANT AGENT; PIPERIDINE DERIVATIVE; SEROTONIN 1A RECEPTOR; SEROTONIN UPTAKE INHIBITOR;

ARTICLE; DRUG ACTIVITY; DRUG BINDING; DRUG CONFORMATION; DRUG MECHANISM; DRUG STRUCTURE; RECEPTOR BLOCKING; STEREOCHEMISTRY; STRUCTURE ACTIVITY RELATION; STRUCTURE ANALYSIS;

EID: 10744229720     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2003.09.002     Document Type: Article

References (14)

1. Annanth J. Psychother. Psychosom. 67:1998;61.
2. Evrard D.A., Harrison B.L. Annu. Rep. Med. Chem. 34:1999;1.
3. Rutter J.J., Gundlah C., Auerbach S.B. Synapse. 20:1995;225.
4. Tome' M.B., Isaac M.T., Harte R., Holland C. Int. Clin. Psychopharmacol. 12:1997;81.
5. Zanardi R., Artigas F., Franchini L., Sforzini L., Gasperini M., Smeraldi E., Perez J. J. Clin. Psychopharmacol. 17:1997;446.
6. 14.
7. Moreno F.A., Gelenberg A.J., Bachar K., Delgadro P.L. J. Clin. Psychiatry. 58:1997;437.
8. Takeuchi K., Kohn T.J., Honigschmidt N.A., Rocco V.P., Spinazze P.G., Koch D.J., Nelson D.L.G., Wainscott D.B., Ahmad L.J., Shaw J., Threlkeld P.G., Wong D.T. Bioorg. Med. Chem. Lett. 13:2003;1903.
9. Takeuchi K., Kohn T.J., Honigschmidt N.A., Rocco V.P., Spinazze P.G., Koch D.J., Nelson D.L.G., Wainscott D.B., Ahmad L.J., Shaw J., Threlkeld P.G., Wong D.T. Bioorg. Med. Chem. Lett. 13:2003;2393.
10. Meagher K.L., Mewshaw R.E., Evrard D.A., Zhou P., Smith D.L., Scerni R., Spangler T., Abulhawa S., Shi X., Schechter L.E., Andree T.H. Bioorg. Med. Chem. Lett. 11:2001;1885.
11. Orus L., Perez-Silanes S., Oficialdegui A.-M., Martinez-Esparza J., Del Castillo J.-C., Mourelle M., Langer T., Guccione S., Donzella G., Krovat E.M., Poptodorov K., Lasheras B., Ballaz S., Hervias I., Tordera R., Del Rio J., Monge A. J. Med. Chem. 45:2002;4128.
12. 1A receptor with standard assay techniques as previously described: Weinshank R.L., Zgombick J.M., Macchi M.J., Brancheck T.A., Hartig P.R. Proc. Natl. Acad. Sci., U.S.A. 89:1992;3630.
13. Radioligand assays were performed in triplicates, using rat frontal cortex membranes: Wong D.T., Threlkeld P.G., Robertson D.W. Neuropsychopharmacology. 5:1991;43.
14. The method was based on an assay previously described but adapted to a scintillation proximity assay (SPA) format. See: Rasmussen K., Calligaro D.O., Czachura J.F., Dreshfield-Ahmad L.J., Evans D.C., Hemrick-Luecke S.K., Kallman M.J., Kendrick W.T., Leander J.D., Nelson D.L., Overshiner C.D., Wainscott D.B., Wolff M.C., Wong D.T., Brancheck T.A., Zgombick J.M., Xu Y.-C. J. Pharmacol. Exp. Ther. 294:2000;688.