Zobrazeno 1 - 10
of 14
pro vyhledávání: '"Geoffrey Hornby"'
Autor:
Deborah L. Smith, Lee E. Schechter, Michael Z. Kagan, Nicole T. Hatzenbuhler, Amedeo Arturo Failli, Deborah Ann Evrard, Zhang Minsheng, Jeannette Golembieski, Richard Eric Mewshaw, Margaret Lai, Steven Edward Lenicek, Michael Chlenov, Jean Sze, Terrance H. Andree, Dahui Zhou, Annmarie L. Saab, Geoffrey Hornby, Reinhardt Bernhard Baudy, Boyd L. Harrison, Uresh Shantilal Shah, Kelly Sullivan
Publikováno v:
Journal of Medicinal Chemistry. 51:6980-7004
Novel compounds combining a 5-HT 1A moiety (3-aminochroman scaffold) and a 5-HT transporter (indole analogues) linked through a common basic nitrogen via an alkyl chain attached at the 1- or 3-position of the indole were evaluated for dual affinity a
Autor:
Geoffrey Hornby, Valerie Smith, Liza Leventhal, Terrance H. Andree, Kathryn Rogers, Michael R. Brandt
Publikováno v:
Journal of Pharmacology and Experimental Therapeutics. 320:1178-1185
There is increasing recognition that norepinephrine (NE) and serotonin (5-HT) reuptake inhibitors (NRIs and SRIs) are efficacious in treating some types of pain. To date, studies have not systematically evaluated the relative activity at the NE and/o
Autor:
Geoffrey Hornby, Boyd L. Harrison, Deborah L. Smith, Terrance H. Andree, Nicole T. Hatzenbuhler, Kelly Sullivan, Qian Lin, Dahui Zhou, Jennifer Ann Inghrim, Deborah Ann Evrard, Lee E. Schechter, James F. Mattes, Chad E. Beyer, Donna M. Huryn, Richard Eric Mewshaw, Christina M. Kraml
Publikováno v:
Journal of Medicinal Chemistry. 49:4785-4789
Compounds containing a 5-carbamoyl-8-fluoro-3-amino-3,4-dihydro-2H-1-benzopyran and a 3-alkylindole moiety linked through a common basic nitrogen were prepared and evaluated for 5-HT1A affinity, serotonin rat transporter affinity, and functional anta
Autor:
Adam M. Gilbert, Kaapjoo Park, Karen L. Marquis, Guoming Zhang, Geoffrey Hornby, Dmytro Vasylyovych Vasylyev, Mark R. Bowlby, Feng Liu, Terrance H. Andree
Publikováno v:
European Journal of Pharmacology. 536:262-268
Positive allosteric modulators of metabotropic glutamate receptor subtype 5 (mGlu5) have promising therapeutic potential. The effects of selective mGlu5 receptor positive allosteric modulators on signaling molecules in brain slices have not been prev
Autor:
Geoffrey Hornby, Boyd L. Harrison, Lee E. Schechter, Richard Eric Mewshaw, Deborah L. Smith, Terrance H. Andree, Uresh Shantilal Shah, Rosemary Scerni, Kelly Sullivan, Dahui Zhou
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 16:1338-1341
The design, synthesis, and structure-activity relationship of two novel classes of benzoxazine derivatives with dual selective serotonin reuptake inhibitors and 5-HT(1A) receptor activities are described.
Autor:
Gan Zhang, Lisa Potestio, Donna M. Huryn, Stacey J. Sukoff, Deborah L. Smith, Jean Schmid, Terrance H. Andree, Sharon Rosenzweig-Lipson, Lee E. Schechter, Michael G. Kelly, Geoffrey Hornby, Boyd L. Harrison, Douglas M. Ho, Wayne E. Childers, Magid Abou-Gharbia
Publikováno v:
Journal of Medicinal Chemistry. 48:3467-3470
A series of benzodioxanylpiperazine derivatives possessing a 4-aryl amide substituent was prepared and evaluated for 5-HT(1A) affinity and functional antagonist activity in vitro and in vivo. All of the compounds in this series possessed high affinit
Autor:
Lo Jennifer Rebecca, Terrance H. Andree, Deborah Ann Evrard, Adam D. Shilling, Nicole T. Hatzenbuhler, Gary Paul Stack, Qian Lin, Deborah L. Smith, Megan Tran, Jeannette Golembieski, P J Mitchell, Lee E. Schechter, Chad E. Beyer, Dahui Zhou, Christine Huselton, Margaret Lai, Geoffrey Hornby, Boyd L. Harrison, Susan Christman Croce, Amedeo Arturo Failli, Soo Y. Yi
Publikováno v:
Journal of medicinal chemistry. 52(15)
On the basis of the previously reported clinical candidate, SSA-426 (1), a series of related 2-piperazin-1-ylquinoline derivatives 3-16 were synthesized and evaluated as dual-acting serotonin (5-HT) reuptake inhibitors and 5-HT1A receptor antagonists
Autor:
Zhongqi Shen, Geoffrey Hornby, Boyd L. Harrison, Nicole T. Hatzenbuhler, P. Siva Ramamoorthy, Deborah L. Smith, Wayne E. Childers, Kelly Sullivan, Michael Chlenov, Terrance H. Andree, Deborah Ann Evrard, Lee E. Schechter
Publikováno v:
Bioorganicmedicinal chemistry letters. 20(1)
The structure–activity relationship (SAR) for three series of lactam-fused chroman derivatives possessing 3-amino substituents was evaluated. Many compounds exhibited affinities for both the 5-HT1A receptor and the 5-HT transporter. Compounds 45 an
Autor:
Geoffrey Hornby, Kristin Lynne Meagher, Boyd L. Harrison, Terrance H. Andree, Michael A. Webb, Deborah Ann Evrard, Deborah L. Smith, Donna M. Huryn, Jeannette Golembieski, Richard Eric Mewshaw, Ping Zhou, Dahui Zhou, Lee E. Schechter
Publikováno v:
Bioorganicmedicinal chemistry. 16(14)
Based on the previously reported discovery lead, 3-(cis-4-(4-(1H-indol-4-yl)piperazin-1-yl)cyclohexyl)-5-fluoro-1H-indole (2), a series of related arylpiperazin-4-yl-cyclohexyl indole analogs were synthesized then evaluated as 5-HT transporter inhibi
Autor:
Deborah L. Smith, Dahui Zhou, Terrance H. Andree, Jeannette Golembieski, Lee E. Schechter, Geoffrey Hornby, Nicole T. Hatzenbuhler, Boyd L. Harrison, Michael Chlenov, Gary Paul Stack, Deborah Ann Evrard, Jonathan Laird Gross
Publikováno v:
Bioorganicmedicinal chemistry letters. 17(11)
Structural modifications of the initial lead, 3-aminochroman (4), led to the identification of a novel series of pyridyl-fused amino chroman derivatives (5-8) and the structural isomers (9-12). The compounds described were evaluated for dual 5-HT tra