Discovery of potent, orally bioavailable, selective 5-HT1A/B/D receptor antagonists

被引：10

作者：

Ward, Simon E. ^{[1
]}

Eddershaw, Peter J. ^{[1
]}

Scott, Claire M. ^{[1
]}

Gordon, Laurie J. ^{[1
]}

Lovell, Peter J. ^{[1
]}

Moore, Susan H. ^{[1
]}

Smith, Paul W. ^{[1
]}

Starr, Kathryn R. ^{[1
]}

Thewlis, Kevin M. ^{[1
]}

Watson, Jeannette M. ^{[1
]}

机构：

[1] GlaxoSmithKline, Psychiat Ctr Excellence Drug Discovery & Mol Disc, Harlow CM19 5AW, Essex, England

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2008年 / 51卷 / 10期

关键词：

D O I：

10.1021/jm8001444

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

5-HT1 receptor antagonists have been discovered with good selectivity over the 5-HT transporter. This is the first report of highly potent, selective ligands for the 5-HT1A/B/D receptors with low intrinsic activity, which represent a useful set of molecules for further understanding the roles of the 5-HT1 receptor subtypes and providing new approaches,for the treatment of depression.

引用

页码：2887 / 2890

页数：4

共 50 条

[21] RECEPTOR-BINDING PROFILES OF POTENT AND SELECTIVE 5-HT1A RECEPTOR LIGANDS
TULP, MTM
MOL, F
EUROPEAN JOURNAL OF PHARMACOLOGY, 1990, 183 (03) : 1109 - 1109
[22] The identification of potent, orally bioavailable tricyclic CGRP receptor antagonists
Bell, Ian M.
Bednar, Rodney A.
Corcoran, Halea A.
Fay, John F.
Gallicchio, Steven N.
Johnston, Victor K.
Hershey, James C.
Miller-Stein, Cynthia M.
Moore, Eric L.
Mosser, Scott D.
Roller, Shane A.
Salvatore, Christopher A.
Theberge, Cory R.
Wong, Bradley K.
Zartman, C. Blair
Kane, Stefanie A.
Williams, Theresa M.
Graham, Samuel L.
Vacca, Joseph P.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2009, 19 (16) : 4740 - 4742
[23] Design and synthesis of potent and selective 5-HT1A receptor ligands.
Zhang, G
Palmer, Y
Kelly, MG
Smith, DL
Schechter, LE
ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2000, 220 : U557 - U557
[24] High potent and selective arylpiperazine derivatives as ligands for the 5-HT1A receptor
Modica, M
Santagati, M
Santagati, A
Russo, F
Cagnotto, A
Goegan, M
Mennini, T
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2000, 10 (10) : 1089 - 1092
[25] The discovery of potent, orally bioavailable pyrimidine-5-carbonitrile-6-alkyl CXCR2 receptor, antagonists
Porter, David W.
Bradley, Michelle
Brown, Zarin
Charlton, Steven J.
Cox, Brian
Hunt, Peter
Janus, Diana
Lewis, Sarah
Oakley, Paul
O'Connor, Des
Reilly, John
Smith, Nichola
Press, Neil J.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2014, 24 (15) : 3285 - 3290
[26] Novel 5-HT1A/1B/1D receptors antagonists with potent 5-HT reuptake inhibitory activity
Serafinowska, Halina T.
Blaney, Frank E.
Lovell, Peter J.
Merlo, Giancarlo G.
Scott, Claire M.
Smith, Paul W.
Starr, Kathryn R.
Watson, Jeannette M.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2008, 18 (20) : 5581 - 5585
[27] Discovery and synthesis of a potent, selective and orally bioavailable EP4 receptor agonist
Young, RN
Billot, X
Han, YX
Slipetz, DA
Chauret, N
Belley, M
Metters, K
Mathieu, MC
Greig, GM
Denis, D
Girard, M
HETEROCYCLES, 2004, 64 : 437 - 446
[28] Discovery of novel, potent and orally bioavailable CRTH2 antagonists
Terasaka, Tadashi
Ito, Shinji
Zenkoh, Tatsuya
Hayashida, Hisashi
Matsuda, Hiroshi
Miyata, Junji
Nagata, Hiroshi
Takasuna, Yuji
Kobayashi, Miki
Takeuchi, Makoto
Ohta, Mitsuaki
ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2011, 241
[29] Discovery and optimization of potent, selective, and orally bioavailable Jak1 inhibitors
Zak, Mark
Johnson, Adam
Van Abbema, Anne
Waszkowycz, Bohdan
Eigenbrot, Charles
Chang, Christine
Hurley, Christopher
Hanan, Emily
Kenny, Jane
Kulagowski, Janusz
DeVoss, Jason
Murray, Jeremy
Balazs, Mercedesz
Steffek, Micah
Koehler, Michael
Ghilardi, Nico
Chakravarty, Paroma
Lupardus, Patrick
Gibbons, Paul
Dragovich, Peter
Bergeron, Philippe
Pulk, Rebecca
Mendonca, Rohan
Savage, Scott
Labadie, Sharada
Gradl, Stefan
Ward, Stuart
Blair, Wade
Jia, Wei
ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2012, 243
[30] Potent and selective 5-HT6 receptor antagonists
Bromidge, SM
MEDICINAL CHEMISTRY INTO THE MILLENNIUM, 2001, (264): : 101 - 119

← 1 2 3 4 5 →