Modulation of basal and stress-induced amygdaloid substance P release by the potent and selective NK1 receptor antagonist L-822429
Singewald, Nicolas, Chicchi, Gary G, Thurner, Clemens C, Tsao, Kwei-Lan, Spetea, Mariana, Schmidhammer, Helmut, Sreepathi, Hari Kishore, Ferraguti, Francesco, Singewald, Georg M, Ebner, Karl
Published in Journal of neurochemistry (01.09.2008)
Published in Journal of neurochemistry (01.09.2008)
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Potent, Brain-Penetrant, Hydroisoindoline-Based Human Neurokinin-1 Receptor Antagonists
Jiang, Jinlong, Bunda, Jaime L, Doss, Geoge A, Chicchi, Gary G, Kurtz, Marc M, Tsao, Kwei-Lan C, Tong, Xinchun, Zheng, Song, Upthagrove, Alana, Samuel, Koppara, Tschirret-Guth, Richard, Kumar, Sanjeev, Wheeldon, Alan, Carlson, Emma J, Hargreaves, Richard, Burns, Donald, Hamill, Terence, Ryan, Christine, Krause, Stephen M, Eng, WaiSi, DeVita, Robert J, Mills, Sander G
Published in Journal of medicinal chemistry (14.05.2009)
Published in Journal of medicinal chemistry (14.05.2009)
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Fused bicyclic pyrrolizinones as new scaffolds for human NK1 antagonists
Morriello, Gregori J, Devita, Robert J, Mills, Sander G, Young, Jonathan R, Lin, Peter, Doss, George, Chicchi, Gary G, Demartino, Julie, Kurtz, Marc M, Tsao, Kwei-Lan C, Carlson, Emma, Townson, Karen, Wheeldon, Alan, Boyce, Susan, Collinson, Neil, Rupniak, Nadia, Moore, Stephen
Published in Bioorganic & medicinal chemistry (01.03.2008)
Published in Bioorganic & medicinal chemistry (01.03.2008)
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Tetrahydroindolizinone NK1 antagonists
JIANMING BAO, HUAGANG LU, MILLS, Sander G, DEVITA, Robert J, MORRIELLO, Gregori J, CARLSON, Emma J, WHEELDON, Alan, CHICCHI, Gary G, KURTZ, Marc M, TSAO, Kwei-Lan C, SONG ZHENG, XINCHUN TONG
Published in Bioorganic & medicinal chemistry letters (01.04.2010)
Published in Bioorganic & medicinal chemistry letters (01.04.2010)
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Pyrrolidine-carboxamides and oxadiazoles as potent hNK1 antagonists
YOUNG, Jonathan R, EID, Ronsar, TURNER, Cherilyn, DEVITA, Robert J, KURTZ, Marc M, TSAO, Kwei-Lan C, CHICCHI, Gary G, WHEELDON, Alan, CARLSON, Emma, MILLS, Sander G
Published in Bioorganic & medicinal chemistry letters (01.10.2007)
Published in Bioorganic & medicinal chemistry letters (01.10.2007)
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The discovery of potent, selective, and orally bioavailable hNK1 antagonists derived from pyrrolidine
LIN, Peter, LEHUA CHANG, KURTZ, Marc M, TSAO, Kwei-Lan C, WHEELDON, Alan, CARLSON, Emma J, ENG, Waisi, BURNS, H. Donald, HARGREAVES, Richard J, MILLS, Sander G, DEVITA, Robert J, YOUNG, Jonathan R, EID, Ronsar, XINCHUN TONG, SONG ZHENG, BALL, Richard G, TSOU, Nancy N, CHICCHI, Gary G
Published in Bioorganic & medicinal chemistry letters (15.09.2007)
Published in Bioorganic & medicinal chemistry letters (15.09.2007)
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Synthesis and structure-activity relationships of 8-azabicyclo[3.2.1]octane benzylamine NK1 antagonists
THOMSON, Christopher G, CARLSON, Emma, CHICCHI, Gary G, KULAGOWSKI, Janusz J, KURTZ, Marc M, SWAIN, Christopher J, TSAO, Kwei-Lan C, WHEELDON, Alan
Published in Bioorganic & medicinal chemistry letters (15.02.2006)
Published in Bioorganic & medicinal chemistry letters (15.02.2006)
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Cyclopentane-based human NK1 antagonists. Part 2: Development of potent, orally active, water-soluble derivatives
Meurer, Laura C., Finke, Paul E., Owens, Karen A., Tsou, Nancy N., Ball, Richard G., Mills, Sander G., MacCoss, Malcolm, Sadowski, Sharon, Cascieri, Margaret A., Tsao, Kwei-Lan, Chicchi, Gary G., Egger, Linda A., Luell, Silvi, Metzger, Joseph M., MacIntyre, D. Euan, Rupniak, Nadia M.J., Williams, Angela R., Hargreaves, Richard J.
Published in Bioorganic & medicinal chemistry letters (01.09.2006)
Published in Bioorganic & medicinal chemistry letters (01.09.2006)
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Discovery and Pharmacology of a Novel Somatostatin Subtype 5 (SSTR5) Antagonist: Synergy with DPP‑4 Inhibition
Liu, Weiguo, Shao, Pengcheng P, Liang, Gui-Bai, Bawiec, John, He, Jiafang, Aster, Susan D, Wu, Margaret, Chicchi, Garry, Wang, John, Tsao, Kwei-Lan, Shang, Jin, Salituro, Gino, Zhou, Yun-Ping, Li, Cai, Akiyama, Taro E, Metzger, Daniel E, Murphy, Beth Ann, Howard, Andrew D, Weber, Ann E, Duffy, Joseph L
Published in ACS medicinal chemistry letters (08.11.2018)
Published in ACS medicinal chemistry letters (08.11.2018)
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SAR exploration at the C-3 position of tetrahydro-β-carboline sstr3 antagonists
He, Shuwen, Dobbelaar, Peter H., Guo, Liangqin, Ye, Zhixiong, Liu, Jian, Jian, Tianying, Truong, Quang, Shah, Shrenik K., Du, Wu, Qi, Hongbo, Bakshi, Raman K., Hong, Qingmei, Dellureficio, James D., Sherer, Edward, Pasternak, Alexander, Feng, Zhe, Reibarkh, Mikhail, Lin, Melissa, Samuel, Koppara, Reddy, Vijay B., Mitelman, Stan, Tong, Sharon X., Chicchi, Gary G., Tsao, Kwei-Lan, Trusca, Dorina, Wu, Margaret, Shao, Qing, Trujillo, Maria E., Fernandez, Guillermo, Nelson, Donald, Bunting, Patricia, Kerr, Janet, Fitzgerald, Patrick, Morissette, Pierre, Volksdorf, Sylvia, Eiermann, George J., Li, Cai, Zhang, Bei B., Howard, Andrew D., Zhou, Yun-Ping, Nargund, Ravi P., Hagmann, William K.
Published in Bioorganic & medicinal chemistry letters (15.03.2016)
Published in Bioorganic & medicinal chemistry letters (15.03.2016)
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Solution Structure of the Ras-Binding Domain of c-Raf-1 and Identification of Its Ras Interaction Surface
Emerson, S. Donald, Madison, Vincent S, Palermo, Robert E, Waugh, David S, Scheffler, Julie E, Tsao, Kwei-Lan, Kiefer, Susan E, Liu, Shuang P, Fry, David C
Published in Biochemistry (Easton) (30.05.1995)
Published in Biochemistry (Easton) (30.05.1995)
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2‑[(3aR,4R,5S,7aS)‑5-{(1S)‑1-[3,5-Bis(trifluoromethyl)phenyl]-2-hydroxyethoxy}-4-(2-methylphenyl)octahydro‑2H‑isoindol-2-yl]-1,3-oxazol-4(5H)‑one: A Potent Human NK1 Receptor Antagonist with Multiple Clearance Pathways
Kassick, Andrew J, Jiang, Jinlong, Bunda, Jaime, Wilson, David, Bao, Jianming, Lu, Huagang, Lin, Peter, Ball, Richard G, Doss, George A, Tong, Xinchun, Tsao, Kwei-Lan C, Wang, Hong, Chicchi, Gary, Karanam, Bindhu, Tschirret-Guth, Richard, Samuel, Koppara, Hora, Donald F, Kumar, Sanjeev, Madeira, Maria, Eng, Waisi, Hargreaves, Richard, Purcell, Mona, Gantert, Liza, Cook, Jacquelyn, DeVita, Robert J, Mills, Sander G
Published in Journal of medicinal chemistry (25.07.2013)
Published in Journal of medicinal chemistry (25.07.2013)
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Discovery of substituted (4-phenyl-1H-imidazol-2-yl)methanamine as potent somatostatin receptor 3 agonists
Lai, Zhong, He, Shuwen, Sherer, Edward C., Wu, Zhicai, Yu, Yang, Ball, Richard, Hong, Qingmei, Yang, David X., Guo, Liangqing, Li, Derun, Tuang, Quang, Chicchi, Gary G., Trusca, Dorina, Tsao, Kwei-Lan, Zhou, Yun-Ping, Howard, Andrew D., Nargund, Ravi P., Hagmann, William K.
Published in Bioorganic & medicinal chemistry letters (01.09.2015)
Published in Bioorganic & medicinal chemistry letters (01.09.2015)
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4,4-Disubstituted cyclohexylamine NK1 receptor antagonists II
COOPER, Laura C, CARLSON, Emma J, RYCROFT, Wayne, TSAO, Kwei-Lan, SWAIN, Christopher J, CASTRO, Jose L, CHICCHI, Gary G, DINNELL, Kevin, DI SALVO, Jerry, ELLIOTT, Jason M, HOLLINGWORTH, Gregory J, KURTZ, Marc M, RIDGILL, Mark P
Published in Bioorganic & medicinal chemistry letters (08.07.2002)
Published in Bioorganic & medicinal chemistry letters (08.07.2002)
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Stimulation of Glucose-Dependent Insulin Secretion by a Potent, Selective sst 3 Antagonist
Pasternak, Alexander, Feng, Zhe, de Jesus, Reynalda, Ye, Zhixiong, He, Shuwen, Dobbelaar, Peter, Bradley, Scott A., Chicchi, Gary G., Tsao, Kwei-Lan, Trusca, Dorina, Eiermann, George J., Li, Cai, Feng, Yue, Wu, Margaret, Shao, Qing, Zhang, Bei B., Nargund, Ravi, Mills, Sander G., Howard, Andrew D., Yang, Lihu, Zhou, Yun-Ping
Published in ACS medicinal chemistry letters (12.04.2012)
Published in ACS medicinal chemistry letters (12.04.2012)
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Journal Article
Investigation of Cardiovascular Effects of Tetrahydro-β-carboline sstr3 antagonists
He, Shuwen, Lai, Zhong, Ye, Zhixiong, Dobbelaar, Peter H, Shah, Shrenik K, Truong, Quang, Du, Wu, Guo, Liangqin, Liu, Jian, Jian, Tianying, Qi, Hongbo, Bakshi, Raman K, Hong, Qingmei, Dellureficio, James, Reibarkh, Mikhail, Samuel, Koppara, Reddy, Vijay B, Mitelman, Stan, Tong, Sharon X, Chicchi, Gary G, Tsao, Kwei-Lan, Trusca, Dorina, Wu, Margaret, Shao, Qing, Trujillo, Maria E, Fernandez, Guillermo, Nelson, Donald, Bunting, Patricia, Kerr, Janet, Fitzgerald, Patrick, Morissette, Pierre, Volksdorf, Sylvia, Eiermann, George J, Li, Cai, Zhang, Bei, Howard, Andrew D, Zhou, Yun-Ping, Nargund, Ravi P, Hagmann, William K
Published in ACS medicinal chemistry letters (10.07.2014)
Published in ACS medicinal chemistry letters (10.07.2014)
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Journal Article
Cyclopentane-based human NK1 antagonists. Part 1: Discovery and initial SAR
Finke, Paul E., Meurer, Laura C., Levorse, Dorothy A., Mills, Sander G., MacCoss, Malcolm, Sadowski, Sharon, Cascieri, Margaret A., Tsao, Kwei-Lan, Chicchi, Gary G., Metzger, Joseph M., MacIntyre, D. Euan
Published in Bioorganic & medicinal chemistry letters (01.09.2006)
Published in Bioorganic & medicinal chemistry letters (01.09.2006)
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Journal Article
N',2-Diphenylquinoline-4-carbohydrazide based NK3 receptor antagonists
ELLIOTT, Jason M, CARTING, Robert W, MURRAY, Fraser, RIGBY, Michael, ROYO, Inmaculada, RUSSELL, Michael G. N, SOHAL, Bindi, KWEI LAN TSAO, WILLIAMS, Brian, CHAMBERS, Mark, CHICCHI, Gary G, HUTSON, Peter H, JONES, A. Brian, MACLEOD, Angus, MARWOOD, Rose, MENESES-LORENTE, Georgina, MEZZOGORI, Elena
Published in Bioorganic & medicinal chemistry letters (15.11.2006)
Published in Bioorganic & medicinal chemistry letters (15.11.2006)
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Journal Article
The Discovery of MK-4256, a Potent SSTR3 Antagonist as a Potential Treatment of Type 2 Diabetes
He, Shuwen, Ye, Zhixiong, Truong, Quang, Shah, Shrenik, Du, Wu, Guo, Liangqin, Dobbelaar, Peter H, Lai, Zhong, Liu, Jian, Jian, Tianying, Qi, Hongbo, Bakshi, Raman K, Hong, Qingmei, Dellureficio, James, Pasternak, Alexander, Feng, Zhe, deJesus, Reynalda, Yang, Lihu, Reibarkh, Mikhail, Bradley, Scott A, Holmes, Mark A, Ball, Richard G, Ruck, Rebecca T, Huffman, Mark A, Wong, Frederick, Samuel, Koppara, Reddy, Vijay B, Mitelman, Stan, Tong, Sharon X, Chicchi, Gary G, Tsao, Kwei-Lan, Trusca, Dorina, Wu, Margaret, Shao, Qing, Trujillo, Maria E, Eiermann, George J, Li, Cai, Zhang, Bei B, Howard, Andrew D, Zhou, Yun-Ping, Nargund, Ravi P, Hagmann, William K
Published in ACS medicinal chemistry letters (14.06.2012)
Published in ACS medicinal chemistry letters (14.06.2012)
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