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Identification and Characterization of GAL-021 as a Novel Breathing Control Modulator

Golder, Francis J ; Dax, Scott ; Baby, Santhosh M ; Gruber, Ryan ; Hoshi, Toshinori ; Ideo, Courtney ; Kennedy, Andrew ; Peng, Sean ; Puskovic, Veljko ; Ritchie, David ; Woodward, Richard ; Wardle, Robert L ; Van Scott, Michael R ; Mannion, James C ; Macintyre, D Euan

Anesthesiology, November 2015, Vol.123(5), pp.1093-104 [Peer Reviewed Journal]

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Inhibition of soluble epoxide hydrolase attenuates endothelial dysfunction in animal models of diabetes, obesity and hypertension

Zhang, Le-Ning ; Vincelette, Jon ; Chen, Dawn ; Gless, Richard D ; Anandan, Sampath-Kumar ; Rubanyi, Gabor M ; Webb, Heather K ; Macintyre, D. Euan ; Wang, Yi-Xin (Jim)

European Journal of Pharmacology, 01 March 2011, Vol.654(1), pp.68-74 [Peer Reviewed Journal]

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Impaired neuropathic pain responses in mice lacking the chemokine receptor CCR2

Abbadie, Catherine ; Lindia, Jill A ; Cumiskey, Anne Marie ; Peterson, Larry B ; Mudgett, John S ; Bayne, Ellen K ; Demartino, Julie A ; Macintyre, D Euan ; Forrest, Michael J

Proceedings of the National Academy of Sciences of the United States of America, 24 June 2003, Vol.100(13), pp.7947-52 [Peer Reviewed Journal]

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4
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Contribution of the tetrodotoxin-resistant voltage-gated sodium channel NaV1.9 to sensory transmission and nociceptive behavior

Priest, Birgit T ; Murphy, Beth A ; Lindia, Jill A ; Diaz, Carmen ; Abbadie, Catherine ; Ritter, Amy M ; Liberator, Paul ; Iyer, Leslie M ; Kash, Shera F ; Kohler, Martin G ; Kaczorowski, Gregory J ; Macintyre, D Euan ; Martin, William J

Proceedings of the National Academy of Sciences of the United States of America, 28 June 2005, Vol.102(26), pp.9382-7 [Peer Reviewed Journal]

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1-(1-Acetyl-piperidin-4-yl)-3-adamantan-1-yl-urea (AR9281) as a potent, selective, and orally available soluble epoxide hydrolase inhibitor with efficacy in rodent models of hypertension and dysglycemia

Anandan, Sampath-Kumar ; Webb, Heather Kay ; Chen, Dawn ; Wang, Yi-Xin (Jim) ; Aavula, Basker R ; Cases, Sylvaine ; Cheng, Ying ; Do, Zung N ; Mehra, Upasana ; Tran, Vinh ; Vincelette, Jon ; Waszczuk, Joanna ; White, Kathy ; Wong, Kenneth R ; Zhang, Le-Ning ; Jones, Paul D ; Hammock, Bruce D ; Patel, Dinesh V ; Whitcomb, Randall ; Macintyre, D. Euan ; Sabry, James ; Gless, Richard

Bioorganic & Medicinal Chemistry Letters, 2011, Vol.21(3), pp.983-988 [Peer Reviewed Journal]

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The proof of the pudding is in the eating: editorial focus on "Hyperphagia, not hypometabolism, causes early onset obesity in melanocortin-4-receptor knockout mice"

Macintyre, D Euan ; Glueck, Susan B

Physiological genomics, 18 March 2003, Vol.13(1), pp.11-4 [Peer Reviewed Journal]

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7
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Melanin-concentrating hormone 1 receptor-deficient mice are lean, hyperactive, and hyperphagic and have altered metabolism

Marsh, Donald J ; Weingarth, Drew T ; Novi, Dawn E ; Chen, Howard Y ; Trumbauer, Myrna E ; Chen, Airu S ; Guan, Xiao-Ming ; Jiang, Michael M ; Feng, Yue ; Camacho, Ramon E ; Shen, Zhu ; Frazier, Easter G ; Yu, Hong ; Metzger, Joseph M ; Kuca, Stephanie J ; Shearman, Lauren P ; Gopal-Truter, Shobhna ; Macneil, Douglas J ; Strack, Alison M ; Macintyre, D Euan ; Van Der Ploeg, Lex H T ; Qian, Su

Proceedings of the National Academy of Sciences of the United States of America, 05 March 2002, Vol.99(5), pp.3240-5 [Peer Reviewed Journal]

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A role for the melanocortin 4 receptor in sexual function

Van Der Ploeg, Lex H T ; Martin, William J ; Howard, Andrew D ; Nargund, Ravi P ; Austin, Christopher P ; Guan, Xiaoming ; Drisko, Jennifer ; Cashen, Doreen ; Sebhat, Iyassu ; Patchett, Arthur A ; Figueroa, David J ; Dilella, Anthony G ; Connolly, Brett M ; Weinberg, David H ; Tan, Carina P ; Palyha, Oksana C ; Pong, Sheng-Shung ; Macneil, Tanya ; Rosenblum, Charles ; Vongs, Aurawan ; Tang, Rui ; Yu, Hong ; Sailer, Andreas W ; Fong, Tung Ming ; Huang, Cathy ; Tota, Michael R ; Chang, Ray S ; Stearns, Ralph ; Tamvakopoulos, Constantin ; Christ, George ; Drazen, Deborah L ; Spar, Brian D ; Nelson, Randy J ; Macintyre, D Euan

Proceedings of the National Academy of Sciences of the United States of America, 20 August 2002, Vol.99(17), pp.11381-6 [Peer Reviewed Journal]

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9
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Discovery of a piperazine urea based compound as a potent, selective, orally bioavailable melanocortin subtype-4 receptor partial agonist

Hong, Qingmei ; Bakshi, Raman K ; Palucki, Brenda L ; Park, Min K ; Ye, Zhixiong ; He, Shuwen ; Pollard, Patrick G ; Sebhat, Iyassu K ; Liu, Jian ; Guo, Liangqin ; Cashen, Doreen E ; Martin, William J ; Weinberg, David H ; Macneil, Tanya ; Tang, Rui ; Tamvakopoulos, Constantin ; Peng, Qianping ; Miller, Randy R ; Stearns, Ralph A ; Chen, Howard Y ; Chen, Airu S ; Strack, Alison M ; Fong, Tung M ; Macintyre, D. Euan ; Wyvratt, Matthew J ; Nargund, Ravi P

Bioorganic & Medicinal Chemistry Letters, 2011, Vol.21(8), pp.2330-2334 [Peer Reviewed Journal]

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Effects of protein kinase C activation on human platelet cyclic AMP metabolism

Bushfield, Mark ; Hopple, Sara L. ; Gibson, Iain F. ; Murdoch, Fiona A. ; Macintyre, D. Euan

FEBS Letters, 05 October 1987, Vol.222(2), pp.299-304 [Peer Reviewed Journal]

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Effects of sildenafil on erectile activity in mice lacking neuronal or endothelial nitric oxide synthase

Cashen, Doreen E ; Macintyre, D Euan ; Martin, William J

British Journal of Pharmacology, July 2002, Vol.136(5), pp.693-700 [Peer Reviewed Journal]

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12
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The target of ezetimibe is Niemann-Pick C1-Like 1 (NPC1L1)

Garcia-Calvo, Margarita ; Lisnock, Jeanmarie ; Bull, Herbert G ; Hawes, Brian E ; Burnett, Duane A ; Braun, Matthew P ; Crona, James H ; Davis, Harry R ; Dean, Dennis C ; Detmers, Patricia A ; Graziano, Michael P ; Hughes, Meredith ; Macintyre, D Euan ; Ogawa, Anthony ; O'Neill, Kim A ; Iyer, Sai Prasad N ; Shevell, Diane E ; Smith, Marsha M ; Tang, Yui S ; Makarewicz, Amanda M ; Ujjainwalla, Feroze ; Altmann, Scott W ; Chapman, Kevin T ; Thornberry, Nancy A

Proceedings of the National Academy of Sciences of the United States of America, 07 June 2005, Vol.102(23), pp.8132-7 [Peer Reviewed Journal]

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13
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Activation of melanocortin MC(4) receptors increases erectile activity in rats ex copula

Martin, William J ; Mcgowan, Erin ; Cashen, Doreen E ; Gantert, Liza T ; Drisko, Jennifer E ; Hom, Gary J ; Nargund, Ravi ; Sebhat, Iyassu ; Howard, Andrew D ; Van Der Ploeg, Lex H T ; Macintyre, D Euan

European journal of pharmacology, 01 November 2002, Vol.454(1), pp.71-9 [Peer Reviewed Journal]

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14
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Chronic MCH-1 receptor modulation alters appetite, body weight and adiposity in rats

Shearman, Lauren P ; Camacho, Ramon E ; Sloan Stribling, D ; Zhou, Dan ; Bednarek, Maria A ; Hreniuk, Donna L ; Feighner, Scott D ; Tan, Carina P ; Howard, Andrew D ; Van Der Ploeg, Lex H T ; Macintyre, D Euan ; Hickey, Gerard J ; Strack, Alison M

European journal of pharmacology, 15 August 2003, Vol.475(1-3), pp.37-47 [Peer Reviewed Journal]

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15
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Discovery of potent, selective, and orally bioavailable 3 H-spiro[isobenzofuran-1,4′-piperidine] based melanocortin subtype-4 receptor agonists

Guo, Liangqin ; Ye, Zhixiong ; Liu, Jian ; He, Shuwen ; Bakshi, Raman K ; Sebhat, Iyassu K ; Dobbelaar, Peter H ; Hong, Qingmei ; Jian, Tianying ; Dellureficio, James P ; Tsou, Nancy N ; Ball, Richard G ; Weinberg, David H ; Macneil, Tanya ; Tang, Rui ; Tamvakopoulos, Constantin ; Peng, Qianping ; Chen, Howard Y ; Chen, Airu S ; Martin, William J ; Macintyre, D. Euan ; Strack, Alison M ; Fong, Tung M ; Wyvratt, Matthew J ; Nargund, Ravi P

Bioorganic & Medicinal Chemistry Letters, 2010, Vol.20(16), pp.4895-4900 [Peer Reviewed Journal]

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16
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Discovery of a spiroindane based compound as a potent, selective, orally bioavailable melanocortin subtype-4 receptor agonist

He, Shuwen ; Ye, Zhixiong ; Dobbelaar, Peter H ; Sebhat, Iyassu K ; Guo, Liangqin ; Liu, Jian ; Jian, Tianying ; Lai, Yingjie ; Franklin, Christopher L ; Bakshi, Raman K ; Dellureficio, James P ; Hong, Qingmei ; Tsou, Nancy N ; Ball, Richard G ; Cashen, Doreen E ; Martin, William J ; Weinberg, David H ; Macneil, Tanya ; Tang, Rui ; Tamvakopoulos, Constantin ; Peng, Qianping ; Miller, Randy R ; Stearns, Ralph A ; Chen, Howard Y ; Chen, Airu S ; Strack, Alison M ; Fong, Tung M ; Macintyre, D. Euan ; Wyvratt, Matthew J ; Nargund, Ravi P

Bioorganic & Medicinal Chemistry Letters, 2010, Vol.20(7), pp.2106-2110 [Peer Reviewed Journal]

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17
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Effects of the ventilatory stimulant, doxapram on human TASK-3 (KCNK9, K2P9.1) channels and TASK-1 (KCNK3, K2P3.1) channels

Cunningham, Kevin P ; Macintyre, D Euan ; Mathie, Alistair ; Veale, Emma L

Acta physiologica (Oxford, England), 19 August 2019, pp.e13361 [Peer Reviewed Journal]

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18
2( S )-((3,5-Bis(trifluoromethyl)benzyl)oxy)-3( S )-phenyl-4-((3-oxo-1,2,4-triazol- 5-yl)methyl)morpholine ( 1 ):  A Potent, Orally Active, Morpholine-Based Human Neurokinin-1 Receptor Antagonist
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2( S )-((3,5-Bis(trifluoromethyl)benzyl)oxy)-3( S )-phenyl-4-((3-oxo-1,2,4-triazol- 5-yl)methyl)morpholine ( 1 ):  A Potent, Orally Active, Morpholine-Based Human Neurokinin-1 Receptor Antagonist

Hale, Jeffrey J. ; Mills, Sander G. ; Maccoss, Malcolm ; Shah, Shrenik K. ; Qi, Hongbo ; Mathre, David J. ; Cascieri, Margaret A. ; Sadowski, Sharon ; Strader, Catherine D. ; Macintyre, D. Euan ; Metzger, Joseph M.

Journal of Medicinal Chemistry, 01/1996, Vol.39(9), pp.1760-1762 [Peer Reviewed Journal]

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19
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Characterization of a novel and selective cannabinoid CB 1 receptor inverse agonist, Imidazole 24b, in rodents

Shearman, Lauren P ; Stribling, D. Sloan ; Camacho, Ramon E ; Rosko, Kimberly M ; Wang, Junying ; Tong, Sharon ; Feng, Yue ; Marsh, Donald J ; Yu, Hong ; Guan, Xiaoming ; Spann, Stephanie K ; Macneil, Douglas J ; Fong, Tung M ; Metzger, Joseph M ; Goulet, Mark T ; Hagmann, William K ; Plummer, Christopher W ; Finke, Paul E ; Mills, Sander G ; Shah, Shrenik K ; Truong, Quang ; Van Der Ploeg, L.H.T ; Macintyre, D. Euan ; Strack, Alison M

European Journal of Pharmacology, 2008, Vol.579(1), pp.215-224 [Peer Reviewed Journal]

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20
A Potent, Nonpeptidyl 1 H -Quinolone Antagonist for the Gonadotropin-Releasing Hormone Receptor
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A Potent, Nonpeptidyl 1 H -Quinolone Antagonist for the Gonadotropin-Releasing Hormone Receptor

Devita, Robert J. ; Walsh, Thomas F. ; Young, Jonathan R. ; Jiang, Jinlong ; Ujjainwalla, Feroze ; Toupence, Richard B. ; Parikh, Mamta ; Huang, Song X. ; Fair, Jason A. ; Goulet, Mark T. ; Wyvratt, Matthew J. ; Lo, Jane-L. ; Ren, Ning ; Yudkovitz, Joel B. ; Yang, Yi T. ; Cheng, Kang ; Cui, Jisong ; Mount, George ; Rohrer, Susan P. ; Schaeffer, James M. ; Rhodes, Linda ; Drisko, Jennifer E. ; Mcgowan, Erin ; Macintyre, D. Euan ; Vincent, Styliani ; Carlin, Josephine R. ; Cameron, Judith ; Smith, Roy G.

Journal of Medicinal Chemistry, 03/2001, Vol.44(6), pp.917-922 [Peer Reviewed Journal]

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21
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Design and pharmacology of N-(3R)-1,2,3,4-tetrahydroisoquinolinium- 3-ylcarbonyl-(1R)-1-(4-chlorobenzyl)- 2-4-cyclohexyl-4-(1H-1,2,4-triazol- 1-ylmethyl)piperidin-1-yl-2-oxoethylamine (1), a potent, selective, melanocortin subtype-4 receptor agonist

Sebhat, Iyassu K ; Martin, William J ; Ye, Zhixiong ; Barakat, Khaled ; Mosley, Ralph T ; Johnston, David B R ; Bakshi, Raman ; Palucki, Brenda ; Weinberg, David H ; Macneil, Tanya ; Kalyani, Rubana N ; Tang, Rui ; Stearns, Ralph A ; Miller, Randy R ; Tamvakopoulos, Constantin ; Strack, Alison M ; Mcgowan, Erin ; Cashen, Doreen E ; Drisko, Jennifer E ; Hom, Gary J ; Howard, Andrew D ; Macintyre, D Euan ; Van Der Ploeg, Lex H T ; Patchett, Arthur A ; Nargund, Ravi P

Journal of medicinal chemistry, 10 October 2002, Vol.45(21), pp.4589-93 [Peer Reviewed Journal]

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22
Structural Optimization Affording 2-( R )-(1-( R )-3,5-Bis(trifluoromethyl)phenylethoxy)-3-( S )-(4-fluoro)phenyl-4- (3-oxo-1,2,4-triazol-5-yl)methylmorpholine, a Potent, Orally Active, Long-Acting Morpholine Acetal Human NK-1 Receptor Antagonist
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Structural Optimization Affording 2-( R )-(1-( R )-3,5-Bis(trifluoromethyl)phenylethoxy)-3-( S )-(4-fluoro)phenyl-4- (3-oxo-1,2,4-triazol-5-yl)methylmorpholine, a Potent, Orally Active, Long-Acting Morpholine Acetal Human NK-1 Receptor Antagonist

Hale, Jeffrey J. ; Mills, Sander G. ; Maccoss, Malcolm ; Finke, Paul E. ; Cascieri, Margaret A. ; Sadowski, Sharon ; Ber, Elzbieta ; Chicchi, Gary G. ; Kurtz, Marc ; Metzger, Joseph ; Eiermann, George ; Tsou, Nancy N. ; Tattersall, F. David ; Rupniak, Nadia M. J. ; Williams, Angela R. ; Rycroft, Wayne ; Hargreaves, Richard ; Macintyre, D. Euan

Journal of Medicinal Chemistry, 11/1998, Vol.41(23), pp.4607-4614 [Peer Reviewed Journal]

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23
Discovery of a Potent, Orally Bioavailable β 3 Adrenergic Receptor Agonist, ( R )- N -[4-[2-[[2-Hydroxy-2-(3-pyridinyl)ethyl]amino]ethyl]phenyl]-4-[4-[4-(trifluoromethyl)phenyl]thiazol-2-yl]benzenesulfonamide
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Discovery of a Potent, Orally Bioavailable β 3 Adrenergic Receptor Agonist, ( R )- N -[4-[2-[[2-Hydroxy-2-(3-pyridinyl)ethyl]amino]ethyl]phenyl]-4-[4-[4-(trifluoromethyl)phenyl]thiazol-2-yl]benzenesulfonamide

Mathvink, Robert J. ; Tolman, J. Samuel ; Chitty, Dawn ; Candelore, Mari R. ; Cascieri, Margaret A. ; Colwell, Lawrence F. ; Deng, Liping ; Feeney, William P. ; Forrest, Michael J. ; Hom, Gary J. ; Macintyre, D. Euan ; Miller, Randall R. ; Stearns, Ralph A. ; Tota, Laurie ; Wyvratt, Matthew J. ; Fisher, Michael H. ; Weber, Ann E.

Journal of Medicinal Chemistry, 10/2000, Vol.43(21), pp.3832-3836 [Peer Reviewed Journal]

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24
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Molecular approaches to the discovery of new treatments for obesity

Strader, Catherine D ; Macintyre, D Euan ; Candelore, Mari R ; Parker, Eric M

Current Opinion in Chemical Biology, 1997, Vol.1(2), pp.204-209 [Peer Reviewed Journal]

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25
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Antiobesity efficacy of a novel cannabinoid-1 receptor inverse agonist, N-(1S,2S)-3-(4-chlorophenyl)-2-(3-cyanophenyl)-1-methylpropyl-2-methyl-2-5-(trifluoromethyl)pyridin-2-yloxypropanamide (MK-0364), in rodents

Fong, Tung M ; Guan, Xiao-Ming ; Marsh, Donald J ; Shen, Chun-Pyn ; Stribling, D Sloan ; Rosko, Kim M ; Lao, Julie ; Yu, Hong ; Feng, Yue ; Xiao, Jing C ; Van Der Ploeg, Lex H T ; Goulet, Mark T ; Hagmann, Williams K ; Lin, Linus S ; Lanza, Thomas J ; Jewell, James P ; Liu, Ping ; Shah, Shrenik K ; Qi, Hongbo ; Tong, Xinchun ; Wang, Junying ; Xu, Suoyu S ; Francis, Barbara ; Strack, Alison M ; Macintyre, D Euan ; Shearman, Lauren P

The Journal of pharmacology and experimental therapeutics, June 2007, Vol.321(3), pp.1013-22 [Peer Reviewed Journal]

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26
Phosphorylated Morpholine Acetal Human Neurokinin-1 Receptor Antagonists as Water-Soluble Prodrugs
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Phosphorylated Morpholine Acetal Human Neurokinin-1 Receptor Antagonists as Water-Soluble Prodrugs

Hale, Jeffrey J. ; Mills, Sander G. ; Maccoss, Malcolm ; Dorn, Conrad P. ; Finke, Paul E. ; Budhu, Richard J. ; Reamer, Robert A. ; Huskey, Su-Er W. ; Luffer-Atlas, Debra ; Dean, Brian J. ; Mcgowan, Erin M. ; Feeney, William P. ; Chiu, Shuet-Hing Lee ; Cascieri, Margaret A. ; Chicchi, Gary G. ; Kurtz, Marc M. ; Sadowski, Sharon ; Ber, Elzbieta ; Tattersall, F. David ; Rupniak, Nadia M. J. ; Williams, Angela R. ; Rycroft, Wayne ; Hargreaves, Richard ; Metzger, Joseph M. ; Macintyre, D. Euan

Journal of Medicinal Chemistry, 03/2000, Vol.43(6), pp.1234-1241 [Peer Reviewed Journal]

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27
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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

Bioorganic & Medicinal Chemistry Letters, 2006, Vol.16(17), pp.4497-4503 [Peer Reviewed Journal]

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28
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Lead optimization of 5,6-diarylpyridines as CB1 receptor inverse agonists

Madsen-Duggan, Christina B ; Debenham, John S ; Walsh, Thomas F ; Toupence, Richard B ; Huang, Song X ; Wang, Junying ; Tong, Xinchun ; Lao, Julie ; Fong, Tung M ; Schaeffer, Marie-Therese ; Xiao, Jing Chen ; Huang, Cathy R.-R.C ; Shen, Chun-Pyn ; Stribling, D. Sloan ; Shearman, Lauren P ; Strack, Alison M ; Macintyre, D. Euan ; Van Der Ploeg, Lex H.T ; Goulet, Mark T

Bioorganic & Medicinal Chemistry Letters, 2007, Vol.17(7), pp.2031-2035 [Peer Reviewed Journal]

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29
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Discovery of a novel class of benzazepinone Nav1.7 blockers: Potential treatments for neuropathic pain

Hoyt, Scott B ; London, Clare ; Gorin, David ; Wyvratt, Matthew J ; Fisher, Michael H ; Abbadie, Catherine ; Felix, John P ; Garcia, Maria L ; Li, Xiaohua ; Lyons, Kathryn A ; Mcgowan, Erin ; Macintyre, D. Euan ; Martin, William J ; Priest, Birgit T ; Ritter, Amy ; Smith, Mchardy M ; Warren, Vivien A ; Williams, Brande S ; Kaczorowski, Gregory J ; Parsons, William H

Bioorganic & Medicinal Chemistry Letters, 15 August 2007, Vol.17(16), pp.4630-4634 [Peer Reviewed Journal]

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30
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Benzazepinone Na v1.7 blockers: Potential treatments for neuropathic pain

Hoyt, Scott B ; London, Clare ; Ok, Hyun ; Gonzalez, Edward ; Duffy, Joseph L ; Abbadie, Catherine ; Dean, Brian ; Felix, John P ; Garcia, Maria L ; Jochnowitz, Nina ; Karanam, Bindhu V ; Li, Xiaohua ; Lyons, Kathryn A ; Mcgowan, Erin ; Macintyre, D. Euan ; Martin, William J ; Priest, Birgit T ; Smith, Mchardy M ; Tschirret-Guth, Richard ; Warren, Vivien A ; Williams, Brande S ; Kaczorowski, Gregory J ; Parsons, William H

Bioorganic & Medicinal Chemistry Letters, 2007, Vol.17(22), pp.6172-6177 [Peer Reviewed Journal]

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31
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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

Bioorganic & Medicinal Chemistry Letters, 2006, Vol.16(17), pp.4504-4511 [Peer Reviewed Journal]

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32
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Synthesis of functionalized 1,8-naphthyridinones and their evaluation as novel, orally active CB1 receptor inverse agonists

Debenham, John S ; Madsen-Duggan, Christina B ; Walsh, Thomas F ; Wang, Junying ; Tong, Xinchun ; Doss, George A ; Lao, Julie ; Fong, Tung M ; Schaeffer, Marie-Therese ; Xiao, Jing Chen ; Huang, Cathy R.-R.C ; Shen, Chun-Pyn ; Feng, Yue ; Marsh, Donald J ; Stribling, D. Sloan ; Shearman, Lauren P ; Strack, Alison M ; Macintyre, D. Euan ; Van Der Ploeg, Lex H.T ; Goulet, Mark T

Bioorganic & Medicinal Chemistry Letters, 2006, Vol.16(3), pp.681-685 [Peer Reviewed Journal]

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33
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Discovery of (2 S)- N-[(1 R)-2-[4-cyclohexyl-4-[[(1,1-dimethylethyl)amino]carbonyl]-1-piperidinyl]-1-[(4-fluorophenyl)methyl]-2-oxoethyl]-4-methyl-2-piperazinecarboxamide (MB243), a potent and selective melanocortin subtype-4 receptor agonist

Palucki, Brenda L ; Park, Min K ; Nargund, Ravi P ; Ye, Zhixiong ; Sebhat, Iyassu K ; Pollard, Patrick G ; Kalyani, Rubana N ; Tang, Rui ; Macneil, Tanya ; Weinberg, David H ; Vongs, Aurawan ; Rosenblum, Charles I ; Doss, George A ; Miller, Randall R ; Stearns, Ralph A ; Peng, Qianping ; Tamvakopoulos, Constantin ; Mcgowan, Erin ; Martin, William J ; Metzger, Joseph M ; Shepherd, Cherrie A ; Strack, Alison M ; Macintyre, D. Euan ; Van Der Ploeg, Lex H.T ; Patchett, Arthur A

Bioorganic & Medicinal Chemistry Letters, 2005, Vol.15(1), pp.171-175 [Peer Reviewed Journal]

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34
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Discovery and activity of (1 R,4 S,6 R)- N-[(1 R)-2-[4-cyclohexyl-4-[[(1,1-dimethylethyl)amino]carbonyl]-1-piperidinyl]-1-[(4-fluorophenyl)methyl]-2-oxoethyl]-2-methyl-2-azabicyclo[2.2.2]octane-6-carboxamide (3, RY764), a potent and selective melanocortin subtype-4 receptor agonist

Ye, Zhixiong ; Guo, Liangqin ; Barakat, Khaled J ; Pollard, Patrick G ; Palucki, Brenda L ; Sebhat, Iyassu K ; Bakshi, Raman K ; Tang, Rui ; Kalyani, Rubana N ; Vongs, Aurawan ; Chen, Airu S ; Chen, Howard Y ; Rosenblum, Charles I ; Macneil, Tanya ; Weinberg, David H ; Peng, Qianping ; Tamvakopoulos, Constantin ; Miller, Randy R ; Stearns, Ralph A ; Cashen, Doreen E ; Martin, William J ; Metzger, Joseph M ; Strack, Alison M ; Macintyre, D. Euan ; Van Der Ploeg, Lex H.T ; Patchett, Arthur A ; Wyvratt, Matthew J ; Nargund, Ravi P

Bioorganic & Medicinal Chemistry Letters, 2005, Vol.15(15), pp.3501-3505 [Peer Reviewed Journal]

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35
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Melanocortin receptors and erectile function

Martin, William J ; Macintyre, D Euan

European urology, June 2004, Vol.45(6), pp.706-13 [Peer Reviewed Journal]

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