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APD791, 3-Methoxy-N-(3-(1-methyl-1H-pyrazol-5-yl)-4-(2-morpholinoethoxy)phenyl)benzamide, a Novel 5-Hydroxytryptamine 2A Receptor Antagonist: Pharmacological Profile, Pharmacokinetics, Platelet Activity and Vascular Biology
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Effects of a niacin receptor partial agonist, MK-0354, on plasma free fatty acids, lipids, and cutaneous flushing in humans
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Published in Science (American Association for the Advancement of Science) (08.12.1989)
Published in Science (American Association for the Advancement of Science) (08.12.1989)
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Niacin lipid efficacy is independent of both the niacin receptor GPR109A and free fatty acid suppression
Lauring, Brett, Taggart, Andrew K P, Tata, James R, Dunbar, Richard, Caro, Luzelena, Cheng, Kang, Chin, Jayne, Colletti, Steven L, Cote, Josee, Khalilieh, Sauzanne, Liu, Jiajun, Luo, Wen-Lin, Maclean, Alexandra A, Peterson, Laurence B, Polis, Adam B, Sirah, Waheeda, Wu, Tsuei-Ju, Liu, Xuan, Jin, Lan, Wu, Kenneth, Boatman, P Douglas, Semple, Graeme, Behan, Dominic P, Connolly, Daniel T, Lai, Eseng, Wagner, John A, Wright, Samuel D, Cuffie, Cynthia, Mitchel, Yale B, Rader, Daniel J, Paolini, John F, Waters, M Gerard, Plump, Andrew
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Inhibition of Mas G-protein signaling improves coronary blood flow, reduces myocardial infarct size, and provides long-term cardioprotection
Zhang, Tong, Li, Zhuangjie, Dang, Huong, Chen, Ruoping, Liaw, Chen, Tran, Thuy-Anh, Boatman, P Douglas, Connolly, Daniel T, Adams, John W
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(1aR,5aR)1a,3,5,5a-Tetrahydro-1H-2,3-diaza-cyclopropa[a]pentalene-4-carboxylic Acid (MK-1903): A Potent GPR109a Agonist that Lowers Free Fatty Acids in Humans
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3-(1H-Tetrazol-5-yl)-1,4,5,6-tetrahydro-cyclopentapyrazole (MK-0354): A Partial Agonist of the Nicotinic Acid Receptor, G-Protein Coupled Receptor 109a, with Antilipolytic but No Vasodilatory Activity in Mice
Semple, Graeme, Skinner, Philip J, Gharbaoui, Tawfik, Shin, Young-Jun, Jung, Jae-Kyu, Cherrier, Martin C, Webb, Peter J, Tamura, Susan Y, Boatman, P. Douglas, Sage, Carleton R, Schrader, Thomas O, Chen, Ruoping, Colletti, Steven L, Tata, James R, Waters, M. Gerard, Cheng, Kang, Taggart, Andrew K, Cai, Tian-Quan, Carballo-Jane, Ester, Behan, Dominic P, Connolly, Daniel T, Richman, Jeremy G
Published in Journal of medicinal chemistry (28.08.2008)
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Inhibition of cholesteryl ester transfer protein by substituted dithiobisnicotinic acid dimethyl ester: involvement Of a critical cysteine
Hope, H R, Heuvelman, D, Duffin, K, Smith, C, Zablocki, J, Schilling, R, Hegde, S, Lee, L, Witherbee, B, Baganoff, M, Bruce, C, Tall, A R, Krul, E, Glenn, K, Connolly, D T
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Analogues of Acifran: Agonists of the High and Low Affinity Niacin Receptors, GPR109a and GPR109b
Jung, Jae-Kyu, Johnson, Benjamin R, Duong, Tracy, Decaire, Marc, Uy, Jane, Gharbaoui, Tawfik, Boatman, P. Douglas, Sage, Carleton R, Chen, Ruoping, Richman, Jeremy G, Connolly, Daniel T, Semple, Graeme
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5-N,N-Disubstituted 5-aminopyrazole-3-carboxylic acids are highly potent agonists of GPR109b
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Published in Bioorganic & medicinal chemistry letters (01.08.2009)
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Discovery and Structure−Activity Relationship of 3-Methoxy-N-(3-(1-methyl-1H-pyrazol-5-yl)-4-(2-morpholinoethoxy)phenyl)benzamide (APD791): A Highly Selective 5-Hydroxytryptamine2A Receptor Inverse Agonist for the Treatment of Arterial Thrombosis
Xiong, Yifeng, Teegarden, Bradley R, Choi, Jin-Sun Karoline, Strah-Pleynet, Sonja, Decaire, Marc, Jayakumar, Honnappa, Dosa, Peter I, Casper, Martin D, Pham, Lan, Feichtinger, Konrad, Ullman, Brett, Adams, John, Yuskin, Diane, Frazer, John, Morgan, Michael, Sadeque, Abu, Chen, Weichao, Webb, Robert R, Connolly, Daniel T, Semple, Graeme, Al-Shamma, Hussien
Published in Journal of medicinal chemistry (10.06.2010)
Published in Journal of medicinal chemistry (10.06.2010)
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Anti-thrombotic and vascular effects of AR246686, a novel 5-HT2A receptor antagonist
ADAMS, John W, RAMIREZ, Juan, BEHAN, Dominic P, CONNOLLY, Daniel T, ORTUNO, Danny, YUNQING SHI, THOMSEN, William, RICHMAN, Jeremy G, MORGAN, Michael, DOSA, Peter, TEEGARDEN, Bradley R, AL-SHAMMA, Hussien
Published in European journal of pharmacology (31.05.2008)
Published in European journal of pharmacology (31.05.2008)
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