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(a) Borowsky, B.; Durkin, M. M.; Ogozalek, K.; Marzabadi, M. R.; DeLeon, J.; Lagu, B.; Heurich, R.; Lichtblau, H.; Shaposhnik, Z.; Daniewska, I.; Blackburn, T. P.; Branchek, T. A.; Gerald, C.; Vaysse, P. J.; Forray, C. Antidepressant, anxiolytic and anorectic effects of a melanin-concentrating hormone-1 receptor antagonist. Nature Med. 2002, 8, 779-781.
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(b) An orally active small molecule MCHr1 antagonist in an acute feeding model was reported in the following: Takekawa, S.; Asami, A.; Ishihara, Y.; Terauchi, J.; Kato, K.; Shimomura, Y.; Mori, M.; Murakoshi, H.; Kato, K.; Suzuki, N.; Nishimura. O.; Fujino, M. T-226296: A novel, orally active and selective melanin-concentrating hormone receptor antagonist. Eur. J. Pharmacol. 2002. 438, 129-135.
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Identification of 2-(4-benzyloxyphenyl)-N-[1-(2-pyrrolidin-1-yl-ethyl)- 1H-indazol-6-y1]-acetamide, an orally efficacious melanin-concentrating hormone receptor 1 antagonist for the treatment of obesity
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Souers, A. J.; Gao, J.; Brune, M.; Bush, E.; Wodka, D.; Vasudevan, A.; Judd, A. S.; Mulhern, M.; Brodjian, S.; Dayton, B.; Shapiro, R.; Hernandez, L.; Collins, C. A.; Kym, P. R. Identification of 2-(4-benzyloxyphenyl)-N-[1-(2- pyrrolidin-1-yl-ethyl)-1H-indazol-6-y1]-acetamide, an orally efficacious melanin-concentrating hormone receptor 1 antagonist for the treatment of obesity. J. Med. Chem. 2005, 48, 1318-1321.
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Identification of ortho-amino benzamides and nicotinamides as MCHr1 antagonists
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Vasudevan, A.; LaMarche, M. J.; Blackburn, C.; Che, J. L.; Luchaco-Cullis, C. A.; Lai, S.; Marsilje, T. H.; Patane, M. A.; Souers, A. J.; Wodka, D.; Geddes, B.; Chen, S.; Brodjian, S.; Falls, D. H.; Dayton, B. D.; Bush, E.; Brune, M.; Shapiro, R. D.; Marsh, K. C.; Hernandez, L. E.; Sham, H. L.; Collins, C. A.; Kym, P. R.. Identification of ortho-amino benzamides and nicotinamides as MCHr1 antagonists. Bioorg. Med. Chem. Lett. 2005, 15, 4174-4179.
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Vasudevan, A.; Souers, A. J.; Freeman, J. C.; Verzal, M. K.; Gao, J.; Mulhern, M. M.; Wodka, D.; Lynch, J. K.; Engstrom, K. M.; Wagaw, S. H.; Brodjian, S.; Dayton, B.; Falls, D. H.; Bush, E.; Brune, M.; Shapiro, R. D.; Marsh, K. C.; Hernandez, L. E.; Collins, C. A.; Kym, P. R. Aminopiperidine indazoles as orally efficacious melanin concentrating hormone receptor-1 antagonists. Bioorg. Med. Chem. Lett. 2005, 15, 5293-5297.
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(-)-(9S)-9-(3-bromo-4-fluorophenyl)-2,3,5,6,7,9-hexahydrothieno-[3,2-b] quinolin-8(4H)-one 1,1-dioxide (A-278637), a novel ATP-sensitive potassium channel opener: Hemodynamic comparison to ZD-6169, WAY-133537 and nifedipine in the anesthetized canine
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Fryer R. M.; Preusser L. C.; Calzadilla S. C.; Hu Y.; Xu H.; Marsh K. C.; Cox B. F.; Lin C. T.; Gopalakrishnan M.; Reinhart G. A. (-)-(9S)-9-(3-Bromo-4- fluorophenyl)-2,3,5,6,7,9-hexahydrothieno-[3,2-b]quinolin-8(4H)-one 1,1-dioxide (A-278637), a novel ATP-sensitive potassium channel opener: Hemodynamic comparison to ZD-6169, WAY-133537 and nifedipine in the anesthetized canine. J Cardiovasc. Pharmacol. 2004, 44, 137-147.
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84888799533
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Compounds were tested for % inhibition @ 10 μM in a standard panel of 78 receptors and ion channels offered from CEREP (www.cerep.com).
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84888770782
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note
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Screening of 130 MCHr1 antagonists for hERG blockade using cell-based dofetilide binding assays showed no correlation between hERG blockade and hemodynamic effects in vivo.
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19
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Effects of selective dopamine receptor subtype agonists on cardiac contractility and regional haemodynamics in rats
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Predictive, non-GLP models of secondary pharmacodynamics: Putting the best compounds forward
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84888809842
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For studies in anesthetized dogs, the minimum pressure limit tolerated was 50% reduction in the MAP relative to vehicle treated animals. For studies in inactin-anesthetized rats, the minimum pressure limit tolerated was 70 mmHg. This minimum pressure level was implemented to ensure a functional cardiovascular system for the collection of the end-of-study blood sample used for drug plasma level determinations.
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21144448631
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Synthesis and evaluation of urea-based indazoles as melanin-concentrating hormone receptor 1 antagonists for the treatment of obesity
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Souers, A. J.; Gao, J.; Wodka, D.; Judd, A. S.; Mulhern, M. M.; Napier, J. J.; Brune, M. E.; Bush, E. N.; Brodjian, S. J.; Dayton, B. D.; Shapiro, R.; Hernandez, L. E.; Marsh, K. C.; Sham, H. L.; Collins, C. A.; Kym, P. R. Synthesis and evaluation of urea-based indazoles as melanin-concentrating hormone receptor 1 antagonists for the treatment of obesity. Bioorg. Med. Chem. Lett. 2005, 15, 2752-2757.
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Characterization of a neuronal cell line expressing native human melanin-concentrating hormone receptor 1 (MCHr1)
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in press
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Fry, D.; Dayton, B.; Brodjian, S.; Ogiela, C.; Sidorowicz, H.; Frost, L. J.; McNally, T.; Reilly, R. M.; Coffins, C. A. Characterization of a neuronal cell line expressing native human melanin-concentrating hormone receptor 1 (MCHr1). Int. J. Biochem. Cell-Biol. 2006, in press.
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