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A G protein-biased ligand at the μ-opioid receptor is potently analgesic with reduced gastrointestinal and respiratory dysfunction compared with morphine.
DeWire SM, Yamashita DS, Rominger DH, Liu G, Cowan CL, Graczyk TM, Chen XT, Pitis PM, Gotchev D, Yuan C, Koblish M, Lark MW, Violin JD. DeWire SM, et al. Among authors: yuan c. J Pharmacol Exp Ther. 2013 Mar;344(3):708-17. doi: 10.1124/jpet.112.201616. Epub 2013 Jan 8. J Pharmacol Exp Ther. 2013. PMID: 23300227
Structure-activity relationships and discovery of a G protein biased μ opioid receptor ligand, [(3-methoxythiophen-2-yl)methyl]({2-[(9R)-9-(pyridin-2-yl)-6-oxaspiro-[4.5]decan-9-yl]ethyl})amine (TRV130), for the treatment of acute severe pain.
Chen XT, Pitis P, Liu G, Yuan C, Gotchev D, Cowan CL, Rominger DH, Koblish M, Dewire SM, Crombie AL, Violin JD, Yamashita DS. Chen XT, et al. Among authors: yuan c. J Med Chem. 2013 Oct 24;56(20):8019-31. doi: 10.1021/jm4010829. Epub 2013 Oct 14. J Med Chem. 2013. PMID: 24063433
Discovery of potent nonpeptide vitronectin receptor (alpha v beta 3) antagonists.
Keenan RM, Miller WH, Kwon C, Ali FE, Callahan JF, Calvo RR, Hwang SM, Kopple KD, Peishoff CE, Samanen JM, Wong AS, Yuan CK, Huffman WF. Keenan RM, et al. Among authors: yuan ck. J Med Chem. 1997 Jul 18;40(15):2289-92. doi: 10.1021/jm970205r. J Med Chem. 1997. PMID: 9240343 No abstract available.
Potent, selective, orally active 3-oxo-1,4-benzodiazepine GPIIb/IIIa integrin antagonists.
Samanen JM, Ali FE, Barton LS, Bondinell WE, Burgess JL, Callahan JF, Calvo RR, Chen W, Chen L, Erhard K, Feuerstein G, Heys R, Hwang SM, Jakas DR, Keenan RM, Ku TW, Kwon C, Lee CP, Miller WH, Newlander KA, Nichols A, Parker M, Peishoff CE, Rhodes G, Ross S, Shu A, Simpson R, Takata D, Yellin TO, Uzsinskas I, Venslavsky JW, Yuan CK, Huffman WF. Samanen JM, et al. Among authors: yuan ck. J Med Chem. 1996 Dec 6;39(25):4867-70. doi: 10.1021/jm960558a. J Med Chem. 1996. PMID: 8960544 No abstract available.
7,753 results