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Synthesis and Pharmacological Characterization of 2-(2,6-Dichlorophenyl)-1-((1S,3R)-5-(3-hydroxy-3-methylbutyl)-3-(hydroxymethyl)-1-methyl-3,4-dihydroisoquinolin-2(1H)-yl)ethan-1-one (LY3154207), a Potent, Subtype Selective, and Orally Available Positive Allosteric Modulator of the Human Dopamine D1 Receptor.
Hao J, Beck JP, Schaus JM, Krushinski JH, Chen Q, Beadle CD, Vidal P, Reinhard MR, Dressman BA, Massey SM, Boulet SL, Cohen MP, Watson BM, Tupper D, Gardinier KM, Myers J, Johansson AM, Richardson J, Richards DS, Hembre EJ, Remick DM, Coates DA, Bhardwaj RM, Diseroad BA, Bender D, Stephenson G, Wolfangel CD, Diaz N, Getman BG, Wang XS, Heinz BA, Cramer JW, Zhou X, Maren DL, Falcone JF, Wright RA, Mitchell SN, Carter G, Yang CR, Bruns RF, Svensson KA. Hao J, et al. Among authors: krushinski jh. J Med Chem. 2019 Oct 10;62(19):8711-8732. doi: 10.1021/acs.jmedchem.9b01234. Epub 2019 Sep 30. J Med Chem. 2019. PMID: 31532644
An Allosteric Potentiator of the Dopamine D1 Receptor Increases Locomotor Activity in Human D1 Knock-In Mice without Causing Stereotypy or Tachyphylaxis.
Svensson KA, Heinz BA, Schaus JM, Beck JP, Hao J, Krushinski JH, Reinhard MR, Cohen MP, Hellman SL, Getman BG, Wang X, Menezes MM, Maren DL, Falcone JF, Anderson WH, Wright RA, Morin SM, Knopp KL, Adams BL, Rogovoy B, Okun I, Suter TM, Statnick MA, Gehlert DR, Nelson DL, Lucaites VL, Emkey R, DeLapp NW, Wiernicki TR, Cramer JW, Yang CR, Bruns RF. Svensson KA, et al. Among authors: krushinski jh. J Pharmacol Exp Ther. 2017 Jan;360(1):117-128. doi: 10.1124/jpet.116.236372. Epub 2016 Nov 3. J Pharmacol Exp Ther. 2017. PMID: 27811173 Free PMC article.
Discovery of selective N-[3-(1-methyl-piperidine-4-carbonyl)-phenyl]-benzamide-based 5-HT₁ F receptor agonists: Evolution from bicyclic to monocyclic cores.
Zhang D, Blanco MJ, Ying BP, Kohlman D, Liang SX, Victor F, Chen Q, Krushinski J, Filla SA, Hudziak KJ, Mathes BM, Cohen MP, Zacherl D, Nelson DL, Wainscott DB, Nutter SE, Gough WH, Schaus JM, Xu YC. Zhang D, et al. Among authors: krushinski j. Bioorg Med Chem Lett. 2015 Oct 1;25(19):4337-41. doi: 10.1016/j.bmcl.2015.07.042. Epub 2015 Jul 22. Bioorg Med Chem Lett. 2015. PMID: 26271587
Indoloxypropanolamine analogues as 5-HT(1A) receptor antagonists.
Krushinski JH Jr, Schaus JM, Thompson DC, Calligaro DO, Nelson DL, Luecke SH, Wainscott DB, Wong DT. Krushinski JH Jr, et al. Bioorg Med Chem Lett. 2007 Oct 15;17(20):5600-4. doi: 10.1016/j.bmcl.2007.07.086. Epub 2007 Aug 22. Bioorg Med Chem Lett. 2007. PMID: 17804228
The PET radioligand [11C]MePPEP binds reversibly and with high specific signal to cannabinoid CB1 receptors in nonhuman primate brain.
Yasuno F, Brown AK, Zoghbi SS, Krushinski JH, Chernet E, Tauscher J, Schaus JM, Phebus LA, Chesterfield AK, Felder CC, Gladding RL, Hong J, Halldin C, Pike VW, Innis RB. Yasuno F, et al. Among authors: krushinski jh. Neuropsychopharmacology. 2008 Jan;33(2):259-69. doi: 10.1038/sj.npp.1301402. Epub 2007 Mar 28. Neuropsychopharmacology. 2008. PMID: 17392732
35 results