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Page 1
Development of ProTx-II Analogues as Highly Selective Peptide Blockers of Nav1.7 for the Treatment of Pain.
Adams GL, Pall PS, Grauer SM, Zhou X, Ballard JE, Vavrek M, Kraus RL, Morissette P, Li N, Colarusso S, Bianchi E, Palani A, Klein R, John CT, Wang D, Tudor M, Nolting AF, Biba M, Nowak T, Makarov AA, Reibarkh M, Buevich AV, Zhong W, Regalado EL, Wang X, Gao Q, Shahripour A, Zhu Y, de Simone D, Frattarelli T, Pasquini NM, Magotti P, Iaccarino R, Li Y, Solly K, Lee KJ, Wang W, Chen F, Zeng H, Wang J, Regan H, Amin RP, Regan CP, Burgey CS, Henze DA, Sun C, Tellers DM. Adams GL, et al. Among authors: grauer sm. J Med Chem. 2022 Jan 13;65(1):485-496. doi: 10.1021/acs.jmedchem.1c01570. Epub 2021 Dec 21. J Med Chem. 2022. PMID: 34931831
Novel alpha-7 nicotinic acetylcholine receptor agonists containing a urea moiety: identification and characterization of the potent, selective, and orally efficacious agonist 1-[6-(4-fluorophenyl)pyridin-3-yl]-3-(4-piperidin-1-ylbutyl) urea (SEN34625/WYE-103914).
Ghiron C, Haydar SN, Aschmies S, Bothmann H, Castaldo C, Cocconcelli G, Comery TA, Di L, Dunlop J, Lock T, Kramer A, Kowal D, Jow F, Grauer S, Harrison B, La Rosa S, Maccari L, Marquis KL, Micco I, Nencini A, Quinn J, Robichaud AJ, Roncarati R, Scali C, Terstappen GC, Turlizzi E, Valacchi M, Varrone M, Zanaletti R, Zanelli U. Ghiron C, et al. J Med Chem. 2010 Jun 10;53(11):4379-89. doi: 10.1021/jm901692q. J Med Chem. 2010. PMID: 20465311
Tetrahydrocarbazole-based serotonin reuptake inhibitor/dopamine D2 partial agonists for the potential treatment of schizophrenia.
Rotella DP, McFarlane GR, Greenfield A, Grosanu C, Robichaud AJ, Denny RA, Feenstra RW, Núñez-García S, Reinders JH, Neut Mv, McCreary A, Kruse CG, Sullivan K, Pruthi F, Lai M, Zhang J, Kowal DM, Carrick T, Grauer SM, Navarra RL, Graf R, Brennan J, Marquis KL, Pausch MH. Rotella DP, et al. Among authors: grauer sm. Bioorg Med Chem Lett. 2009 Oct 1;19(19):5552-5. doi: 10.1016/j.bmcl.2009.08.050. Epub 2009 Aug 15. Bioorg Med Chem Lett. 2009. PMID: 19720528
Highly potent, selective, and orally active phosphodiesterase 10A inhibitors.
Malamas MS, Ni Y, Erdei J, Stange H, Schindler R, Lankau HJ, Grunwald C, Fan KY, Parris K, Langen B, Egerland U, Hage T, Marquis KL, Grauer S, Brennan J, Navarra R, Graf R, Harrison BL, Robichaud A, Kronbach T, Pangalos MN, Hoefgen N, Brandon NJ. Malamas MS, et al. J Med Chem. 2011 Nov 10;54(21):7621-38. doi: 10.1021/jm2009138. Epub 2011 Oct 11. J Med Chem. 2011. PMID: 21988093
The synthesis and biological evaluation of quinolyl-piperazinyl piperidines as potent serotonin 5-HT1A antagonists.
Childers WE Jr, Havran LM, Asselin M, Bicksler JJ, Chong DC, Grosu GT, Shen Z, Abou-Gharbia MA, Bach AC 3rd, Harrison BL, Kagan N, Kleintop T, Magolda R, Marathias V, Robichaud AJ, Sabb AL, Zhang MY, Andree TH, Aschmies SH, Beyer C, Comery TA, Day M, Grauer SM, Hughes ZA, Rosenzweig-Lipson S, Platt B, Pulicicchio C, Smith DE, Sukoff-Rizzo SJ, Sullivan KM, Adedoyin A, Huselton C, Hirst WD. Childers WE Jr, et al. Among authors: grauer sm. J Med Chem. 2010 May 27;53(10):4066-84. doi: 10.1021/jm1000908. J Med Chem. 2010. PMID: 20443629
Procognitive and neuroprotective activity of a novel alpha7 nicotinic acetylcholine receptor agonist for treatment of neurodegenerative and cognitive disorders.
Roncarati R, Scali C, Comery TA, Grauer SM, Aschmi S, Bothmann H, Jow B, Kowal D, Gianfriddo M, Kelley C, Zanelli U, Ghiron C, Haydar S, Dunlop J, Terstappen GC. Roncarati R, et al. Among authors: grauer sm. J Pharmacol Exp Ther. 2009 May;329(2):459-68. doi: 10.1124/jpet.108.150094. Epub 2009 Feb 17. J Pharmacol Exp Ther. 2009. PMID: 19223665
Preclinical assessment of an adjunctive treatment approach for cognitive impairment associated with schizophrenia using the alpha7 nicotinic acetylcholine receptor agonist WYE-103914/SEN34625.
Marquis KL, Comery TA, Jow F, Navarra RL, Grauer SM, Pulicicchio C, Kelley C, Brennan JA, Roncarati R, Scali C, Haydar S, Ghiron C, Terstappen GC, Dunlop J. Marquis KL, et al. Among authors: grauer sm. Psychopharmacology (Berl). 2011 Dec;218(4):635-47. doi: 10.1007/s00213-011-2357-6. Epub 2011 Jun 4. Psychopharmacology (Berl). 2011. PMID: 21643676
Old and new pharmacology: positive allosteric modulation of the alpha7 nicotinic acetylcholine receptor by the 5-hydroxytryptamine(2B/C) receptor antagonist SB-206553 (3,5-dihydro-5-methyl-N-3-pyridinylbenzo[1,2-b:4,5-b']di pyrrole-1(2H)-carboxamide).
Dunlop J, Lock T, Jow B, Sitzia F, Grauer S, Jow F, Kramer A, Bowlby MR, Randall A, Kowal D, Gilbert A, Comery TA, Larocque J, Soloveva V, Brown J, Roncarati R. Dunlop J, et al. J Pharmacol Exp Ther. 2009 Mar;328(3):766-76. doi: 10.1124/jpet.108.146514. Epub 2008 Dec 2. J Pharmacol Exp Ther. 2009. PMID: 19050173
Novel triazines as potent and selective phosphodiesterase 10A inhibitors.
Malamas MS, Stange H, Schindler R, Lankau HJ, Grunwald C, Langen B, Egerland U, Hage T, Ni Y, Erdei J, Fan KY, Parris K, Marquis KL, Grauer S, Brennan J, Navarra R, Graf R, Harrison BL, Robichaud A, Kronbach T, Pangalos MN, Brandon NJ, Hoefgen N. Malamas MS, et al. Bioorg Med Chem Lett. 2012 Sep 15;22(18):5876-84. doi: 10.1016/j.bmcl.2012.07.076. Epub 2012 Jul 31. Bioorg Med Chem Lett. 2012. PMID: 22902656
26 results