Vincent Setola, Ph.D. - Publications

Affiliations: 
Case Western Reserve University, Cleveland Heights, OH, United States 
Area:
Psychopharmacology, 5-HT2A receptors, hallucinogens

54 high-probability publications. We are testing a new system for linking publications to authors. You can help! If you notice any inaccuracies, please sign in and mark papers as correct or incorrect matches. If you identify any major omissions or other inaccuracies in the publication list, please let us know.

Year Citation  Score
2018 Roth BL, Gibbons S, Arunotayanun W, Huang XP, Setola V, Treble R, Iversen L. Correction: The Ketamine Analogue Methoxetamine and 3- and 4-Methoxy Analogues of Phencyclidine Are High Affinity and Selective Ligands for the Glutamate NMDA Receptor. Plos One. 13: e0194984. PMID 29566092 DOI: 10.1371/journal.pone.0194984  0.92
2014 Polepally PR, Huben K, Vardy E, Setola V, Mosier PD, Roth BL, Zjawiony JK. Michael acceptor approach to the design of new salvinorin A-based high affinity ligands for the kappa-opioid receptor. European Journal of Medicinal Chemistry. 85: 818-29. PMID 25193297 DOI: 10.1016/j.ejmech.2014.07.077  0.72
2014 Sampson D, Bricker B, Zhu XY, Peprah K, Lamango NS, Setola V, Roth BL, Ablordeppey SY. Further evaluation of the tropane analogs of haloperidol. Bioorganic & Medicinal Chemistry Letters. 24: 4294-7. PMID 25070422 DOI: 10.1016/j.bmcl.2014.07.018  0.92
2014 Sampson D, Zhu XY, Eyunni SV, Etukala JR, Ofori E, Bricker B, Lamango NS, Setola V, Roth BL, Ablordeppey SY. Identification of a new selective dopamine D4 receptor ligand. Bioorganic & Medicinal Chemistry. 22: 3105-14. PMID 24800940 DOI: 10.1016/j.bmc.2014.04.026  0.72
2014 Kimple AJ, Garland AL, Cohen SP, Setola V, Willard FS, Zielinski T, Lowery RG, Tarran R, Siderovski DP. RGS21, a regulator of taste and mucociliary clearance? The Laryngoscope. 124: E56-63. PMID 23908053 DOI: 10.1002/lary.24326  0.72
2013 Arunotayanun W, Dalley JW, Huang XP, Setola V, Treble R, Iversen L, Roth BL, Gibbons S. An analysis of the synthetic tryptamines AMT and 5-MeO-DALT: emerging 'Novel Psychoactive Drugs'. Bioorganic & Medicinal Chemistry Letters. 23: 3411-5. PMID 23602445 DOI: 10.1016/j.bmcl.2013.03.066  0.72
2013 Roth BL, Gibbons S, Arunotayanun W, Huang XP, Setola V, Treble R, Iversen L. The ketamine analogue methoxetamine and 3- and 4-methoxy analogues of phencyclidine are high affinity and selective ligands for the glutamate NMDA receptor. Plos One. 8: e59334. PMID 23527166 DOI: 10.1371/journal.pone.0059334  0.72
2013 Kokel D, Cheung CY, Mills R, Coutinho-Budd J, Huang L, Setola V, Sprague J, Jin S, Jin YN, Huang XP, Bruni G, Woolf CJ, Roth BL, Hamblin MR, Zylka MJ, et al. Photochemical activation of TRPA1 channels in neurons and animals. Nature Chemical Biology. 9: 257-63. PMID 23396078 DOI: 10.1038/nchembio.1183  0.72
2013 Iversen L, Gibbons S, Treble R, Setola V, Huang XP, Roth BL. Neurochemical profiles of some novel psychoactive substances. European Journal of Pharmacology. 700: 147-51. PMID 23261499 DOI: 10.1016/j.ejphar.2012.12.006  0.72
2013 Wu H, Li J, Fronczek FR, Ferreira D, Burandt CL, Setola V, Roth BL, Zjawiony JK. Labdane diterpenoids from Leonotis leonurus. Phytochemistry. 91: 229-35. PMID 22445074 DOI: 10.1016/j.phytochem.2012.02.021  0.72
2012 Besnard J, Ruda GF, Setola V, Abecassis K, Rodriguiz RM, Huang XP, Norval S, Sassano MF, Shin AI, Webster LA, Simeons FR, Stojanovski L, Prat A, Seidah NG, Constam DB, et al. Automated design of ligands to polypharmacological profiles. Nature. 492: 215-20. PMID 23235874 DOI: 10.1038/nature11691  0.72
2012 Hutcheson JD, Ryzhova LM, Setola V, Merryman WD. 5-HT(2B) antagonism arrests non-canonical TGF-β1-induced valvular myofibroblast differentiation. Journal of Molecular and Cellular Cardiology. 53: 707-14. PMID 22940605 DOI: 10.1016/j.yjmcc.2012.08.012  0.32
2012 Chen X, Sassano MF, Zheng L, Setola V, Chen M, Bai X, Frye SV, Wetsel WC, Roth BL, Jin J. Structure-functional selectivity relationship studies of β-arrestin-biased dopamine Dâ‚‚ receptor agonists. Journal of Medicinal Chemistry. 55: 7141-53. PMID 22845053 DOI: 10.1021/jm300603y  0.72
2012 Mangin F, Dilly S, Joly B, Scuvée-Moreau J, Evans J, Setola V, Roth BL, Liégeois JF. Moderate chemical modifications of WAY-100635 improve the selectivity for 5-HT1A versus D4 receptors. Bioorganic & Medicinal Chemistry Letters. 22: 4550-4. PMID 22738628 DOI: 10.1016/j.bmcl.2012.05.119  0.72
2012 Korboukh I, Hull-Ryde EA, Rittiner JE, Randhawa AS, Coleman J, Fitzpatrick BJ, Setola V, Janzen WP, Frye SV, Zylka MJ, Jin J. Orally active adenosine A(1) receptor agonists with antinociceptive effects in mice. Journal of Medicinal Chemistry. 55: 6467-77. PMID 22738238 DOI: 10.1021/jm3004834  0.72
2012 Gregori-Puigjané E, Setola V, Hert J, Crews BA, Irwin JJ, Lounkine E, Marnett L, Roth BL, Shoichet BK. Identifying mechanism-of-action targets for drugs and probes. Proceedings of the National Academy of Sciences of the United States of America. 109: 11178-83. PMID 22711801 DOI: 10.1073/pnas.1204524109  0.72
2012 Hajjo R, Setola V, Roth BL, Tropsha A. Chemocentric informatics approach to drug discovery: identification and experimental validation of selective estrogen receptor modulators as ligands of 5-hydroxytryptamine-6 receptors and as potential cognition enhancers. Journal of Medicinal Chemistry. 55: 5704-19. PMID 22537153 DOI: 10.1021/jm2011657  0.72
2012 Zhu XY, Etukala JR, Eyunni SV, Setola V, Roth BL, Ablordeppey SY. Benzothiazoles as probes for the 5HT1A receptor and the serotonin transporter (SERT): a search for new dual-acting agents as potential antidepressants. European Journal of Medicinal Chemistry. 53: 124-32. PMID 22520153 DOI: 10.1016/j.ejmech.2012.03.042  0.72
2012 Li J, Fronczek FR, Ferreira D, Burandt CL, Setola V, Roth BL, Zjawiony JK. Bis-spirolabdane diterpenoids from Leonotis nepetaefolia. Journal of Natural Products. 75: 728-34. PMID 22475308 DOI: 10.1021/np3000156  0.72
2012 Peprah K, Zhu XY, Eyunni SV, Etukala JR, Setola V, Roth BL, Ablordeppey SY. Structure-activity relationship studies of SYA 013, a homopiperazine analog of haloperidol. Bioorganic & Medicinal Chemistry. 20: 1671-8. PMID 22336245 DOI: 10.1016/j.bmc.2012.01.022  0.72
2012 Peprah K, Zhu XY, Eyunni SV, Setola V, Roth BL, Ablordeppey SY. Multi-receptor drug design: Haloperidol as a scaffold for the design and synthesis of atypical antipsychotic agents. Bioorganic & Medicinal Chemistry. 20: 1291-7. PMID 22245230 DOI: 10.1016/j.bmc.2011.12.019  0.72
2012 Laggner C, Kokel D, Setola V, Tolia A, Lin H, Irwin JJ, Keiser MJ, Cheung CY, Minor DL, Roth BL, Peterson RT, Shoichet BK. Chemical informatics and target identification in a zebrafish phenotypic screen. Nature Chemical Biology. 8: 144-6. PMID 22179068 DOI: 10.1038/nchembio.732  0.72
2012 Jacobsen JP, Siesser WB, Sachs BD, Peterson S, Cools MJ, Setola V, Folgering JH, Flik G, Caron MG. Deficient serotonin neurotransmission and depression-like serotonin biomarker alterations in tryptophan hydroxylase 2 (Tph2) loss-of-function mice. Molecular Psychiatry. 17: 694-704. PMID 21537332 DOI: 10.1038/mp.2011.50  0.72
2011 Allen JA, Yadav PN, Setola V, Farrell M, Roth BL. Schizophrenia risk gene CAV1 is both pro-psychotic and required for atypical antipsychotic drug actions in vivo. Translational Psychiatry. 1: e33. PMID 22832607 DOI: 10.1038/tp.2011.35  0.72
2011 Allen JA, Yost JM, Setola V, Chen X, Sassano MF, Chen M, Peterson S, Yadav PN, Huang XP, Feng B, Jensen NH, Che X, Bai X, Frye SV, Wetsel WC, et al. Discovery of β-arrestin-biased dopamine D2 ligands for probing signal transduction pathways essential for antipsychotic efficacy. Proceedings of the National Academy of Sciences of the United States of America. 108: 18488-93. PMID 22025698 DOI: 10.1073/pnas.1104807108  0.72
2011 Carlsson J, Coleman RG, Setola V, Irwin JJ, Fan H, Schlessinger A, Sali A, Roth BL, Shoichet BK. Ligand discovery from a dopamine D3 receptor homology model and crystal structure. Nature Chemical Biology. 7: 769-78. PMID 21926995 DOI: 10.1038/nchembio.662  0.72
2011 Whitby LR, Ando Y, Setola V, Vogt PK, Roth BL, Boger DL. Design, synthesis, and validation of a β-turn mimetic library targeting protein-protein and peptide-receptor interactions. Journal of the American Chemical Society. 133: 10184-94. PMID 21609016 DOI: 10.1021/ja201878v  0.72
2011 Hutcheson JD, Setola V, Roth BL, Merryman WD. Serotonin receptors and heart valve disease--it was meant 2B. Pharmacology & Therapeutics. 132: 146-57. PMID 21440001 DOI: 10.1016/j.pharmthera.2011.03.008  0.72
2011 Frankowski KJ, Setola V, Evans JM, Neuenswander B, Roth BL, Aubé J. Synthesis and receptor profiling of Stemona alkaloid analogues reveal a potent class of sigma ligands. Proceedings of the National Academy of Sciences of the United States of America. 108: 6727-32. PMID 21368188 DOI: 10.1073/pnas.1016558108  0.72
2011 Yadav PN, Abbas AI, Farrell MS, Setola V, Sciaky N, Huang XP, Kroeze WK, Crawford LK, Piel DA, Keiser MJ, Irwin JJ, Shoichet BK, Deneris ES, Gingrich J, Beck SG, et al. The presynaptic component of the serotonergic system is required for clozapine's efficacy. Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology. 36: 638-51. PMID 21048700 DOI: 10.1038/npp.2010.195  0.72
2010 Huang XP, Mangano T, Hufeisen S, Setola V, Roth BL. Identification of human Ether-à-go-go related gene modulators by three screening platforms in an academic drug-discovery setting. Assay and Drug Development Technologies. 8: 727-42. PMID 21158687 DOI: 10.1089/adt.2010.0331  0.72
2010 Hajjo R, Grulke CM, Golbraikh A, Setola V, Huang XP, Roth BL, Tropsha A. Development, validation, and use of quantitative structure-activity relationship models of 5-hydroxytryptamine (2B) receptor ligands to identify novel receptor binders and putative valvulopathic compounds among common drugs. Journal of Medicinal Chemistry. 53: 7573-86. PMID 20958049 DOI: 10.1021/jm100600y  0.72
2010 Frankowski KJ, Ghosh P, Setola V, Tran TB, Roth BL, Aubé J. N-Alkyl-octahydroisoquinolin-1-one-8-carboxamides: a Novel Class of Selective, Nonbasic, Nitrogen-Containing κ-Opioid Receptor Ligands. Acs Medicinal Chemistry Letters. 1: 189-193. PMID 20729985 DOI: 10.1021/ml100040t  0.72
2010 Kwon YJ, Saubern S, Macdonald JM, Huang XP, Setola V, Roth BL. N-tetrahydrothiochromenoisoxazole-1-carboxamides as selective antagonists of cloned human 5-HT2B. Bioorganic & Medicinal Chemistry Letters. 20: 5488-90. PMID 20692833 DOI: 10.1016/j.bmcl.2010.07.074  0.72
2009 Setola V. Receptorome screening: a powerful, facile approach to better understand and engineer drugs. Drug News & Perspectives. 22: 459-66. PMID 20016855  0.52
2009 Keiser MJ, Setola V, Irwin JJ, Laggner C, Abbas AI, Hufeisen SJ, Jensen NH, Kuijer MB, Matos RC, Tran TB, Whaley R, Glennon RA, Hert J, Thomas KL, Edwards DD, et al. Predicting new molecular targets for known drugs. Nature. 462: 175-81. PMID 19881490 DOI: 10.1038/nature08506  0.72
2009 Huang XP, Setola V, Yadav PN, Allen JA, Rogan SC, Hanson BJ, Revankar C, Robers M, Doucette C, Roth BL. Parallel functional activity profiling reveals valvulopathogens are potent 5-hydroxytryptamine(2B) receptor agonists: implications for drug safety assessment. Molecular Pharmacology. 76: 710-22. PMID 19570945 DOI: 10.1124/mol.109.058057  0.72
2009 Kimple AJ, Soundararajan M, Hutsell SQ, Roos AK, Urban DJ, Setola V, Temple BR, Roth BL, Knapp S, Willard FS, Siderovski DP. Structural determinants of G-protein alpha subunit selectivity by regulator of G-protein signaling 2 (RGS2). The Journal of Biological Chemistry. 284: 19402-11. PMID 19478087 DOI: 10.1074/jbc.M109.024711  0.72
2009 Hwang JY, Arnold LA, Zhu F, Kosinski A, Mangano TJ, Setola V, Roth BL, Guy RK. Improvement of pharmacological properties of irreversible thyroid receptor coactivator binding inhibitors. Journal of Medicinal Chemistry. 52: 3892-901. PMID 19469546 DOI: 10.1021/jm9002704  0.72
2009 Zolkowska D, Jain R, Rothman RB, Partilla JS, Roth BL, Setola V, Prisinzano TE, Baumann MH. Evidence for the involvement of dopamine transporters in behavioral stimulant effects of modafinil. The Journal of Pharmacology and Experimental Therapeutics. 329: 738-46. PMID 19197004 DOI: 10.1124/jpet.108.146142  0.72
2009 Sikazwe DM, Nkansah NT, Altundas R, Zhu XY, Roth BL, Setola V, Ablordeppey SY. Synthesis and evaluation of ligands for D2-like receptors: the role of common pharmacophoric groups. Bioorganic & Medicinal Chemistry. 17: 1716-23. PMID 19155177 DOI: 10.1016/j.bmc.2008.12.054  0.72
2008 Doly S, Valjent E, Setola V, Callebert J, Hervé D, Launay JM, Maroteaux L. Serotonin 5-HT2B receptors are required for 3,4-methylenedioxymethamphetamine-induced hyperlocomotion and 5-HT release in vivo and in vitro. The Journal of Neuroscience : the Official Journal of the Society For Neuroscience. 28: 2933-40. PMID 18337424 DOI: 10.1523/JNEUROSCI.5723-07.2008  0.72
2006 Davies MA, Setola V, Strachan RT, Sheffler DJ, Salay E, Hufeisen SJ, Roth BL. Pharmacologic analysis of non-synonymous coding h5-HT2A SNPs reveals alterations in atypical antipsychotic and agonist efficacies. The Pharmacogenomics Journal. 6: 42-51. PMID 16314884 DOI: 10.1038/sj.tpj.6500342  0.72
2005 Setola V, Roth BL. Screening the receptorome reveals molecular targets responsible for drug-induced side effects: focus on 'fen-phen'. Expert Opinion On Drug Metabolism & Toxicology. 1: 377-87. PMID 16863450 DOI: 10.1517/17425255.1.3.377  0.92
2005 Pullagurla M, Siripurapu U, Kolanos R, Bondarev ML, Dukat M, Setola V, Roth BL, Glennon RA. Binding of amine-substituted N1-benzenesulfonylindoles at human 5-HT6 serotonin receptors. Bioorganic & Medicinal Chemistry Letters. 15: 5298-302. PMID 16183286 DOI: 10.1016/j.bmcl.2005.08.059  0.72
2005 Abate C, Kolanos R, Dukat M, Setola V, Roth BL, Glennon RA. Interaction of chiral MS-245 analogs at h5-HT6 receptors. Bioorganic & Medicinal Chemistry Letters. 15: 3510-3. PMID 15990303 DOI: 10.1016/j.bmcl.2005.05.092  0.72
2005 Setola V, Dukat M, Glennon RA, Roth BL. Molecular determinants for the interaction of the valvulopathic anorexigen norfenfluramine with the 5-HT2B receptor. Molecular Pharmacology. 68: 20-33. PMID 15831837 DOI: 10.1124/mol.104.009266  0.72
2005 Kolanos R, Siripurapu U, Pullagurla M, Riaz M, Setola V, Roth BL, Dukat M, Glennon RA. Binding of isotryptamines and indenes at h5-HT6 serotonin receptors. Bioorganic & Medicinal Chemistry Letters. 15: 1987-91. PMID 15808453 DOI: 10.1016/j.bmcl.2005.02.070  0.72
2005 Lee M, Rangisetty JB, Pullagurla MR, Dukat M, Setola V, Roth BL, Glennon RA. 1-(1-Naphthyl)piperazine as a novel template for 5-HT6 serotonin receptor ligands. Bioorganic & Medicinal Chemistry Letters. 15: 1707-11. PMID 15745826 DOI: 10.1016/j.bmcl.2005.01.031  0.72
2004 Chang-Fong J, Rangisetty JB, Dukat M, Setola V, Raffay T, Roth B, Glennon RA. 1,2,3,4-Tetrahydrocarbazoles as 5-HT6 serotonin receptor ligands Bioorganic and Medicinal Chemistry Letters. 14: 1961-1964. PMID 15050637 DOI: 10.1016/j.bmcl.2004.01.071  0.72
2003 Setola V, Roth BL. Why mice are neither miniature humans nor small rats: a cautionary tale involving 5-hydroxytryptamine-6 serotonin receptor species variants. Molecular Pharmacology. 64: 1277-8. PMID 14645656 DOI: 10.1124/mol.64.6.1277  0.92
2003 Pullagurla MR, Dukat M, Setola V, Roth B, Glennon RA. N1-benzenesulfonylgramine and N1-benzenesulfonylskatole: novel 5-HT6 receptor ligand templates. Bioorganic & Medicinal Chemistry Letters. 13: 3355-9. PMID 12951125  0.52
2003 Setola V, Hufeisen SJ, Grande-Allen KJ, Vesely I, Glennon RA, Blough B, Rothman RB, Roth BL. 3,4-methylenedioxymethamphetamine (MDMA, "Ecstasy") induces fenfluramine-like proliferative actions on human cardiac valvular interstitial cells in vitro. Molecular Pharmacology. 63: 1223-9. PMID 12761331 DOI: 10.1124/mol.63.6.1223  0.72
2001 Nguyen T, Shapiro DA, George SR, Setola V, Lee DK, Cheng R, Rauser L, Lee SP, Lynch KR, Roth BL, O'Dowd BF. Discovery of a novel member of the histamine receptor family. Molecular Pharmacology. 59: 427-33. PMID 11179435  0.72
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