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Preclinical Testing of Nalfurafine as an Opioid-sparing Adjuvant that Potentiates Analgesia by the Mu Opioid Receptor-targeting Agonist Morphine.

Kaski SW, White AN, Gross JD, Trexler KR, Wix K, Harland AA, Prisinzano TE, Aubé J, Kinsey SG, Kenakin T, Siderovski DP, Setola V.

J Pharmacol Exp Ther. 2019 Nov;371(2):487-499. doi: 10.1124/jpet.118.255661. Epub 2019 Sep 6.


A role for Regulator of G protein Signaling-12 (RGS12) in the balance between myoblast proliferation and differentiation.

Schroer AB, Mohamed JS, Willard MD, Setola V, Oestreich E, Siderovski DP.

PLoS One. 2019 Aug 13;14(8):e0216167. doi: 10.1371/journal.pone.0216167. eCollection 2019.


Role of RGS12 in the differential regulation of kappa opioid receptor-dependent signaling and behavior.

Gross JD, Kaski SW, Schmidt KT, Cogan ES, Boyt KM, Wix K, Schroer AB, McElligott ZA, Siderovski DP, Setola V.

Neuropsychopharmacology. 2019 Sep;44(10):1728-1741. doi: 10.1038/s41386-019-0423-7. Epub 2019 May 29.


Single Nucleotide Polymorphisms in Chemosensory Pathway Genes GNB3, TAS2R19, and TAS2R38 Are Associated with Chronic Rhinosinusitis.

Purnell PR, Addicks BL, Zalzal HG, Shapiro S, Wen S, Ramadan HH, Setola V, Siderovski DP.

Int Arch Allergy Immunol. 2019;180(1):72-78. doi: 10.1159/000499875. Epub 2019 May 28.


Four single nucleotide polymorphisms in genes involved in neuronal signaling are associated with Opioid Use Disorder in West Virginia.

Kaski SW, Brooks S, Wen S, Haut MW, Siderovski DP, Berry JH, Lander LR, Setola V.

J Opioid Manag. 2019 Mar-Apr;15(2):103-109. doi: 10.5055/jom.2019.0491.


Development of Full Sweet, Umami, and Bitter Taste Responsiveness Requires Regulator of G protein Signaling-21 (RGS21).

Schroer AB, Gross JD, Kaski SW, Wix K, Siderovski DP, Vandenbeuch A, Setola V.

Chem Senses. 2018 May 23;43(5):367-378. doi: 10.1093/chemse/bjy024.


Correction: The Ketamine Analogue Methoxetamine and 3- and 4-Methoxy Analogues of Phencyclidine Are High Affinity and Selective Ligands for the Glutamate NMDA Receptor.

Roth BL, Gibbons S, Arunotayanun W, Huang XP, Setola V, Treble R, Iversen L.

PLoS One. 2018 Mar 22;13(3):e0194984. doi: 10.1371/journal.pone.0194984. eCollection 2018.


Regulator of G protein signaling-12 modulates the dopamine transporter in ventral striatum and locomotor responses to psychostimulants.

Gross JD, Kaski SW, Schroer AB, Wix KA, Siderovski DP, Setola V.

J Psychopharmacol. 2018 Feb;32(2):191-203. doi: 10.1177/0269881117742100. Epub 2018 Jan 24.


Reduction of GPSM3 expression akin to the arthritis-protective SNP rs204989 differentially affects migration in a neutrophil model.

Gall BJ, Schroer AB, Gross JD, Setola V, Siderovski DP.

Genes Immun. 2016 Sep;17(6):321-7. doi: 10.1038/gene.2016.26. Epub 2016 Jun 16.


Identification and Validation of Small Molecules That Enhance Recombinant Adeno-associated Virus Transduction following High-Throughput Screens.

Nicolson SC, Li C, Hirsch ML, Setola V, Samulski RJ.

J Virol. 2016 Jul 27;90(16):7019-7031. doi: 10.1128/JVI.02953-15. Print 2016 Aug 15.


Genetic variations in GPSM3 associated with protection from rheumatoid arthritis affect its transcript abundance.

Gall BJ, Wilson A, Schroer AB, Gross JD, Stoilov P, Setola V, Watkins CM, Siderovski DP.

Genes Immun. 2016 Mar;17(2):139-47. doi: 10.1038/gene.2016.3. Epub 2016 Jan 28.


Correction: Exome Sequencing in 53 Sporadic Cases of Schizophrenia Identifies 18 Putative Candidate Genes.

Guipponi M, Santoni FA, Setola V, Gehrig C, Rotharmel M, Cuenca M, Guillin O, Dikeos D, Georgantopoulos G, Papadimitriou G, Curtis L, Méary A, Schürhoff F, Jamain S, Avramopoulos D, Leboyer M, Rujescu D, Pulver A, Campion D, Siderovski DP, Antonarakis SE.

PLoS One. 2015 Oct 21;10(10):e0141630. doi: 10.1371/journal.pone.0141630. eCollection 2015. No abstract available.


Exome sequencing in 53 sporadic cases of schizophrenia identifies 18 putative candidate genes.

Guipponi M, Santoni FA, Setola V, Gehrig C, Rotharmel M, Cuenca M, Guillin O, Dikeos D, Georgantopoulos G, Papadimitriou G, Curtis L, Méary A, Schürhoff F, Jamain S, Avramopoulos D, Leboyer M, Rujescu D, Pulver A, Campion D, Siderovski DP, Antonarakis SE.

PLoS One. 2014 Nov 24;9(11):e112745. doi: 10.1371/journal.pone.0112745. eCollection 2014. Erratum in: PLoS One. 2015;10(10):e0141630.


Michael acceptor approach to the design of new salvinorin A-based high affinity ligands for the kappa-opioid receptor.

Polepally PR, Huben K, Vardy E, Setola V, Mosier PD, Roth BL, Zjawiony JK.

Eur J Med Chem. 2014 Oct 6;85:818-29. doi: 10.1016/j.ejmech.2014.07.077. Epub 2014 Aug 23.


Further evaluation of the tropane analogs of haloperidol.

Sampson D, Bricker B, Zhu XY, Peprah K, Lamango NS, Setola V, Roth BL, Ablordeppey SY.

Bioorg Med Chem Lett. 2014 Sep 1;24(17):4294-7. doi: 10.1016/j.bmcl.2014.07.018. Epub 2014 Jul 14.


Identification of a new selective dopamine D4 receptor ligand.

Sampson D, Zhu XY, Eyunni SV, Etukala JR, Ofori E, Bricker B, Lamango NS, Setola V, Roth BL, Ablordeppey SY.

Bioorg Med Chem. 2014 Jun 15;22(12):3105-14. doi: 10.1016/j.bmc.2014.04.026. Epub 2014 Apr 20.


Intracerebroventricular injection of adeno-associated virus 6 and 9 vectors for cell type-specific transgene expression in the spinal cord.

Dirren E, Towne CL, Setola V, Redmond DE Jr, Schneider BL, Aebischer P.

Hum Gene Ther. 2014 Feb;25(2):109-20. doi: 10.1089/hum.2013.021. Epub 2014 Jan 15.


Role of the N-terminal region in G protein-coupled receptor functions: negative modulation revealed by 5-HT2B receptor polymorphisms.

Belmer A, Doly S, Setola V, Banas SM, Moutkine I, Boutourlinsky K, Kenakin T, Maroteaux L.

Mol Pharmacol. 2014 Jan;85(1):127-38. doi: 10.1124/mol.113.089086. Epub 2013 Oct 30.


RGS21, a regulator of taste and mucociliary clearance?

Kimple AJ, Garland AL, Cohen SP, Setola V, Willard FS, Zielinski T, Lowery RG, Tarran R, Siderovski DP.

Laryngoscope. 2014 Mar;124(3):E56-63. doi: 10.1002/lary.24326. Epub 2013 Oct 2.


Discovery of Novel General Anesthetics Using Apoferritin as a Surrogate System.

Rai G, Bu W, Lea WA, Liang D, Weiser B, Setola V, Austin CP, Simeonov A, Jadhav A, Eckenhoff R, Maloney DJ.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2012 Apr 16 [updated 2013 May 8].


An analysis of the synthetic tryptamines AMT and 5-MeO-DALT: emerging 'Novel Psychoactive Drugs'.

Arunotayanun W, Dalley JW, Huang XP, Setola V, Treble R, Iversen L, Roth BL, Gibbons S.

Bioorg Med Chem Lett. 2013 Jun 1;23(11):3411-5. doi: 10.1016/j.bmcl.2013.03.066. Epub 2013 Mar 28.


The ketamine analogue methoxetamine and 3- and 4-methoxy analogues of phencyclidine are high affinity and selective ligands for the glutamate NMDA receptor.

Roth BL, Gibbons S, Arunotayanun W, Huang XP, Setola V, Treble R, Iversen L.

PLoS One. 2013;8(3):e59334. doi: 10.1371/journal.pone.0059334. Epub 2013 Mar 19. Erratum in: PLoS One. 2018 Mar 22;13(3):e0194984.


Photochemical activation of TRPA1 channels in neurons and animals.

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, Milan DJ, Peterson RT.

Nat Chem Biol. 2013 Apr;9(4):257-63. doi: 10.1038/nchembio.1183. Epub 2013 Feb 10.


Neurochemical profiles of some novel psychoactive substances.

Iversen L, Gibbons S, Treble R, Setola V, Huang XP, Roth BL.

Eur J Pharmacol. 2013 Jan 30;700(1-3):147-51. doi: 10.1016/j.ejphar.2012.12.006. Epub 2012 Dec 21.


Automated design of ligands to polypharmacological profiles.

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, Bickerton GR, Read KD, Wetsel WC, Gilbert IH, Roth BL, Hopkins AL.

Nature. 2012 Dec 13;492(7428):215-20. doi: 10.1038/nature11691.


5-HT(2B) antagonism arrests non-canonical TGF-β1-induced valvular myofibroblast differentiation.

Hutcheson JD, Ryzhova LM, Setola V, Merryman WD.

J Mol Cell Cardiol. 2012 Nov;53(5):707-14. doi: 10.1016/j.yjmcc.2012.08.012. Epub 2012 Aug 23.


Structure-functional selectivity relationship studies of β-arrestin-biased dopamine D₂ receptor agonists.

Chen X, Sassano MF, Zheng L, Setola V, Chen M, Bai X, Frye SV, Wetsel WC, Roth BL, Jin J.

J Med Chem. 2012 Aug 23;55(16):7141-53. doi: 10.1021/jm300603y. Epub 2012 Aug 13.


Moderate chemical modifications of WAY-100635 improve the selectivity for 5-HT1A versus D4 receptors.

Mangin F, Dilly S, Joly B, Scuvée-Moreau J, Evans J, Setola V, Roth BL, Liégeois JF.

Bioorg Med Chem Lett. 2012 Jul 15;22(14):4550-4. doi: 10.1016/j.bmcl.2012.05.119. Epub 2012 Jun 7.


Orally active adenosine A(1) receptor agonists with antinociceptive effects in mice.

Korboukh I, Hull-Ryde EA, Rittiner JE, Randhawa AS, Coleman J, Fitzpatrick BJ, Setola V, Janzen WP, Frye SV, Zylka MJ, Jin J.

J Med Chem. 2012 Jul 26;55(14):6467-77. doi: 10.1021/jm3004834. Epub 2012 Jul 16.


Identifying mechanism-of-action targets for drugs and probes.

Gregori-Puigjané E, Setola V, Hert J, Crews BA, Irwin JJ, Lounkine E, Marnett L, Roth BL, Shoichet BK.

Proc Natl Acad Sci U S A. 2012 Jul 10;109(28):11178-83. doi: 10.1073/pnas.1204524109. Epub 2012 Jun 18.


Benzothiazoles as probes for the 5HT1A receptor and the serotonin transporter (SERT): a search for new dual-acting agents as potential antidepressants.

Zhu XY, Etukala JR, Eyunni SV, Setola V, Roth BL, Ablordeppey SY.

Eur J Med Chem. 2012 Jul;53:124-32. doi: 10.1016/j.ejmech.2012.03.042. Epub 2012 Apr 4.


Bis-spirolabdane diterpenoids from Leonotis nepetaefolia.

Li J, Fronczek FR, Ferreira D, Burandt CL Jr, Setola V, Roth BL, Zjawiony JK.

J Nat Prod. 2012 Apr 27;75(4):728-34. doi: 10.1021/np3000156. Epub 2012 Apr 4.


Labdane diterpenoids from Leonotis leonurus.

Wu H, Li J, Fronczek FR, Ferreira D, Burandt CL Jr, Setola V, Roth BL, Zjawiony JK.

Phytochemistry. 2013 Jul;91:229-35. doi: 10.1016/j.phytochem.2012.02.021. Epub 2012 Mar 21.


Structure-activity relationship studies of SYA 013, a homopiperazine analog of haloperidol.

Peprah K, Zhu XY, Eyunni SV, Etukala JR, Setola V, Roth BL, Ablordeppey SY.

Bioorg Med Chem. 2012 Mar 1;20(5):1671-8. doi: 10.1016/j.bmc.2012.01.022. Epub 2012 Jan 21.


Spinal muscular atrophy pathogenic mutations impair the axonogenic properties of axonal-survival of motor neuron.

Locatelli D, d'Errico P, Capra S, Finardi A, Colciaghi F, Setola V, Terao M, Garattini E, Battaglia G.

J Neurochem. 2012 May;121(3):465-74. doi: 10.1111/j.1471-4159.2012.07689.x. Epub 2012 Mar 14.


Multi-receptor drug design: Haloperidol as a scaffold for the design and synthesis of atypical antipsychotic agents.

Peprah K, Zhu XY, Eyunni SV, Setola V, Roth BL, Ablordeppey SY.

Bioorg Med Chem. 2012 Feb 1;20(3):1291-7. doi: 10.1016/j.bmc.2011.12.019. Epub 2011 Dec 22.


Chemical informatics and target identification in a zebrafish phenotypic screen.

Laggner C, Kokel D, Setola V, Tolia A, Lin H, Irwin JJ, Keiser MJ, Cheung CY, Minor DL Jr, Roth BL, Peterson RT, Shoichet BK.

Nat Chem Biol. 2011 Dec 18;8(2):144-6. doi: 10.1038/nchembio.732.


Discovery of β-arrestin-biased dopamine D2 ligands for probing signal transduction pathways essential for antipsychotic efficacy.

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, Caron MG, Javitch JA, Roth BL, Jin J.

Proc Natl Acad Sci U S A. 2011 Nov 8;108(45):18488-93. doi: 10.1073/pnas.1104807108. Epub 2011 Oct 24.


Ligand discovery from a dopamine D3 receptor homology model and crystal structure.

Carlsson J, Coleman RG, Setola V, Irwin JJ, Fan H, Schlessinger A, Sali A, Roth BL, Shoichet BK.

Nat Chem Biol. 2011 Sep 18;7(11):769-78. doi: 10.1038/nchembio.662.


Design, synthesis, and validation of a β-turn mimetic library targeting protein-protein and peptide-receptor interactions.

Whitby LR, Ando Y, Setola V, Vogt PK, Roth BL, Boger DL.

J Am Chem Soc. 2011 Jul 6;133(26):10184-94. doi: 10.1021/ja201878v. Epub 2011 Jun 15.


Deficient serotonin neurotransmission and depression-like serotonin biomarker alterations in tryptophan hydroxylase 2 (Tph2) loss-of-function mice.

Jacobsen JP, Siesser WB, Sachs BD, Peterson S, Cools MJ, Setola V, Folgering JH, Flik G, Caron MG.

Mol Psychiatry. 2012 Jul;17(7):694-704. doi: 10.1038/mp.2011.50. Epub 2011 May 3.


Chronic delivery of antibody fragments using immunoisolated cell implants as a passive vaccination tool.

Marroquin Belaunzaran O, Cordero MI, Setola V, Bianchi S, Galli C, Bouche N, Mlynarik V, Gruetter R, Sandi C, Bensadoun JC, Molinari M, Aebischer P.

PLoS One. 2011 Apr 20;6(4):e18268. doi: 10.1371/journal.pone.0018268.


Serotonin receptors and heart valve disease--it was meant 2B.

Hutcheson JD, Setola V, Roth BL, Merryman WD.

Pharmacol Ther. 2011 Nov;132(2):146-57. doi: 10.1016/j.pharmthera.2011.03.008. Epub 2011 Apr 2. Review.


Synthesis and receptor profiling of Stemona alkaloid analogues reveal a potent class of sigma ligands.

Frankowski KJ, Setola V, Evans JM, Neuenswander B, Roth BL, Aubé J.

Proc Natl Acad Sci U S A. 2011 Apr 26;108(17):6727-32. doi: 10.1073/pnas.1016558108. Epub 2011 Feb 28. Erratum in: Proc Natl Acad Sci U S A. 2012 Sep 18;109(38):15526.


Schizophrenia risk gene CAV1 is both pro-psychotic and required for atypical antipsychotic drug actions in vivo.

Allen JA, Yadav PN, Setola V, Farrell M, Roth BL.

Transl Psychiatry. 2011 Aug 16;1:e33. doi: 10.1038/tp.2011.35.


Identification of human Ether-à-go-go related gene modulators by three screening platforms in an academic drug-discovery setting.

Huang XP, Mangano T, Hufeisen S, Setola V, Roth BL.

Assay Drug Dev Technol. 2010 Dec;8(6):727-42. doi: 10.1089/adt.2010.0331.


Neuroprotection by gene therapy targeting mutant SOD1 in individual pools of motor neurons does not translate into therapeutic benefit in fALS mice.

Towne C, Setola V, Schneider BL, Aebischer P.

Mol Ther. 2011 Feb;19(2):274-83. doi: 10.1038/mt.2010.260. Epub 2010 Nov 23.


The presynaptic component of the serotonergic system is required for clozapine's efficacy.

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, Roth BL.

Neuropsychopharmacology. 2011 Feb;36(3):638-51. doi: 10.1038/npp.2010.195. Epub 2010 Nov 3.


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