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Inhibition of IL-23 mediated inflammation with a novel small molecule inverse agonist of RORgt.

Gauld S, Jacquet S, Gauvin D, Wallace C, Wang Y, McCarthy R, Goess C, Leys L, Huang S, Su Z, Edelmayer R, Wetter J, Salte K, McGaraughty S, Argiriadi M, Honore P, Luccarini JM, Bressac D, Desino K, Breinlinger E, Cusack K, Potin D, Kort M, Masson P.

J Pharmacol Exp Ther. 2019 Aug 2. pii: jpet.119.258046. doi: 10.1124/jpet.119.258046. [Epub ahead of print]


Small Molecule IL-36γ Antagonist as a Novel Therapeutic Approach for Plaque Psoriasis.

Todorović V, Su Z, Putman CB, Kakavas SJ, Salte KM, McDonald HA, Wetter JB, Paulsboe SE, Sun Q, Gerstein CE, Medina L, Sielaff B, Sadhukhan R, Stockmann H, Richardson PL, Qiu W, Argiriadi MA, Henry RF, Herold JM, Shotwell JB, McGaraughty SP, Honore P, Gopalakrishnan SM, Sun CC, Scott VE.

Sci Rep. 2019 Jun 24;9(1):9089. doi: 10.1038/s41598-019-45626-w.


Characterization of psoriasiform dermatitis induced by systemic injection of interleukin-23 minicircles in mice.

Leys L, Wang Y, Paulsboe S, Edelmayer R, Salte K, Wetter J, Namovic M, Phillips L, Dunstan R, Gauvin D, Donnelly-Roberts D, Su Z, Honore P, McGaraughty S.

J Dermatol. 2019 Jun;46(6):482-497. doi: 10.1111/1346-8138.14899. Epub 2019 May 7.


Monocytes/Macrophages play a pathogenic role in IL-23 mediated psoriasis-like skin inflammation.

Wang Y, Edelmayer R, Wetter J, Salte K, Gauvin D, Leys L, Paulsboe S, Su Z, Weinberg I, Namovic M, Gauld SB, Honore P, Scott VE, McGaraughty S.

Sci Rep. 2019 Mar 29;9(1):5310. doi: 10.1038/s41598-019-41655-7.


IL-36 receptor antagonistic antibodies inhibit inflammatory responses in preclinical models of psoriasiform dermatitis.

Su Z, Paulsboe S, Wetter J, Salte K, Kannan A, Mathew S, Horowitz A, Gerstein C, Namovic M, Todorović V, Seagal J, Edelmayer RM, Viner M, Rinaldi L, Zhou L, Leys L, Huang S, Wang L, Sadhukhan R, Honore P, McGaraughty S, Scott VE.

Exp Dermatol. 2019 Feb;28(2):113-120. doi: 10.1111/exd.13841. Epub 2018 Dec 21.


Mechanistic and pharmacological assessment of murine IL-23 mediated psoriasiform dermatitis; implications for drug discovery.

Gauld SB, Gauvin D, Olson L, Leys L, Paulsboe S, Liu Z, Edelmayer RM, Wetter J, Salte K, Wang Y, Huang S, Honore P, McGaraughty S.

J Dermatol Sci. 2018 Oct;92(1):45-53. doi: 10.1016/j.jdermsci.2018.08.001. Epub 2018 Aug 7.


Characterization and pharmacological modulation of noci-responsive deep dorsal horn neurons across diverse rat models of pathological pain.

McGaraughty S, Chu KL, Xu J.

J Neurophysiol. 2018 Oct 1;120(4):1893-1905. doi: 10.1152/jn.00325.2018. Epub 2018 Aug 1.


Short-term oral gavage administration of adenine induces a model of fibrotic kidney disease in rats.

Zhu CZ, Doyle KJ, Nikkel AL, Olsen L, Namovic MT, Salte K, Widomski D, Su Z, Donnelly-Roberts DL, Gopalakrishnan MM, McGaraughty S.

J Pharmacol Toxicol Methods. 2018 Nov - Dec;94(Pt 1):34-43. doi: 10.1016/j.vascn.2018.04.003. Epub 2018 Apr 22.


Characterization and comparison of rat monosodium iodoacetate and medial meniscal tear models of osteoarthritic pain.

Brederson JD, Chu KL, Xu J, Nikkel AL, Markosyan S, Jarvis MF, Edelmayer R, Bitner RS, McGaraughty S.

J Orthop Res. 2018 Feb 11. doi: 10.1002/jor.23869. [Epub ahead of print]


Losartan improves renal function and pathology in obese ZSF-1 rats.

Su Z, Widomski D, Nikkel A, Leys L, Namovic M, Donnelly-Roberts D, Gopalakrishnan M, McGaraughty S.

J Basic Clin Physiol Pharmacol. 2018 Jun 27;29(3):281-290. doi: 10.1515/jbcpp-2017-0157.


Targeting Anti-TGF-β Therapy to Fibrotic Kidneys with a Dual Specificity Antibody Approach.

McGaraughty S, Davis-Taber RA, Zhu CZ, Cole TB, Nikkel AL, Chhaya M, Doyle KJ, Olson LM, Preston GM, Grinnell CM, Salte KM, Giamis AM, Luo Y, Sun V, Goodearl AD, Gopalakrishnan M, Lacy SE.

J Am Soc Nephrol. 2017 Dec;28(12):3616-3626. doi: 10.1681/ASN.2017010013. Epub 2017 Aug 21.


TRPV3 modulates nociceptive signaling through peripheral and supraspinal sites in rats.

McGaraughty S, Chu KL, Xu J, Leys L, Radek RJ, Dart MJ, Gomtsyan A, Schmidt RG, Kym PR, Brederson JD.

J Neurophysiol. 2017 Aug 1;118(2):904-916. doi: 10.1152/jn.00104.2017. Epub 2017 May 3.


Longitudinal Changes in Measured Glomerular Filtration Rate, Renal Fibrosis and Biomarkers in a Rat Model of Type 2 Diabetic Nephropathy.

Su Z, Widomski D, Ma J, Namovic M, Nikkel A, Leys L, Olson L, Salte K, Donnelly-Roberts D, Esbenshade T, McGaraughty S.

Am J Nephrol. 2016;44(5):339-353. Epub 2016 Oct 14.


A-306989, an inhibitor of adenosine kinase, is renoprotective in rodent models of podocyte, basement membrane, and obstructive injury.

Zhu CZ, Gopalakrishnan S, Doyle K, Nikkel AL, Olson L, Abraham VC, Leys L, Widomski D, Salte K, Putman B, Pratt S, Ma J, Su Z, Gopalakrishnan M, Lee CH, McGaraughty SP.

Eur J Pharmacol. 2016 Oct 5;788:1-11. doi: 10.1016/j.ejphar.2016.06.012. Epub 2016 Jun 8.


Synthesis and Pharmacology of (Pyridin-2-yl)methanol Derivatives as Novel and Selective Transient Receptor Potential Vanilloid 3 Antagonists.

Gomtsyan A, Schmidt RG, Bayburt EK, Gfesser GA, Voight EA, Daanen JF, Schmidt DL, Cowart MD, Liu H, Altenbach RJ, Kort ME, Clapham B, Cox PB, Shrestha A, Henry R, Whittern DN, Reilly RM, Puttfarcken PS, Brederson JD, Song P, Li B, Huang SM, McDonald HA, Neelands TR, McGaraughty SP, Gauvin DM, Joshi SK, Banfor PN, Segreti JA, Shebley M, Faltynek CR, Dart MJ, Kym PR.

J Med Chem. 2016 May 26;59(10):4926-47. doi: 10.1021/acs.jmedchem.6b00287. Epub 2016 May 2.


Characterization of the triazine, T4, a representative from a novel series of CaV2 inhibitors with strong state-dependence, poor use-dependence, and distinctively fast kinetics.

Swensen AM, Niforatos W, Lee CH, Jarvis MF, McGaraughty S.

Eur J Pharmacol. 2014 Dec 15;745:234-42. doi: 10.1016/j.ejphar.2014.10.037. Epub 2014 Oct 30.


A selective α2 B adrenoceptor agonist (A-1262543) and duloxetine modulate nociceptive neurones in the medial prefrontal cortex, but not in the spinal cord of neuropathic rats.

Chu KL, Xu J, Frost J, Li L, Gomez E, Dart MJ, Jarvis MF, Meyer MD, McGaraughty S.

Eur J Pain. 2015 May;19(5):649-60. doi: 10.1002/ejp.586. Epub 2014 Aug 25.


A peripherally acting, selective T-type calcium channel blocker, ABT-639, effectively reduces nociceptive and neuropathic pain in rats.

Jarvis MF, Scott VE, McGaraughty S, Chu KL, Xu J, Niforatos W, Milicic I, Joshi S, Zhang Q, Xia Z.

Biochem Pharmacol. 2014 Jun 15;89(4):536-44. doi: 10.1016/j.bcp.2014.03.015. Epub 2014 Apr 12.


Mechanistic insights into the analgesic efficacy of A-1264087, a novel neuronal Ca(2+) channel blocker that reduces nociception in rat preclinical pain models.

Zhu CZ, Vortherms TA, Zhang M, Xu J, Swensen AM, Niforatos W, Neelands T, Milicic I, Lewis LG, Zhong C, Gauvin D, Mikusa J, Zhan C, Pai M, Roderwald V, Chu KL, Cole EE, Bespalov A, Searle XB, McGaraughty S, Bitner RS, Jarvis MF, Bannon AW, Joshi SK, Scott VE, Lee CH.

J Pain. 2014 Apr;15(4):387.e1-14. doi: 10.1016/j.jpain.2013.12.002. Epub 2013 Dec 25.


A mixed Ca2+ channel blocker, A-1264087, utilizes peripheral and spinal mechanisms to inhibit spinal nociceptive transmission in a rat model of neuropathic pain.

Xu J, Chu KL, Zhu CZ, Niforatos W, Swensen A, Searle X, Lee L, Jarvis MF, McGaraughty S.

J Neurophysiol. 2014 Jan;111(2):394-404. doi: 10.1152/jn.00463.2013. Epub 2013 Oct 23.


Disturbances in slow-wave sleep are induced by models of bilateral inflammation, neuropathic, and postoperative pain, but not osteoarthritic pain in rats.

Leys LJ, Chu KL, Xu J, Pai M, Yang HS, Robb HM, Jarvis MF, Radek RJ, McGaraughty S.

Pain. 2013 Jul;154(7):1092-102. doi: 10.1016/j.pain.2013.03.019. Epub 2013 Mar 15.


Rats housed on corncob bedding show less slow-wave sleep.

Leys LJ, McGaraughty S, Radek RJ.

J Am Assoc Lab Anim Sci. 2012 Nov;51(6):764-8.


Development and validation of a medium-throughput electrophysiological assay for KCNQ2/3 channel openers using QPatch HT.

Zhang XF, Zhang D, Surowy CS, Yao B, Jarvis MF, McGaraughty S, Neelands TR.

Assay Drug Dev Technol. 2013 Feb;11(1):17-24. doi: 10.1089/adt.2012.446. Epub 2012 Sep 24.


Antagonism of supraspinal histamine H3 receptors modulates spinal neuronal activity in neuropathic rats.

McGaraughty S, Chu KL, Cowart MD, Brioni JD.

J Pharmacol Exp Ther. 2012 Oct;343(1):13-20. doi: 10.1124/jpet.112.194761. Epub 2012 Jun 22.


An automated electrophysiological assay for differentiating Ca(v)2.2 inhibitors based on state dependence and kinetics.

Swensen AM, Niforatos W, Vortherms TA, Perner RJ, Li T, Schrimpf MR, Scott VE, Lee L, Jarvis MF, McGaraughty S.

Assay Drug Dev Technol. 2012 Dec;10(6):542-50. doi: 10.1089/adt.2011.437. Epub 2012 Mar 19.


Spontaneous firing and evoked responses of spinal nociceptive neurons are attenuated by blockade of P2X3 and P2X2/3 receptors in inflamed rats.

Xu J, Chu KL, Brederson JD, Jarvis MF, McGaraughty S.

J Neurosci Res. 2012 Aug;90(8):1597-606. doi: 10.1002/jnr.23042. Epub 2012 Mar 16.


TRPV1 antagonist, A-889425, inhibits mechanotransmission in a subclass of rat primary afferent neurons following peripheral inflammation.

Brederson JD, Chu KL, Reilly RM, Brown BS, Kym PR, Jarvis MF, McGaraughty S.

Synapse. 2012 Mar;66(3):187-95. doi: 10.1002/syn.20992. Epub 2011 Dec 13.


Coexpression and activation of TRPV1 suppress the activity of the KCNQ2/3 channel.

Zhang XF, Han P, Neelands TR, McGaraughty S, Honore P, Surowy CS, Zhang D.

J Gen Physiol. 2011 Sep;138(3):341-52. doi: 10.1085/jgp.201110618. Epub 2011 Aug 15.


Selective blockade of TRPA1 channel attenuates pathological pain without altering noxious cold sensation or body temperature regulation.

Chen J, Joshi SK, DiDomenico S, Perner RJ, Mikusa JP, Gauvin DM, Segreti JA, Han P, Zhang XF, Niforatos W, Bianchi BR, Baker SJ, Zhong C, Simler GH, McDonald HA, Schmidt RG, McGaraughty SP, Chu KL, Faltynek CR, Kort ME, Reilly RM, Kym PR.

Pain. 2011 May;152(5):1165-72. doi: 10.1016/j.pain.2011.01.049. Epub 2011 Mar 12.


Oral and cutaneous thermosensory profile of selective TRPV1 inhibition by ABT-102 in a randomized healthy volunteer trial.

Rowbotham MC, Nothaft W, Duan WR, Wang Y, Faltynek C, McGaraughty S, Chu KL, Svensson P.

Pain. 2011 May;152(5):1192-200. doi: 10.1016/j.pain.2011.01.051. Epub 2011 Mar 4.


TRPV1-related modulation of spinal neuronal activity and behavior in a rat model of osteoarthritic pain.

Chu KL, Chandran P, Joshi SK, Jarvis MF, Kym PR, McGaraughty S.

Brain Res. 2011 Jan 19;1369:158-66. doi: 10.1016/j.brainres.2010.10.101. Epub 2010 Nov 1.


Characterization of Fasudil in preclinical models of pain.

Boyce-Rustay JM, Simler GH, McGaraughty S, Chu KL, Wensink EJ, Vasudevan A, Honore P.

J Pain. 2010 Oct;11(10):941-9. doi: 10.1016/j.jpain.2009.12.014. Epub 2010 Mar 24.


TRPA1 modulation of spontaneous and mechanically evoked firing of spinal neurons in uninjured, osteoarthritic, and inflamed rats.

McGaraughty S, Chu KL, Perner RJ, Didomenico S, Kort ME, Kym PR.

Mol Pain. 2010 Mar 5;6:14. doi: 10.1186/1744-8069-6-14.


Antagonism of TRPV1 receptors indirectly modulates activity of thermoregulatory neurons in the medial preoptic area of rats.

McGaraughty S, Segreti JA, Fryer RM, Brown BS, Faltynek CR, Kym PR.

Brain Res. 2009 May 1;1268:58-67. doi: 10.1016/j.brainres.2009.02.018. Epub 2009 Feb 21.


A CB(2) receptor agonist, A-836339, modulates wide dynamic range neuronal activity in neuropathic rats: contributions of spinal and peripheral CB(2) receptors.

McGaraughty S, Chu KL, Dart MJ, Yao BB, Meyer MD.

Neuroscience. 2009 Feb 18;158(4):1652-61. doi: 10.1016/j.neuroscience.2008.11.015. Epub 2008 Nov 14.


Contributions of central and peripheral TRPV1 receptors to mechanically evoked and spontaneous firing of spinal neurons in inflamed rats.

McGaraughty S, Chu KL, Brown BS, Zhu CZ, Zhong C, Joshi SK, Honore P, Faltynek CR, Jarvis MF.

J Neurophysiol. 2008 Dec;100(6):3158-66. doi: 10.1152/jn.90768.2008. Epub 2008 Oct 1.


(R)-(5-tert-butyl-2,3-dihydro-1H-inden-1-yl)-3-(1H-indazol-4-yl)-urea (ABT-102) blocks polymodal activation of transient receptor potential vanilloid 1 receptors in vitro and heat-evoked firing of spinal dorsal horn neurons in vivo.

Surowy CS, Neelands TR, Bianchi BR, McGaraughty S, El Kouhen R, Han P, Chu KL, McDonald HA, Vos M, Niforatos W, Bayburt EK, Gomtsyan A, Lee CH, Honore P, Sullivan JP, Jarvis MF, Faltynek CR.

J Pharmacol Exp Ther. 2008 Sep;326(3):879-88. doi: 10.1124/jpet.108.138511. Epub 2008 May 30.


A selective Nav1.8 sodium channel blocker, A-803467 [5-(4-chlorophenyl-N-(3,5-dimethoxyphenyl)furan-2-carboxamide], attenuates spinal neuronal activity in neuropathic rats.

McGaraughty S, Chu KL, Scanio MJ, Kort ME, Faltynek CR, Jarvis MF.

J Pharmacol Exp Ther. 2008 Mar;324(3):1204-11. Epub 2007 Dec 18.


Pharmacological MRI in awake rats predicts selective binding of alpha4beta2 nicotinic receptors.

Chin CL, Pauly JR, Surber BW, Skoubis PD, McGaraughty S, Hradil VP, Luo Y, Cox BF, Fox GB.

Synapse. 2008 Mar;62(3):159-68.


Painful purinergic receptors.

Donnelly-Roberts D, McGaraughty S, Shieh CC, Honore P, Jarvis MF.

J Pharmacol Exp Ther. 2008 Feb;324(2):409-15. Epub 2007 Nov 27. Review.


A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat.

Jarvis MF, Honore P, Shieh CC, Chapman M, Joshi S, Zhang XF, Kort M, Carroll W, Marron B, Atkinson R, Thomas J, Liu D, Krambis M, Liu Y, McGaraughty S, Chu K, Roeloffs R, Zhong C, Mikusa JP, Hernandez G, Gauvin D, Wade C, Zhu C, Pai M, Scanio M, Shi L, Drizin I, Gregg R, Matulenko M, Hakeem A, Gross M, Johnson M, Marsh K, Wagoner PK, Sullivan JP, Faltynek CR, Krafte DS.

Proc Natl Acad Sci U S A. 2007 May 15;104(20):8520-5. Epub 2007 May 2.


P2X7-related modulation of pathological nociception in rats.

McGaraughty S, Chu KL, Namovic MT, Donnelly-Roberts DL, Harris RR, Zhang XF, Shieh CC, Wismer CT, Zhu CZ, Gauvin DM, Fabiyi AC, Honore P, Gregg RJ, Kort ME, Nelson DW, Carroll WA, Marsh K, Faltynek CR, Jarvis MF.

Neuroscience. 2007 Jun 8;146(4):1817-28. Epub 2007 May 3.


4-amino-5-aryl-6-arylethynylpyrimidines: structure-activity relationships of non-nucleoside adenosine kinase inhibitors.

Matulenko MA, Paight ES, Frey RR, Gomtsyan A, DiDomenico S Jr, Jiang M, Lee CH, Stewart AO, Yu H, Kohlhaas KL, Alexander KM, McGaraughty S, Mikusa J, Marsh KC, Muchmore SW, Jakob CL, Kowaluk EA, Jarvis MF, Bhagwat SS.

Bioorg Med Chem. 2007 Feb 15;15(4):1586-605. Epub 2006 Dec 20.


Pharmacological MRI in awake rats reveals neural activity in area postrema and nucleus tractus solitarius: relevance as a potential biomarker for detecting drug-induced emesis.

Chin CL, Fox GB, Hradil VP, Osinski MA, McGaraughty SP, Skoubis PD, Cox BF, Luo Y.

Neuroimage. 2006 Dec;33(4):1152-60. Epub 2006 Oct 4.


Blockade of mGluR1 receptor results in analgesia and disruption of motor and cognitive performances: effects of A-841720, a novel non-competitive mGluR1 receptor antagonist.

El-Kouhen O, Lehto SG, Pan JB, Chang R, Baker SJ, Zhong C, Hollingsworth PR, Mikusa JP, Cronin EA, Chu KL, McGaraughty SP, Uchic ME, Miller LN, Rodell NM, Patel M, Bhatia P, Mezler M, Kolasa T, Zheng GZ, Fox GB, Stewart AO, Decker MW, Moreland RB, Brioni JD, Honore P.

Br J Pharmacol. 2006 Nov;149(6):761-74. Epub 2006 Oct 3.


Pharmacological and functional magnetic resonance imaging techniques in CNS drug discovery.

Fox GB, McGaraughty S, Luo Y.

Expert Opin Drug Discov. 2006 Aug;1(3):211-24. doi: 10.1517/17460441.1.3.211.


Antinociceptive properties of a non-nucleotide P2X3/P2X2/3 receptor antagonist.

McGaraughty S, Jarvis MF.

Drug News Perspect. 2005 Oct;18(8):501-7. Review.


Mapping brain activity following administration of a nicotinic acetylcholine receptor agonist, ABT-594, using functional magnetic resonance imaging in awake rats.

Skoubis PD, Hradil V, Chin CL, Luo Y, Fox GB, McGaraughty S.

Neuroscience. 2006;137(2):583-91. Epub 2005 Nov 14.


Endogenous opioid mechanisms partially mediate P2X3/P2X2/3-related antinociception in rat models of inflammatory and chemogenic pain but not neuropathic pain.

McGaraughty S, Honore P, Wismer CT, Mikusa J, Zhu CZ, McDonald HA, Bianchi B, Faltynek CR, Jarvis MF.

Br J Pharmacol. 2005 Sep;146(2):180-8.

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