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Items: 22


IL-23 induces regulatory T cell plasticity with implications for inflammatory skin diseases.

Kannan AK, Su Z, Gauvin DM, Paulsboe SE, Duggan R, Lasko LM, Honore P, Kort ME, McGaraughty SP, Scott VE, Gauld SB.

Sci Rep. 2019 Nov 27;9(1):17675. doi: 10.1038/s41598-019-53240-z.


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.


Discovery of (R)-1-(7-chloro-2,2-bis(fluoromethyl)chroman-4-yl)-3-(3-methylisoquinolin-5-yl)urea (A-1165442): a temperature-neutral transient receptor potential vanilloid-1 (TRPV1) antagonist with analgesic efficacy.

Voight EA, Gomtsyan AR, Daanen JF, Perner RJ, Schmidt RG, Bayburt EK, DiDomenico S, McDonald HA, Puttfarcken PS, Chen J, Neelands TR, Bianchi BR, Han P, Reilly RM, Franklin PH, Segreti JA, Nelson RA, Su Z, King AJ, Polakowski JS, Baker SJ, Gauvin DM, Lewis LR, Mikusa JP, Joshi SK, Faltynek CR, Kym PR, Kort ME.

J Med Chem. 2014 Sep 11;57(17):7412-24. doi: 10.1021/jm500916t. Epub 2014 Aug 21.


Characterization of nerve growth factor-induced mechanical and thermal hypersensitivity in rats.

Mills CD, Nguyen T, Tanga FY, Zhong C, Gauvin DM, Mikusa J, Gomez EJ, Salyers AK, Bannon AW.

Eur J Pain. 2013 Apr;17(4):469-79. doi: 10.1002/j.1532-2149.2012.00202.x. Epub 2012 Aug 23.


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.


A-995662 [(R)-8-(4-methyl-5-(4-(trifluoromethyl)phenyl)oxazol-2-ylamino)-1,2,3,4-tetrahydronaphthalen-2-ol], a novel, selective TRPV1 receptor antagonist, reduces spinal release of glutamate and CGRP in a rat knee joint pain model.

Puttfarcken PS, Han P, Joshi SK, Neelands TR, Gauvin DM, Baker SJ, Lewis LG, Bianchi BR, Mikusa JP, Koenig JR, Perner RJ, Kort ME, Honore P, Faltynek CR, Kym PR, Reilly RM.

Pain. 2010 Aug;150(2):319-26. doi: 10.1016/j.pain.2010.05.015. Epub 2010 Jun 19.


Synthesis and biological evaluation of 5-substituted and 4,5-disubstituted-2-arylamino oxazole TRPV1 antagonists.

Perner RJ, Koenig JR, Didomenico S, Gomtsyan A, Schmidt RG, Lee CH, Hsu MC, McDonald HA, Gauvin DM, Joshi S, Turner TM, Reilly RM, Kym PR, Kort ME.

Bioorg Med Chem. 2010 Jul 1;18(13):4821-9. doi: 10.1016/j.bmc.2010.04.099. Epub 2010 May 10.


Repeated dosing of ABT-102, a potent and selective TRPV1 antagonist, enhances TRPV1-mediated analgesic activity in rodents, but attenuates antagonist-induced hyperthermia.

Honore P, Chandran P, Hernandez G, Gauvin DM, Mikusa JP, Zhong C, Joshi SK, Ghilardi JR, Sevcik MA, Fryer RM, Segreti JA, Banfor PN, Marsh K, Neelands T, Bayburt E, Daanen JF, Gomtsyan A, Lee CH, Kort ME, Reilly RM, Surowy CS, Kym PR, Mantyh PW, Sullivan JP, Jarvis MF, Faltynek CR.

Pain. 2009 Mar;142(1-2):27-35. doi: 10.1016/j.pain.2008.11.004. Epub 2009 Jan 9.


Discovery of potent furan piperazine sodium channel blockers for treatment of neuropathic pain.

Drizin I, Gregg RJ, Scanio MJ, Shi L, Gross MF, Atkinson RN, Thomas JB, Johnson MS, Carroll WA, Marron BE, Chapman ML, Liu D, Krambis MJ, Shieh CC, Zhang X, Hernandez G, Gauvin DM, Mikusa JP, Zhu CZ, Joshi S, Honore P, Marsh KC, Roeloffs R, Werness S, Krafte DS, Jarvis MF, Faltynek CR, Kort ME.

Bioorg Med Chem. 2008 Jun 15;16(12):6379-86. doi: 10.1016/j.bmc.2008.05.003. Epub 2008 May 6.


Analgesic activity of metabotropic glutamate receptor 1 antagonists on spontaneous post-operative pain in rats.

Zhu CZ, Baker S, EI-Kouhen O, Lehto SG, Hollingsworth PR, Gauvin DM, Hernandez G, Zheng G, Chang R, Moreland RB, Stewart AO, Brioni JD, Honore P.

Eur J Pharmacol. 2008 Feb 12;580(3):314-21. Epub 2007 Nov 13.


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.


A-740003 [N-(1-{[(cyanoimino)(5-quinolinylamino) methyl]amino}-2,2-dimethylpropyl)-2-(3,4-dimethoxyphenyl)acetamide], a novel and selective P2X7 receptor antagonist, dose-dependently reduces neuropathic pain in the rat.

Honore P, Donnelly-Roberts D, Namovic MT, Hsieh G, Zhu CZ, Mikusa JP, Hernandez G, Zhong C, Gauvin DM, Chandran P, Harris R, Medrano AP, Carroll W, Marsh K, Sullivan JP, Faltynek CR, Jarvis MF.

J Pharmacol Exp Ther. 2006 Dec;319(3):1376-85. Epub 2006 Sep 18.


A-425619 [1-isoquinolin-5-yl-3-(4-trifluoromethyl-benzyl)-urea], a novel transient receptor potential type V1 receptor antagonist, relieves pathophysiological pain associated with inflammation and tissue injury in rats.

Honore P, Wismer CT, Mikusa J, Zhu CZ, Zhong C, Gauvin DM, Gomtsyan A, El Kouhen R, Lee CH, Marsh K, Sullivan JP, Faltynek CR, Jarvis MF.

J Pharmacol Exp Ther. 2005 Jul;314(1):410-21. Epub 2005 Apr 18.


Assessing the role of metabotropic glutamate receptor 5 in multiple nociceptive modalities.

Zhu CZ, Wilson SG, Mikusa JP, Wismer CT, Gauvin DM, Lynch JJ 3rd, Wade CL, Decker MW, Honore P.

Eur J Pharmacol. 2004 Dec 15;506(2):107-18.


Synthesis and structure-activity studies on N-[5-(1H-imidazol-4-yl)-5,6,7,8-tetrahydro-1-naphthalenyl]methanesulfonamide, an imidazole-containing alpha(1A)-adrenoceptor agonist.

Altenbach RJ, Khilevich A, Kolasa T, Rohde JJ, Bhatia PA, Patel MV, Searle XB, Yang F, Bunnelle WH, Tietje K, Bayburt EK, Carroll WA, Meyer MD, Henry R, Buckner SA, Kuk J, Daza AV, Milicic IV, Cain JC, Kang CH, Ireland LM, Carr TL, Miller TR, Hancock AA, Nakane M, Esbenshade TA, Brune ME, O'Neill AB, Gauvin DM, Katwala SP, Holladay MW, Brioni JD, Sullivan JP.

J Med Chem. 2004 Jun 3;47(12):3220-35.


N-[3-(1H-imidazol-4-ylmethyl)phenyl]ethanesulfonamide (ABT-866, 1),(1) a novel alpha(1)-adrenoceptor ligand with an enhanced in vitro and in vivo profile relative to phenylpropanolamine and midodrine.

Altenbach RJ, Khilevich A, Meyer MD, Buckner SA, Milicic I, Daza AV, Brune ME, O'Neill AB, Gauvin DM, Cain JC, Nakane M, Holladay MW, Williams M, Brioni JD, Sullivan JP.

J Med Chem. 2002 Sep 26;45(20):4395-7.


Pharmacological properties of A-204176, a novel and selective alpha1A adrenergic agonist, in in vitro and in vivo models of urethral function.

O'Neill AB, Buckner SA, Brune ME, Milicic I, Daza AV, Gauvin DM, Altenbach RJ, Meyer MD, Williams M, Sullivan JP, Brioni JD.

Life Sci. 2001 Nov 30;70(2):181-97.


Comparison of alpha 1-adrenoceptor agonists in canine urethral pressure profilometry and abdominal leak point pressure models.

Brune ME, O'Neill AB, Gauvin DM, Katwala SP, Altenbach RJ, Brioni JD, Hancock AA, Sullivan JP.

J Urol. 2001 Oct;166(4):1555-9.


A macrolactam inhibitor of T helper type 1 and T helper type 2 cytokine biosynthesis for topical treatment of inflammatory skin diseases.

Mollison KW, Fey TA, Gauvin DM, Kolano RM, Sheets MP, Smith ML, Pong M, Nikolaidis NM, Lane BC, Trevillyan JM, Cannon J, Marsh K, Carter GW, Or YS, Chen YW, Hsieh GC, Luly JR.

J Invest Dermatol. 1999 May;112(5):729-38.


Discovery of ascomycin analogs with potent topical but weak systemic activity for treatment of inflammatory skin diseases.

Mollison KW, Fey TA, Gauvin DM, Sheets MP, Smith ML, Pong M, Krause R, Miller L, Or YS, Kawai M, Wagner R, Wiedeman PE, Clark RF, Gunawardana IW, Rhoades TA, Henry CL, Tu NP, BaMaung NY, Kopecka H, Liu L, Xie Q, Lane BC, Trevillyan JM, Marsh K, Luly JR, et al.

Curr Pharm Des. 1998 Oct;4(5):367-79. Review.


Ex vivo assessment of immunosuppression in undiluted whole blood from pigs dosed with tacrolimus (FK506).

Chen YW, Smith ML, Sheets MP, Ballaron SJ, Trevillyan JM, Fey TA, Gauvin DM, Kolano R, Pong MS, Hsieh GC, Bauch J, Marsh K, Carter G, Luly J, Djuric S, Mollison KW.

Clin Immunol. 1999 Jan;90(1):133-40.


Inhibition of mature IL-1 beta production in murine macrophages and a murine model of inflammation by WIN 67694, an inhibitor of IL-1 beta converting enzyme.

Miller BE, Krasney PA, Gauvin DM, Holbrook KB, Koonz DJ, Abruzzese RV, Miller RE, Pagani KA, Dolle RE, Ator MA, et al.

J Immunol. 1995 Feb 1;154(3):1331-8.


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