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Therapeutic potential of adenosine kinase inhibition-Revisited.

Jarvis MF.

Pharmacol Res Perspect. 2019 Jul 22;7(4):e00506. doi: 10.1002/prp2.506. eCollection 2019 Aug. Review.


A Patient-Centric Model for Discontinuation of a Single-Sourced Approved Drug.

Caplan A, Teagarden JR, Bacher HP, Jarvis MF.

Clin Pharmacol Ther. 2019 Sep;106(3):494-497. doi: 10.1002/cpt.1411. Epub 2019 Apr 12. No abstract available.


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]



Jarvis MF, Enna SJ.

Biochem Pharmacol. 2018 May;151:143. doi: 10.1016/j.bcp.2018.01.020. Epub 2018 Jan 10. No abstract available.


Erratum to: Gluten and Aluminum Content in Synthroid® (Levothyroxine Sodium Tablets).

Espaillat R, Jarvis MF, Torkelson C, Sinclair B.

Adv Ther. 2017 Sep;34(9):2178. doi: 10.1007/s12325-017-0608-6. No abstract available.


Gluten and Aluminum Content in Synthroid® (Levothyroxine Sodium Tablets).

Espaillat R, Jarvis MF, Torkelson C, Sinclair B.

Adv Ther. 2017 Jul;34(7):1764-1769. doi: 10.1007/s12325-017-0575-y. Epub 2017 Jun 26. Erratum in: Adv Ther. 2017 Aug 30;:.


Irreproducibility in Preclinical Biomedical Research: Perceptions, Uncertainties, and Knowledge Gaps.

Jarvis MF, Williams M.

Trends Pharmacol Sci. 2016 Apr;37(4):290-302. doi: 10.1016/ Epub 2016 Jan 6. Review.


Editor's Note.

Jarvis MF.

J Pharmacol Exp Ther. 2015 Dec;355(3):352. doi: 10.1124/jpet.115.229138. No abstract available.


Optimization of ADME Properties for Sulfonamides Leading to the Discovery of a T-Type Calcium Channel Blocker, ABT-639.

Zhang Q, Xia Z, Joshi S, Scott VE, Jarvis MF.

ACS Med Chem Lett. 2015 Apr 28;6(6):641-4. doi: 10.1021/acsmedchemlett.5b00023. eCollection 2015 Jun 11.


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.


The Concise Guide to PHARMACOLOGY 2013/14: overview.

Alexander SP, Benson HE, Faccenda E, Pawson AJ, Sharman JL, McGrath JC, Catterall WA, Spedding M, Peters JA, Harmar AJ; CGTP Collaborators, Abul-Hasn N, Anderson CM, Anderson CM, Araiksinen MS, Arita M, Arthofer E, Barker EL, Barratt C, Barnes NM, Bathgate R, Beart PM, Belelli D, Bennett AJ, Birdsall NJ, Boison D, Bonner TI, Brailsford L, Bröer S, Brown P, Calo G, Carter WG, Catterall WA, Chan SL, Chao MV, Chiang N, Christopoulos A, Chun JJ, Cidlowski J, Clapham DE, Cockcroft S, Connor MA, Cox HM, Cuthbert A, Dautzenberg FM, Davenport AP, Dawson PA, Dent G, Dijksterhuis JP, Dollery CT, Dolphin AC, Donowitz M, Dubocovich ML, Eiden L, Eidne K, Evans BA, Fabbro D, Fahlke C, Farndale R, Fitzgerald GA, Fong TM, Fowler CJ, Fry JR, Funk CD, Futerman AH, Ganapathy V, Gaisnier B, Gershengorn MA, Goldin A, Goldman ID, Gundlach AL, Hagenbuch B, Hales TG, Hammond JR, Hamon M, Hancox JC, Hauger RL, Hay DL, Hobbs AJ, Hollenberg MD, Holliday ND, Hoyer D, Hynes NA, Inui KI, Ishii S, Jacobson KA, Jarvis GE, Jarvis MF, Jensen R, Jones CE, Jones RL, Kaibuchi K, Kanai Y, Kennedy C, Kerr ID, Khan AA, Klienz MJ, Kukkonen JP, Lapoint JY, Leurs R, Lingueglia E, Lippiat J, Lolait SJ, Lummis SC, Lynch JW, MacEwan D, Maguire JJ, Marshall IL, May JM, McArdle CA, McGrath JC, Michel MC, Millar NS, Miller LJ, Mitolo V, Monk PN, Moore PK, Moorhouse AJ, Mouillac B, Murphy PM, Neubig RR, Neumaier J, Niesler B, Obaidat A, Offermanns S, Ohlstein E, Panaro MA, Parsons S, Pwrtwee RG, Petersen J, Pin JP, Poyner DR, Prigent S, Prossnitz ER, Pyne NJ, Pyne S, Quigley JG, Ramachandran R, Richelson EL, Roberts RE, Roskoski R, Ross RA, Roth M, Rudnick G, Ryan RM, Said SI, Schild L, Sanger GJ, Scholich K, Schousboe A, Schulte G, Schulz S, Serhan CN, Sexton PM, Sibley DR, Siegel JM, Singh G, Sitsapesan R, Smart TG, Smith DM, Soga T, Stahl A, Stewart G, Stoddart LA, Summers RJ, Thorens B, Thwaites DT, Toll L, Traynor JR, Usdin TB, Vandenberg RJ, Villalon C, Vore M, Waldman SA, Ward DT, Willars GB, Wonnacott SJ, Wright E, Ye RD, Yonezawa A, Zimmermann M.

Br J Pharmacol. 2013 Dec;170(8):1449-58. doi: 10.1111/bph.12444.


Characterization of P1 (adenosine) purinoceptors.

Jarvis MF.

Curr Protoc Pharmacol. 2013 Oct 8;62:1.9.1-1.9.16. doi: 10.1002/0471141755.ph0109s62.


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.


Biochemical and pharmacological assessment of MAP-kinase signaling along pain pathways in experimental rodent models: a potential tool for the discovery of novel antinociceptive therapeutics.

Edelmayer RM, Brederson JD, Jarvis MF, Bitner RS.

Biochem Pharmacol. 2014 Feb 1;87(3):390-8. doi: 10.1016/j.bcp.2013.11.019. Epub 2013 Dec 1. Review.


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.


Synthesis and SAR of 4-aminocyclopentapyrrolidines as orally active N-type calcium channel inhibitors for inflammatory and neuropathic pain.

Beebe X, Yeung CM, Darczak D, Shekhar S, Vortherms TA, Miller L, Milicic I, Swensen AM, Zhu CZ, Banfor P, Wetter JM, Marsh KC, Jarvis MF, Scott VE, Schrimpf MR, Lee CH.

Bioorg Med Chem Lett. 2013 Sep 1;23(17):4857-61. doi: 10.1016/j.bmcl.2013.06.074. Epub 2013 Jul 4.


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.


P2X receptors as drug targets.

North RA, Jarvis MF.

Mol Pharmacol. 2013 Apr;83(4):759-69. doi: 10.1124/mol.112.083758. Epub 2012 Dec 19. Review.


Spinal microglial activation in rat models of neuropathic and osteoarthritic pain: an autoradiographic study using [3H]PK11195.

Miller TR, Wetter JB, Jarvis MF, Bitner RS.

Eur J Pain. 2013 May;17(5):692-703. doi: 10.1002/j.1532-2149.2012.00232.x. Epub 2012 Oct 16.


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.


High throughput functional assays for P2X receptors.

Namovic MT, Jarvis MF, Donnelly-Roberts D.

Curr Protoc Pharmacol. 2012 Jun;Chapter 9:Unit 9.15.. doi: 10.1002/0471141755.ph0915s57.


Cytochrome P450 mediated linoleic acid metabolism in peripheral inflammatory nociception.

Jarvis MF.

Pain. 2012 Oct;153(10):1987-8. doi: 10.1016/j.pain.2012.05.020. Epub 2012 Jun 6. No abstract available.


Chronic administration of the selective P2X3, P2X2/3 receptor antagonist, A-317491, transiently attenuates cancer-induced bone pain in mice.

Hansen RR, Nasser A, Falk S, Baldvinsson SB, Ohlsson PH, Bahl JM, Jarvis MF, Ding M, Heegaard AM.

Eur J Pharmacol. 2012 Aug 5;688(1-3):27-34. doi: 10.1016/j.ejphar.2012.05.008. Epub 2012 May 22.


Synthesis and SAR of 4-aminocyclopentapyrrolidines as N-type Ca²⁺ channel blockers with analgesic activity.

Beebe X, Darczak D, Henry RF, Vortherms T, Janis R, Namovic M, Donnelly-Roberts D, Kage KL, Surowy C, Milicic I, Niforatos W, Swensen A, Marsh KC, Wetter JM, Franklin P, Baker S, Zhong C, Simler G, Gomez E, Boyce-Rustay JM, Zhu CZ, Stewart AO, Jarvis MF, Scott VE.

Bioorg Med Chem. 2012 Jul 1;20(13):4128-39. doi: 10.1016/j.bmc.2012.04.057. Epub 2012 May 4.


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.


Discovery of diphenyl lactam derivatives as N-type calcium channel blockers.

Doherty GA, Bhatia P, Vortherms TA, Marsh KC, Wetter JM, Mack H, Scott VE, Jarvis MF, Stewart AO.

Bioorg Med Chem Lett. 2012 Feb 15;22(4):1716-8. doi: 10.1016/j.bmcl.2011.12.100. Epub 2012 Jan 8.


A-1048400 is a novel, orally active, state-dependent neuronal calcium channel blocker that produces dose-dependent antinociception without altering hemodynamic function in rats.

Scott VE, Vortherms TA, Niforatos W, Swensen AM, Neelands T, Milicic I, Banfor PN, King A, Zhong C, Simler G, Zhan C, Bratcher N, Boyce-Rustay JM, Zhu CZ, Bhatia P, Doherty G, Mack H, Stewart AO, Jarvis MF.

Biochem Pharmacol. 2012 Feb 1;83(3):406-18. doi: 10.1016/j.bcp.2011.10.019. Epub 2011 Nov 16.


P2X receptor antagonists for pain management: examination of binding and physicochemical properties.

Gum RJ, Wakefield B, Jarvis MF.

Purinergic Signal. 2012 Feb;8(Suppl 1):41-56. doi: 10.1007/s11302-011-9272-5. Epub 2011 Nov 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.


Monosodium iodoacetate-induced joint pain is associated with increased phosphorylation of mitogen activated protein kinases in the rat spinal cord.

Lee Y, Pai M, Brederson JD, Wilcox D, Hsieh G, Jarvis MF, Bitner RS.

Mol Pain. 2011 May 20;7:39. doi: 10.1186/1744-8069-7-39.


Synthesis and in vitro activity of N-benzyl-1-(2,3-dichlorophenyl)-1H-tetrazol-5-amine P2X(7) antagonists.

Perez-Medrano A, Donnelly-Roberts DL, Florjancic AS, Nelson DW, Li T, Namovic MT, Peddi S, Faltynek CR, Jarvis MF, Carroll WA.

Bioorg Med Chem Lett. 2011 Jun 1;21(11):3297-300. doi: 10.1016/j.bmcl.2011.04.024. Epub 2011 Apr 14.


Fibromyalgia: mechanisms, current treatment and animal models.

Brederson JD, Jarvis MF, Honore P, Surowy CS.

Curr Pharm Biotechnol. 2011 Oct;12(10):1613-26. Review.


Comparative analysis of inactivated-state block of N-type (Ca(v)2.2) calcium channels.

Vortherms TA, Swensen AM, Niforatos W, Limberis JT, Neelands TR, Janis RS, Thimmapaya R, Donnelly-Roberts DL, Namovic MT, Zhang D, Brent Putman C, Martin RL, Surowy CS, Jarvis MF, Scott VE.

Inflamm Res. 2011 Jul;60(7):683-93. doi: 10.1007/s00011-011-0322-9. Epub 2011 Mar 11.


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.


Discovery and biological evaluation of potent, selective, orally bioavailable, pyrazine-based blockers of the Na(v)1.8 sodium channel with efficacy in a model of neuropathic pain.

Scanio MJ, Shi L, Drizin I, Gregg RJ, Atkinson RN, Thomas JB, Johnson MS, Chapman ML, Liu D, Krambis MJ, Liu Y, Shieh CC, Zhang X, Simler GH, Joshi S, Honore P, Marsh KC, Knox A, Werness S, Antonio B, Krafte DS, Jarvis MF, Faltynek CR, Marron BE, Kort ME.

Bioorg Med Chem. 2010 Nov 15;18(22):7816-25. doi: 10.1016/j.bmc.2010.09.057. Epub 2010 Sep 29.


Subtype-selective Na(v)1.8 sodium channel blockers: identification of potent, orally active nicotinamide derivatives.

Kort ME, Atkinson RN, Thomas JB, Drizin I, Johnson MS, Secrest MA, Gregg RJ, Scanio MJ, Shi L, Hakeem AH, Matulenko MA, Chapman ML, Krambis MJ, Liu D, Shieh CC, Zhang X, Simler G, Mikusa JP, Zhong C, Joshi S, Honore P, Roeloffs R, Werness S, Antonio B, Marsh KC, Faltynek CR, Krafte DS, Jarvis MF, Marron BE.

Bioorg Med Chem Lett. 2010 Nov 15;20(22):6812-5. doi: 10.1016/j.bmcl.2010.08.121. Epub 2010 Sep 18.


A-887826 is a structurally novel, potent and voltage-dependent Na(v)1.8 sodium channel blocker that attenuates neuropathic tactile allodynia in rats.

Zhang XF, Shieh CC, Chapman ML, Matulenko MA, Hakeem AH, Atkinson RN, Kort ME, Marron BE, Joshi S, Honore P, Faltynek CR, Krafte DS, Jarvis MF.

Neuropharmacology. 2010 Sep;59(3):201-7. doi: 10.1016/j.neuropharm.2010.05.009. Epub 2010 Jun 1.


Animal models of acute and chronic inflammatory and nociceptive pain.

Boyce-Rustay JM, Honore P, Jarvis MF.

Methods Mol Biol. 2010;617:41-55. doi: 10.1007/978-1-60327-323-7_4.


The neural-glial purinergic receptor ensemble in chronic pain states.

Jarvis MF.

Trends Neurosci. 2010 Jan;33(1):48-57. doi: 10.1016/j.tins.2009.10.003. Epub 2009 Nov 14. Review.


Mammalian P2X7 receptor pharmacology: comparison of recombinant mouse, rat and human P2X7 receptors.

Donnelly-Roberts DL, Namovic MT, Han P, Jarvis MF.

Br J Pharmacol. 2009 Aug;157(7):1203-14. doi: 10.1111/j.1476-5381.2009.00233.x. Epub 2009 Jun 22.


The antihyperalgesic activity of a selective P2X7 receptor antagonist, A-839977, is lost in IL-1alphabeta knockout mice.

Honore P, Donnelly-Roberts D, Namovic M, Zhong C, Wade C, Chandran P, Zhu C, Carroll W, Perez-Medrano A, Iwakura Y, Jarvis MF.

Behav Brain Res. 2009 Dec 1;204(1):77-81. doi: 10.1016/j.bbr.2009.05.018. Epub 2009 May 21.


Neuropathic pain: models and mechanisms.

Jarvis MF, Boyce-Rustay JM.

Curr Pharm Des. 2009;15(15):1711-6. Review.


Discovery and biological evaluation of novel cyanoguanidine P2X(7) antagonists with analgesic activity in a rat model of neuropathic pain.

Perez-Medrano A, Donnelly-Roberts DL, Honore P, Hsieh GC, Namovic MT, Peddi S, Shuai Q, Wang Y, Faltynek CR, Jarvis MF, Carroll WA.

J Med Chem. 2009 May 28;52(10):3366-76. doi: 10.1021/jm8015848.


Voltage-gated sodium channels in pain states: role in pathophysiology and targets for treatment.

Dib-Hajj SD, Binshtok AM, Cummins TR, Jarvis MF, Samad T, Zimmermann K.

Brain Res Rev. 2009 Apr;60(1):65-83. doi: 10.1016/j.brainresrev.2008.12.005. Epub 2008 Dec 25. Review.


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.


Additive antinociceptive effects of the selective Nav1.8 blocker A-803467 and selective TRPV1 antagonists in rat inflammatory and neuropathic pain models.

Joshi SK, Honore P, Hernandez G, Schmidt R, Gomtsyan A, Scanio M, Kort M, Jarvis MF.

J Pain. 2009 Mar;10(3):306-15. doi: 10.1016/j.jpain.2008.09.007. Epub 2008 Dec 13.


Behavioral profile of P2X7 receptor knockout mice in animal models of depression and anxiety: relevance for neuropsychiatric disorders.

Basso AM, Bratcher NA, Harris RR, Jarvis MF, Decker MW, Rueter LE.

Behav Brain Res. 2009 Mar 2;198(1):83-90. doi: 10.1016/j.bbr.2008.10.018. Epub 2008 Oct 18.


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