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Items: 43


Pharmacological evaluation of NSAID-induced gastropathy as a "Translatable" model of referred visceral hypersensitivity.

Hummel M, Knappenberger T, Reilly M, Whiteside GT.

World J Gastroenterol. 2017 Sep 7;23(33):6065-6076. doi: 10.3748/wjg.v23.i33.6065.


Measuring and realizing the translational significance of preclinical in vivo studies of painful osteoarthritis.

Hummel M, Whiteside GT.

Osteoarthritis Cartilage. 2017 Mar;25(3):376-384. doi: 10.1016/j.joca.2016.08.007. Epub 2016 Aug 31.


A randomized, double-blind, positive-controlled, 3-way cross-over human experimental pain study of a TRPV1 antagonist (V116517) in healthy volunteers and comparison with preclinical profile.

Arendt-Nielsen L, Harris S, Whiteside GT, Hummel M, Knappenberger T, OʼKeefe S, Kapil R, Kyle D.

Pain. 2016 Sep;157(9):2057-67. doi: 10.1097/j.pain.0000000000000610.


Preclinical Pharmacological Approaches in Drug Discovery for Chronic Pain.

Whiteside GT, Pomonis JD, Kennedy JD.

Adv Pharmacol. 2016;75:303-23. doi: 10.1016/bs.apha.2015.12.002. Epub 2016 Jan 21. Review.


Robustness of arterial blood gas analysis for assessment of respiratory safety pharmacology in rats.

Whiteside GT, Hummel M, Boulet J, Beyenhof JD, Strenkowski B, John JD, Knappenberger T, Maselli H, Koetzner L.

J Pharmacol Toxicol Methods. 2016 Mar-Apr;78:32-41. doi: 10.1016/j.vascn.2015.11.001. Epub 2015 Nov 14.


An industry perspective on the role and utility of animal models of pain in drug discovery.

Whiteside GT, Pomonis JD, Kennedy JD.

Neurosci Lett. 2013 Dec 17;557 Pt A:65-72. doi: 10.1016/j.neulet.2013.08.033. Epub 2013 Aug 27. Review.


Negative allosteric modulation of metabotropic glutamate receptor 5 results in broad spectrum activity relevant to treatment resistant depression.

Hughes ZA, Neal SJ, Smith DL, Sukoff Rizzo SJ, Pulicicchio CM, Lotarski S, Lu S, Dwyer JM, Brennan J, Olsen M, Bender CN, Kouranova E, Andree TH, Harrison JE, Whiteside GT, Springer D, O'Neil SV, Leonard SK, Schechter LE, Dunlop J, Rosenzweig-Lipson S, Ring RH.

Neuropharmacology. 2013 Mar;66:202-14. doi: 10.1016/j.neuropharm.2012.04.007. Epub 2012 Apr 21.


Discovery of novel selective norepinephrine inhibitors: 1-(2-morpholin-2-ylethyl)-3-aryl-1,3-dihydro-2,1,3-benzothiadiazole 2,2-dioxides (WYE-114152).

O'Neill DJ, Adedoyin A, Bray JA, Deecher DC, Fensome A, Goldberg JA, Harrison J, Leventhal L, Mann C, Mark L, Nogle L, Sullivan NR, Spangler TB, Terefenko EA, Trybulski EJ, Uveges AJ, Vu A, Whiteside GT, Zhang P.

J Med Chem. 2011 Oct 13;54(19):6824-31. doi: 10.1021/jm200733r. Epub 2011 Sep 14.


Consideration of Pharmacokinetic Pharmacodynamic Relationships in the Discovery of New Pain Drugs.

Whiteside GT, Kennedy JD.

In: Kruger L, Light AR, editors. Translational Pain Research: From Mouse to Man. Boca Raton, FL: CRC Press/Taylor & Francis; 2010. Chapter 16.


Dynamic changes in the microRNA expression profile reveal multiple regulatory mechanisms in the spinal nerve ligation model of neuropathic pain.

von Schack D, Agostino MJ, Murray BS, Li Y, Reddy PS, Chen J, Choe SE, Strassle BW, Li C, Bates B, Zhang L, Hu H, Kotnis S, Bingham B, Liu W, Whiteside GT, Samad TA, Kennedy JD, Ajit SK.

PLoS One. 2011 Mar 14;6(3):e17670. doi: 10.1371/journal.pone.0017670.


Monoacylglycerol lipase activity is a critical modulator of the tone and integrity of the endocannabinoid system.

Chanda PK, Gao Y, Mark L, Btesh J, Strassle BW, Lu P, Piesla MJ, Zhang MY, Bingham B, Uveges A, Kowal D, Garbe D, Kouranova EV, Ring RH, Bates B, Pangalos MN, Kennedy JD, Whiteside GT, Samad TA.

Mol Pharmacol. 2010 Dec;78(6):996-1003. doi: 10.1124/mol.110.068304. Epub 2010 Sep 20.


Inflammatory cytokine and chemokine expression is differentially modulated acutely in the dorsal root ganglion in response to different nerve root compressions.

Rothman SM, Ma LH, Whiteside GT, Winkelstein BA.

Spine (Phila Pa 1976). 2011 Feb 1;36(3):197-202. doi: 10.1097/BRS.0b013e3181ce4f4d.


Inhibition of osteoclasts prevents cartilage loss and pain in a rat model of degenerative joint disease.

Strassle BW, Mark L, Leventhal L, Piesla MJ, Jian Li X, Kennedy JD, Glasson SS, Whiteside GT.

Osteoarthritis Cartilage. 2010 Oct;18(10):1319-28. doi: 10.1016/j.joca.2010.06.007. Epub 2010 Jul 13.


Purinergic receptor-mediated morphological changes in microglia are transient and independent from inflammatory cytokine release.

McIlvain HB, Ma L, Ludwig B, Manners MT, Martone RL, Dunlop J, Kaftan EJ, Kennedy JD, Whiteside GT.

Eur J Pharmacol. 2010 Sep 25;643(2-3):202-10. doi: 10.1016/j.ejphar.2010.06.046. Epub 2010 Jul 13.


WAY-318068: a novel, potent and selective noradrenaline re-uptake inhibitor with activity in rodent models of pain and depression.

Whiteside GT, Dwyer JM, Harrison JE, Beyer CE, Cummons T, Manzino L, Mark L, Johnston GH, Strassle BW, Adedoyin A, Lu P, Piesla MJ, Pulicicchio CM, Erve JC, Platt BJ, Hughes ZA, Rogers KE, Deecher DC, Trybulski EJ, Kennedy JD, Zhang P, Leventhal L.

Br J Pharmacol. 2010 Jul;160(5):1105-18. doi: 10.1111/j.1476-5381.2010.00690.x.


Pain is a salient "stressor" that is mediated by corticotropin-releasing factor-1 receptors.

Hummel M, Cummons T, Lu P, Mark L, Harrison JE, Kennedy JD, Whiteside GT.

Neuropharmacology. 2010 Sep;59(3):160-6. doi: 10.1016/j.neuropharm.2010.05.001. Epub 2010 May 12.


Discovery of novel selective norepinephrine reuptake inhibitors: 4-[3-aryl-2,2-dioxido-2,1,3-benzothiadiazol-1(3H)-yl]-1-(methylamino)butan-2-ols (WYE-103231).

O'Neill DJ, Adedoyin A, Alfinito PD, Bray JA, Cosmi S, Deecher DC, Fensome A, Harrison J, Leventhal L, Mann C, McComas CC, Sullivan NR, Spangler TB, Uveges AJ, Trybulski EJ, Whiteside GT, Zhang P.

J Med Chem. 2010 Jun 10;53(11):4511-21. doi: 10.1021/jm100053t.


Depression-like phenotype following chronic CB1 receptor antagonism.

Beyer CE, Dwyer JM, Piesla MJ, Platt BJ, Shen R, Rahman Z, Chan K, Manners MT, Samad TA, Kennedy JD, Bingham B, Whiteside GT.

Neurobiol Dis. 2010 Aug;39(2):148-55. doi: 10.1016/j.nbd.2010.03.020. Epub 2010 Apr 8.


Genetic and functional analysis of human P2X5 reveals a distinct pattern of exon 10 polymorphism with predominant expression of the nonfunctional receptor isoform.

Kotnis S, Bingham B, Vasilyev DV, Miller SW, Bai Y, Yeola S, Chanda PK, Bowlby MR, Kaftan EJ, Samad TA, Whiteside GT.

Mol Pharmacol. 2010 Jun;77(6):953-60. doi: 10.1124/mol.110.063636. Epub 2010 Mar 11.


Structure-activity relationships of norepinephrine reuptake inhibitors with benzothiadiazine dioxide or dihydrosulfostyril cores.

Fensome A, Goldberg J, McComas CC, Trybulski EJ, Woodworth RP, Deecher DC, Whiteside GT, Zhang P.

Bioorg Med Chem Lett. 2010 Mar 1;20(5):1555-8. doi: 10.1016/j.bmcl.2010.01.056. Epub 2010 Jan 20.


Loss of retrograde endocannabinoid signaling and reduced adult neurogenesis in diacylglycerol lipase knock-out mice.

Gao Y, Vasilyev DV, Goncalves MB, Howell FV, Hobbs C, Reisenberg M, Shen R, Zhang MY, Strassle BW, Lu P, Mark L, Piesla MJ, Deng K, Kouranova EV, Ring RH, Whiteside GT, Bates B, Walsh FS, Williams G, Pangalos MN, Samad TA, Doherty P.

J Neurosci. 2010 Feb 10;30(6):2017-24. doi: 10.1523/JNEUROSCI.5693-09.2010.


1-(Indolin-1-yl)-1-phenyl-3-propan-2-olamines as potent and selective norepinephrine reuptake inhibitors.

Vu AT, Cohn ST, Zhang P, Kim CY, Mahaney PE, Bray JA, Johnston GH, Koury EJ, Cosmi SA, Deecher DC, Smith VA, Harrison JE, Leventhal L, Whiteside GT, Kennedy JD, Trybulski EJ.

J Med Chem. 2010 Mar 11;53(5):2051-62. doi: 10.1021/jm901559e.


Tri-partite complex for axonal transport drug delivery achieves pharmacological effect.

Filler AG, Whiteside GT, Bacon M, Frederickson M, Howe FA, Rabinowitz MD, Sokoloff AJ, Deacon TW, Abell C, Munglani R, Griffiths JR, Bell BA, Lever AM.

BMC Neurosci. 2010 Jan 20;11:8. doi: 10.1186/1471-2202-11-8.


Estrogen receptor neurobiology and its potential for translation into broad spectrum therapeutics for CNS disorders.

Hughes ZA, Liu F, Marquis K, Muniz L, Pangalos MN, Ring RH, Whiteside GT, Brandon NJ.

Curr Mol Pharmacol. 2009 Nov;2(3):215-36. Review.


1- or 3-(3-Amino-2-hydroxy-1-phenyl propyl)-1,3-dihydro-2H-benzimidazol-2-ones: potent, selective, and orally efficacious norepinephrine reuptake inhibitors.

Zhang P, Terefenko EA, Bray J, Deecher D, Fensome A, Harrison J, Kim C, Koury E, Mark L, McComas CC, Mugford CA, Trybulski EJ, Vu AT, Whiteside GT, Mahaney PE.

J Med Chem. 2009 Sep 24;52(18):5703-11. doi: 10.1021/jm900888c.


Abnormal gait, due to inflammation but not nerve injury, reflects enhanced nociception in preclinical pain models.

Piesla MJ, Leventhal L, Strassle BW, Harrison JE, Cummons TA, Lu P, Whiteside GT.

Brain Res. 2009 Oct 27;1295:89-98. doi: 10.1016/j.brainres.2009.07.091. Epub 2009 Aug 3.


CNS penetration of small molecules following local inflammation, widespread systemic inflammation or direct injury to the nervous system.

Lu P, Gonzales C, Chen Y, Adedoyin A, Hummel M, Kennedy JD, Whiteside GT.

Life Sci. 2009 Sep 9;85(11-12):450-6. doi: 10.1016/j.lfs.2009.07.009. Epub 2009 Jul 24.


Age-dependent effects of the cannabinoid CB1 antagonist SR141716A on food intake, body weight change, and pruritus in rats.

Ward SJ, Lefever TW, Rawls SM, Whiteside GT, Walker EA.

Psychopharmacology (Berl). 2009 Sep;206(1):155-65. doi: 10.1007/s00213-009-1592-6. Epub 2009 Jul 3.


The persistence of a long-term negative affective state following the induction of either acute or chronic pain.

Hummel M, Lu P, Cummons TA, Whiteside GT.

Pain. 2008 Dec;140(3):436-45. doi: 10.1016/j.pain.2008.09.020. Epub 2008 Oct 21.


Predictive validity of animal pain models? A comparison of the pharmacokinetic-pharmacodynamic relationship for pain drugs in rats and humans.

Whiteside GT, Adedoyin A, Leventhal L.

Neuropharmacology. 2008 Apr;54(5):767-75. doi: 10.1016/j.neuropharm.2008.01.001. Epub 2008 Jan 12. Review.


Pharmacological characterization of the muscarinic agonist (3R,4R)-3-(3-hexylsulfanyl-pyrazin-2-yloxy)-1-aza-bicyclo[2.2.1]heptane (WAY-132983) in in vitro and in vivo models of chronic pain.

Sullivan NR, Leventhal L, Harrison J, Smith VA, Cummons TA, Spangler TB, Sun SC, Lu P, Uveges AJ, Strassle BW, Piesla MJ, Ramdass R, Barry A, Schantz J, Adams W, Whiteside GT, Adedoyin A, Jones PG.

J Pharmacol Exp Ther. 2007 Sep;322(3):1294-304. Epub 2007 Jun 22.


Species-specific in vitro pharmacological effects of the cannabinoid receptor 2 (CB2) selective ligand AM1241 and its resolved enantiomers.

Bingham B, Jones PG, Uveges AJ, Kotnis S, Lu P, Smith VA, Sun SC, Resnick L, Chlenov M, He Y, Strassle BW, Cummons TA, Piesla MJ, Harrison JE, Whiteside GT, Kennedy JD.

Br J Pharmacol. 2007 Aug;151(7):1061-70. Epub 2007 Jun 4. Erratum in: Br J Pharmacol. 2007 Aug;151(7):1137.


Pharmacology of 2-[4-(4-chloro-2-fluorophenoxy)phenyl]-pyrimidine-4-carboxamide: a potent, broad-spectrum state-dependent sodium channel blocker for treating pain states.

Ilyin VI, Pomonis JD, Whiteside GT, Harrison JE, Pearson MS, Mark L, Turchin PI, Gottshall S, Carter RB, Nguyen P, Hogenkamp DJ, Olanrewaju S, Benjamin E, Woodward RM.

J Pharmacol Exp Ther. 2006 Sep;318(3):1083-93. Epub 2006 May 25.


A role for cannabinoid receptors, but not endogenous opioids, in the antinociceptive activity of the CB2-selective agonist, GW405833.

Whiteside GT, Gottshall SL, Boulet JM, Chaffer SM, Harrison JE, Pearson MS, Turchin PI, Mark L, Garrison AE, Valenzano KJ.

Eur J Pharmacol. 2005 Dec 28;528(1-3):65-72. Epub 2005 Nov 28.


Neuropathy-induced osteopenia in rats is not due to a reduction in weight born on the affected limb.

Whiteside GT, Boulet JM, Sellers R, Bunton TE, Walker K.

Bone. 2006 Mar;38(3):387-93. Epub 2005 Oct 3.


Pharmacological and pharmacokinetic characterization of the cannabinoid receptor 2 agonist, GW405833, utilizing rodent models of acute and chronic pain, anxiety, ataxia and catalepsy.

Valenzano KJ, Tafesse L, Lee G, Harrison JE, Boulet JM, Gottshall SL, Mark L, Pearson MS, Miller W, Shan S, Rabadi L, Rotshteyn Y, Chaffer SM, Turchin PI, Elsemore DA, Toth M, Koetzner L, Whiteside GT.

Neuropharmacology. 2005 Apr;48(5):658-72.


A-317491, a selective P2X3/P2X2/3 receptor antagonist, reverses inflammatory mechanical hyperalgesia through action at peripheral receptors in rats.

Wu G, Whiteside GT, Lee G, Nolan S, Niosi M, Pearson MS, Ilyin VI.

Eur J Pharmacol. 2004 Nov 3;504(1-2):45-53.


DiPOA ([8-(3,3-diphenyl-propyl)-4-oxo-1-phenyl-1,3,8-triazaspiro[4.5]dec-3-yl]-acetic acid), a novel, systemically available, and peripherally restricted Mu opioid agonist with antihyperalgesic activity: II. In vivo pharmacological characterization in the rat.

Whiteside GT, Harrison JE, Pearson MS, Chen Z, Fundytus ME, Rotshteyn Y, Turchin PI, Pomonis JD, Mark L, Walker K, Broglé KC.

J Pharmacol Exp Ther. 2004 Aug;310(2):793-9. Epub 2004 Mar 30. Erratum in: J Pharmacol Exp Ther. 2005 Mar;312(3):1334. Fundytus, Marian E [added].


Pharmacological characterisation of a rat model of incisional pain.

Whiteside GT, Harrison J, Boulet J, Mark L, Pearson M, Gottshall S, Walker K.

Br J Pharmacol. 2004 Jan;141(1):85-91. Epub 2003 Nov 3.


Cell death in the superficial dorsal horn in a model of neuropathic pain.

Whiteside GT, Munglani R.

J Neurosci Res. 2001 Apr 15;64(2):168-73.


Effect of colchicine on neuropeptide Y expression in rat dorsal root ganglia and spinal cord.

Cougnon-Aptel N, Whiteside GT, Munglani R.

Neurosci Lett. 1999 Jan 4;259(1):45-8.


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