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Items: 27


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 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.


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.


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.


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.


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.


(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.


Activation of TRPA1 channels by the fatty acid amide hydrolase inhibitor 3'-carbamoylbiphenyl-3-yl cyclohexylcarbamate (URB597).

Niforatos W, Zhang XF, Lake MR, Walter KA, Neelands T, Holzman TF, Scott VE, Faltynek CR, Moreland RB, Chen J.

Mol Pharmacol. 2007 May;71(5):1209-16. Epub 2007 Feb 21.


Utility of large-scale transiently transfected cells for cell-based high-throughput screens to identify transient receptor potential channel A1 (TRPA1) antagonists.

Chen J, Lake MR, Sabet RS, Niforatos W, Pratt SD, Cassar SC, Xu J, Gopalakrishnan S, Pereda-Lopez A, Gopalakrishnan M, Holzman TF, Moreland RB, Walter KA, Faltynek CR, Warrior U, Scott VE.

J Biomol Screen. 2007 Feb;12(1):61-9. Epub 2006 Nov 12.


TRPV1 receptors in the CNS play a key role in broad-spectrum analgesia of TRPV1 antagonists.

Cui M, Honore P, Zhong C, Gauvin D, Mikusa J, Hernandez G, Chandran P, Gomtsyan A, Brown B, Bayburt EK, Marsh K, Bianchi B, McDonald H, Niforatos W, Neelands TR, Moreland RB, Decker MW, Lee CH, Sullivan JP, Faltynek CR.

J Neurosci. 2006 Sep 13;26(37):9385-93.


Structure-activity relationship studies on a series of novel, substituted 1-benzyl-5-phenyltetrazole P2X7 antagonists.

Nelson DW, Gregg RJ, Kort ME, Perez-Medrano A, Voight EA, Wang Y, Grayson G, Namovic MT, Donnelly-Roberts DL, Niforatos W, Honore P, Jarvis MF, Faltynek CR, Carroll WA.

J Med Chem. 2006 Jun 15;49(12):3659-66.


Involvement of the TTX-resistant sodium channel Nav 1.8 in inflammatory and neuropathic, but not post-operative, pain states.

Joshi SK, Mikusa JP, Hernandez G, Baker S, Shieh CC, Neelands T, Zhang XF, Niforatos W, Kage K, Han P, Krafte D, Faltynek C, Sullivan JP, Jarvis MF, Honore P.

Pain. 2006 Jul;123(1-2):75-82. Epub 2006 Mar 20.


Distribution and functional characterization of human Nav1.3 splice variants.

Thimmapaya R, Neelands T, Niforatos W, Davis-Taber RA, Choi W, Putman CB, Kroeger PE, Packer J, Gopalakrishnan M, Faltynek CR, Surowy CS, Scott VE.

Eur J Neurosci. 2005 Jul;22(1):1-9.


A-425619 [1-isoquinolin-5-yl-3-(4-trifluoromethyl-benzyl)-urea], a novel and selective transient receptor potential type V1 receptor antagonist, blocks channel activation by vanilloids, heat, and acid.

El Kouhen R, Surowy CS, Bianchi BR, Neelands TR, McDonald HA, Niforatos W, Gomtsyan A, Lee CH, Honore P, Sullivan JP, Jarvis MF, Faltynek CR.

J Pharmacol Exp Ther. 2005 Jul;314(1):400-9. Epub 2005 Apr 18.


Electrophysiological characterization of recombinant and native P2X receptors.

Niforatos W, Jarvis MF.

Curr Protoc Pharmacol. 2004 Oct 1;Chapter 11:Unit 11.9. doi: 10.1002/0471141755.ph1109s26.


2', 3'-O-(2,4,6,trinitrophenyl)-ATP and A-317491 are competitive antagonists at a slowly desensitizing chimeric human P2X3 receptor.

Neelands TR, Burgard EC, Uchic ME, McDonald HA, Niforatos W, Faltynek CR, Lynch KJ, Jarvis MF.

Br J Pharmacol. 2003 Sep;140(1):202-10. Epub 2003 Jul 29.


High throughput electrophysiology using a fully automated, multiplexed recording system.

Trumbull JD, Maslana ES, McKenna DG, Nemcek TA, Niforatos W, Pan JY, Parihar AS, Shieh CC, Wilkins JA, Briggs CA, Bertrand D.

Receptors Channels. 2003;9(1):19-28.


A-317491, a novel potent and selective non-nucleotide antagonist of P2X3 and P2X2/3 receptors, reduces chronic inflammatory and neuropathic pain in the rat.

Jarvis MF, Burgard EC, McGaraughty S, Honore P, Lynch K, Brennan TJ, Subieta A, Van Biesen T, Cartmell J, Bianchi B, Niforatos W, Kage K, Yu H, Mikusa J, Wismer CT, Zhu CZ, Chu K, Lee CH, Stewart AO, Polakowski J, Cox BF, Kowaluk E, Williams M, Sullivan J, Faltynek C.

Proc Natl Acad Sci U S A. 2002 Dec 24;99(26):17179-84. Epub 2002 Dec 13.


Alteration of dorsal root ganglion P2X3 receptor expression and function following spinal nerve ligation in the rat.

Kage K, Niforatos W, Zhu CZ, Lynch KJ, Honore P, Jarvis MF.

Exp Brain Res. 2002 Dec;147(4):511-9. Epub 2002 Oct 25.


Competitive antagonism of recombinant P2X(2/3) receptors by 2', 3'-O-(2,4,6-trinitrophenyl) adenosine 5'-triphosphate (TNP-ATP).

Burgard EC, Niforatos W, van Biesen T, Lynch KJ, Kage KL, Touma E, Kowaluk EA, Jarvis MF.

Mol Pharmacol. 2000 Dec;58(6):1502-10.


Molecular and functional characterization of human P2X(2) receptors.

Lynch KJ, Touma E, Niforatos W, Kage KL, Burgard EC, van Biesen T, Kowaluk EA, Jarvis MF.

Mol Pharmacol. 1999 Dec;56(6):1171-81.


Allosteric modulation and accelerated resensitization of human P2X(3) receptors by cibacron blue.

Alexander K, Niforatos W, Bianchi B, Burgard EC, Lynch KJ, Kowaluk EA, Jarvis MF, van Biesen T.

J Pharmacol Exp Ther. 1999 Dec;291(3):1135-42.


P2X receptor-mediated ionic currents in dorsal root ganglion neurons.

Burgard EC, Niforatos W, van Biesen T, Lynch KJ, Touma E, Metzger RE, Kowaluk EA, Jarvis MF.

J Neurophysiol. 1999 Sep;82(3):1590-8.


Pharmacological characterization of recombinant human and rat P2X receptor subtypes.

Bianchi BR, Lynch KJ, Touma E, Niforatos W, Burgard EC, Alexander KM, Park HS, Yu H, Metzger R, Kowaluk E, Jarvis MF, van Biesen T.

Eur J Pharmacol. 1999 Jul 2;376(1-2):127-38.


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