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Results: 1 to 20 of 28


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.


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.


Pharmacology of modality-specific transient receptor potential vanilloid-1 antagonists that do not alter body temperature.

Reilly RM, McDonald HA, Puttfarcken PS, Joshi SK, Lewis L, Pai M, Franklin PH, Segreti JA, Neelands TR, Han P, Chen J, Mantyh PW, Ghilardi JR, Turner TM, Voight EA, Daanen JF, Schmidt RG, Gomtsyan A, Kort ME, Faltynek CR, Kym PR.

J Pharmacol Exp Ther. 2012 Aug;342(2):416-28. doi: 10.1124/jpet.111.190314. Epub 2012 May 8.


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.


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.


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.


Differential effects of temperature on acid-activated currents mediated by TRPV1 and ASIC channels in rat dorsal root ganglion neurons.

Neelands TR, Zhang XF, McDonald H, Puttfarcken P.

Brain Res. 2010 May 6;1329:55-66. doi: 10.1016/j.brainres.2010.02.064. Epub 2010 Mar 4.


Expression and purification of human TRPV1 in baculovirus-infected insect cells for structural studies.

Korepanova A, Pereda-Lopez A, Solomon LR, Walter KA, Lake MR, Bianchi BR, McDonald HA, Neelands TR, Shen J, Matayoshi ED, Moreland RB, Chiu ML.

Protein Expr Purif. 2009 May;65(1):38-50. doi: 10.1016/j.pep.2008.12.006. Epub 2008 Dec 13.


Elevated temperatures alter TRPV1 agonist-evoked excitability of dorsal root ganglion neurons.

Neelands TR, Jarvis MF, Faltynek CR, Surowy CS.

Inflamm Res. 2008 Sep;57(9):404-9. doi: 10.1007/s00011-008-7223-6.


Characterization of A-425619 at native TRPV1 receptors: a comparison between dorsal root ganglia and trigeminal ganglia.

McDonald HA, Neelands TR, Kort M, Han P, Vos MH, Faltynek CR, Moreland RB, Puttfarcken PS.

Eur J Pharmacol. 2008 Oct 31;596(1-3):62-9. doi: 10.1016/j.ejphar.2008.07.063. Epub 2008 Aug 5.


(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.


Transient receptor potential A1 mediates an osmotically activated ion channel.

Zhang XF, Chen J, Faltynek CR, Moreland RB, Neelands TR.

Eur J Neurosci. 2008 Feb;27(3):605-11. doi: 10.1111/j.1460-9568.2008.06030.x.


[3H]A-778317 [1-((R)-5-tert-butyl-indan-1-yl)-3-isoquinolin-5-yl-urea]: a novel, stereoselective, high-affinity antagonist is a useful radioligand for the human transient receptor potential vanilloid-1 (TRPV1) receptor.

Bianchi BR, El Kouhen R, Neelands TR, Lee CH, Gomtsyan A, Raja SN, Vaidyanathan SN, Surber B, McDonald HA, Surowy CS, Faltynek CR, Moreland RB, Jarvis MF, Puttfarcken PS.

J Pharmacol Exp Ther. 2007 Oct;323(1):285-93. Epub 2007 Jul 27.


TRPV1b overexpression negatively regulates TRPV1 responsiveness to capsaicin, heat and low pH in HEK293 cells.

Vos MH, Neelands TR, McDonald HA, Choi W, Kroeger PE, Puttfarcken PS, Faltynek CR, Moreland RB, Han P.

J Neurochem. 2006 Nov;99(4):1088-102.


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.


Acidification of rat TRPV1 alters the kinetics of capsaicin responses.

Neelands TR, Jarvis MF, Han P, Faltynek CR, Surowy CS.

Mol Pain. 2005 Sep 28;1:28.


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.


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.


SK channels are necessary but not sufficient for denervation-induced hyperexcitability.

Jacobson D, Herson PS, Neelands TR, Maylie J, Adelman JP.

Muscle Nerve. 2002 Dec;26(6):817-22.


Small-conductance calcium-activated potassium currents in mouse hyperexcitable denervated skeletal muscle.

Neelands TR, Herson PS, Jacobson D, Adelman JP, Maylie J.

J Physiol. 2001 Oct 15;536(Pt 2):397-407.

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