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Items: 23

1.

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.

PMID:
25100568
2.

Pharmacological modulation of brain activity in a preclinical model of osteoarthritis.

Upadhyay J, Baker SJ, Rajagovindan R, Hart M, Chandran P, Hooker BA, Cassar S, Mikusa JP, Tovcimak A, Wald MJ, Joshi SK, Bannon A, Medema JK, Beaver J, Honore P, Kamath RV, Fox GB, Day M.

Neuroimage. 2013 Jan 1;64:341-55. doi: 10.1016/j.neuroimage.2012.08.084. Epub 2012 Sep 7.

PMID:
22982372
3.

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.

PMID:
21402443
4.

Vogel conflict test: sex differences and pharmacological validation of the model.

Basso AM, Gallagher KB, Mikusa JP, Rueter LE.

Behav Brain Res. 2011 Mar 17;218(1):174-83. doi: 10.1016/j.bbr.2010.11.041. Epub 2010 Nov 27.

PMID:
21115068
5.

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.

PMID:
20855211
6.

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.

PMID:
20621685
7.

H4 receptor antagonism exhibits anti-nociceptive effects in inflammatory and neuropathic pain models in rats.

Hsieh GC, Chandran P, Salyers AK, Pai M, Zhu CZ, Wensink EJ, Witte DG, Miller TR, Mikusa JP, Baker SJ, Wetter JM, Marsh KC, Hancock AA, Cowart MD, Esbenshade TA, Brioni JD, Honore P.

Pharmacol Biochem Behav. 2010 Mar;95(1):41-50. doi: 10.1016/j.pbb.2009.12.004. Epub 2009 Dec 11.

PMID:
20004681
8.

Peripheral and central sites of action for the non-selective cannabinoid agonist WIN 55,212-2 in a rat model of post-operative pain.

Zhu CZ, Mikusa JP, Fan Y, Hollingsworth PR, Pai M, Chandran P, Daza AV, Yao BB, Dart MJ, Meyer MD, Decker MW, Hsieh GC, Honore P.

Br J Pharmacol. 2009 Jun;157(4):645-55. doi: 10.1111/j.1476-5381.2009.00184.x. Epub 2009 Apr 3.

9.

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.

PMID:
19135797
10.

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.

PMID:
18501613
11.

Discovery and biological evaluation of 5-aryl-2-furfuramides, potent and selective blockers of the Nav1.8 sodium channel with efficacy in models of neuropathic and inflammatory pain.

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

J Med Chem. 2008 Feb 14;51(3):407-16. doi: 10.1021/jm070637u. Epub 2008 Jan 5.

PMID:
18176998
12.
13.

A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat.

Jarvis MF, Honore P, Shieh CC, Chapman M, Joshi S, Zhang XF, Kort M, Carroll W, Marron B, Atkinson R, Thomas J, Liu D, Krambis M, Liu Y, McGaraughty S, Chu K, Roeloffs R, Zhong C, Mikusa JP, Hernandez G, Gauvin D, Wade C, Zhu C, Pai M, Scanio M, Shi L, Drizin I, Gregg R, Matulenko M, Hakeem A, Gross M, Johnson M, Marsh K, Wagoner PK, Sullivan JP, Faltynek CR, Krafte DS.

Proc Natl Acad Sci U S A. 2007 May 15;104(20):8520-5. Epub 2007 May 2.

14.

Blockade of mGluR1 receptor results in analgesia and disruption of motor and cognitive performances: effects of A-841720, a novel non-competitive mGluR1 receptor antagonist.

El-Kouhen O, Lehto SG, Pan JB, Chang R, Baker SJ, Zhong C, Hollingsworth PR, Mikusa JP, Cronin EA, Chu KL, McGaraughty SP, Uchic ME, Miller LN, Rodell NM, Patel M, Bhatia P, Mezler M, Kolasa T, Zheng GZ, Fox GB, Stewart AO, Decker MW, Moreland RB, Brioni JD, Honore P.

Br J Pharmacol. 2006 Nov;149(6):761-74. Epub 2006 Oct 3.

15.

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.

PMID:
16982702
16.

Comparison of antinociceptive actions of standard analgesics in attenuating capsaicin and nerve-injury-induced mechanical hypersensitivity.

Joshi SK, Hernandez G, Mikusa JP, Zhu CZ, Zhong C, Salyers A, Wismer CT, Chandran P, Decker MW, Honore P.

Neuroscience. 2006 Dec 1;143(2):587-96. Epub 2006 Sep 8.

PMID:
16962719
17.

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.

PMID:
16545521
18.

Central oxytocinergic and dopaminergic mechanisms regulating penile erection in conscious rats.

Martino B, Hsieh GC, Hollingsworth PR, Mikusa JP, Moreland RB, Bitner RS.

Pharmacol Biochem Behav. 2005 Aug;81(4):797-804.

PMID:
16005055
19.

Role of central and peripheral mGluR5 receptors in post-operative pain in rats.

Zhu CZ, Hsieh G, Ei-Kouhen O, Wilson SG, Mikusa JP, Hollingsworth PR, Chang R, Moreland RB, Brioni J, Decker MW, Honore P.

Pain. 2005 Mar;114(1-2):195-202. Epub 2005 Jan 21.

PMID:
15733645
20.

ABT-594 (a nicotinic acetylcholine agonist): anti-allodynia in a rat chemotherapy-induced pain model.

Lynch JJ 3rd, Wade CL, Mikusa JP, Decker MW, Honore P.

Eur J Pharmacol. 2005 Feb 10;509(1):43-8.

PMID:
15713428
21.

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.

PMID:
15588730
22.

Attenuation of mechanical allodynia by clinically utilized drugs in a rat chemotherapy-induced neuropathic pain model.

Lynch JJ 3rd, Wade CL, Zhong CM, Mikusa JP, Honore P.

Pain. 2004 Jul;110(1-2):56-63.

PMID:
15275752
23.

Central mechanisms regulating penile erection in conscious rats: the dopaminergic systems related to the proerectile effect of apomorphine.

Hsieh GC, Hollingsworth PR, Martino B, Chang R, Terranova MA, O'Neill AB, Lynch JJ, Moreland RB, Donnelly-Roberts DL, Kolasa T, Mikusa JP, McVey JM, Marsh KC, Sullivan JP, Brioni JD.

J Pharmacol Exp Ther. 2004 Jan;308(1):330-8. Epub 2003 Oct 20.

PMID:
14569075

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