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Items: 32

1.

Rat NaV1.7 loss-of-function genetic model: Deficient nociceptive and neuropathic pain behavior with retained olfactory function and intra-epidermal nerve fibers.

Grubinska B, Chen L, Alsaloum M, Rampal N, Matson DJ, Yang C, Taborn K, Zhang M, Youngblood B, Liu D, Galbreath E, Allred S, Lepherd M, Ferrando R, Kornecook TJ, Lehto SG, Waxman SG, Moyer BD, Dib-Hajj S, Gingras J.

Mol Pain. 2019 Jan-Dec;15:1744806919881846. doi: 10.1177/1744806919881846. No abstract available.

2.

Discovery of TRPM8 Antagonist ( S)-6-(((3-Fluoro-4-(trifluoromethoxy)phenyl)(3-fluoropyridin-2-yl)methyl)carbamoyl)nicotinic Acid (AMG 333), a Clinical Candidate for the Treatment of Migraine.

Horne DB, Biswas K, Brown J, Bartberger MD, Clarine J, Davis CD, Gore VK, Harried S, Horner M, Kaller MR, Lehto SG, Liu Q, Ma VV, Monenschein H, Nguyen TT, Yuan CC, Youngblood BD, Zhang M, Zhong W, Allen JR, Chen JJ, Gavva NR.

J Med Chem. 2018 Sep 27;61(18):8186-8201. doi: 10.1021/acs.jmedchem.8b00518. Epub 2018 Sep 10.

PMID:
30148953
3.

TRPV1 antagonists that cause hypothermia, instead of hyperthermia, in rodents: Compounds' pharmacological profiles, in vivo targets, thermoeffectors recruited and implications for drug development.

Garami A, Pakai E, McDonald HA, Reilly RM, Gomtsyan A, Corrigan JJ, Pinter E, Zhu DXD, Lehto SG, Gavva NR, Kym PR, Romanovsky AA.

Acta Physiol (Oxf). 2018 Jul;223(3):e13038. doi: 10.1111/apha.13038. Epub 2018 Feb 16.

4.

Pharmacologic Characterization of AMG8379, a Potent and Selective Small Molecule Sulfonamide Antagonist of the Voltage-Gated Sodium Channel NaV1.7.

Kornecook TJ, Yin R, Altmann S, Be X, Berry V, Ilch CP, Jarosh M, Johnson D, Lee JH, Lehto SG, Ligutti J, Liu D, Luther J, Matson D, Ortuno D, Roberts J, Taborn K, Wang J, Weiss MM, Yu V, Zhu DXD, Fremeau RT Jr, Moyer BD.

J Pharmacol Exp Ther. 2017 Jul;362(1):146-160. doi: 10.1124/jpet.116.239590. Epub 2017 May 4.

PMID:
28473457
5.

Development of TRPM8 Antagonists to Treat Chronic Pain and Migraine.

Weyer AD, Lehto SG.

Pharmaceuticals (Basel). 2017 Mar 30;10(2). pii: E37. doi: 10.3390/ph10020037. Review.

6.

The Discovery and Hit-to-Lead Optimization of Tricyclic Sulfonamides as Potent and Efficacious Potentiators of Glycine Receptors.

Bregman H, Simard JR, Andrews KL, Ayube S, Chen H, Gunaydin H, Guzman-Perez A, Hu J, Huang L, Huang X, Krolikowski PH, Lehto SG, Lewis RT, Michelsen K, Pegman P, Plant MH, Shaffer PL, Teffera Y, Yi S, Zhang M, Gingras J, DiMauro EF.

J Med Chem. 2017 Feb 9;60(3):1105-1125. doi: 10.1021/acs.jmedchem.6b01496. Epub 2016 Dec 21.

PMID:
28001399
7.

Crystal structures of human glycine receptor α3 bound to a novel class of analgesic potentiators.

Huang X, Shaffer PL, Ayube S, Bregman H, Chen H, Lehto SG, Luther JA, Matson DJ, McDonough SI, Michelsen K, Plant MH, Schneider S, Simard JR, Teffera Y, Yi S, Zhang M, DiMauro EF, Gingras J.

Nat Struct Mol Biol. 2017 Feb;24(2):108-113. doi: 10.1038/nsmb.3329. Epub 2016 Dec 19.

PMID:
27991902
8.

Selective antagonism of TRPA1 produces limited efficacy in models of inflammatory- and neuropathic-induced mechanical hypersensitivity in rats.

Lehto SG, Weyer AD, Youngblood BD, Zhang M, Yin R, Wang W, Teffera Y, Cooke M, Stucky CL, Schenkel L, Geuns-Meyer S, Moyer BD, Wild KD, Gavva NR.

Mol Pain. 2016 Nov 29;12. pii: 1744806916677761. Print 2016.

9.

Optimization of a Novel Quinazolinone-Based Series of Transient Receptor Potential A1 (TRPA1) Antagonists Demonstrating Potent in Vivo Activity.

Schenkel LB, Olivieri PR, Boezio AA, Deak HL, Emkey R, Graceffa RF, Gunaydin H, Guzman-Perez A, Lee JH, Teffera Y, Wang W, Youngblood BD, Yu VL, Zhang M, Gavva NR, Lehto SG, Geuns-Meyer S.

J Med Chem. 2016 Mar 24;59(6):2794-809. doi: 10.1021/acs.jmedchem.6b00039. Epub 2016 Mar 4.

PMID:
26942860
10.

Pharmacologic Characterization of AMG 334, a Potent and Selective Human Monoclonal Antibody against the Calcitonin Gene-Related Peptide Receptor.

Shi L, Lehto SG, Zhu DX, Sun H, Zhang J, Smith BP, Immke DC, Wild KD, Xu C.

J Pharmacol Exp Ther. 2016 Jan;356(1):223-31. doi: 10.1124/jpet.115.227793. Epub 2015 Nov 11.

PMID:
26559125
11.

AMG2850, a potent and selective TRPM8 antagonist, is not effective in rat models of inflammatory mechanical hypersensitivity and neuropathic tactile allodynia.

Lehto SG, Weyer AD, Zhang M, Youngblood BD, Wang J, Wang W, Kerstein PC, Davis C, Wild KD, Stucky CL, Gavva NR.

Naunyn Schmiedebergs Arch Pharmacol. 2015 Apr;388(4):465-76. doi: 10.1007/s00210-015-1090-9. Epub 2015 Feb 10.

12.

Voltage-gated sodium channel function and expression in injured and uninjured rat dorsal root ganglia neurons.

Yin R, Liu D, Chhoa M, Li CM, Luo Y, Zhang M, Lehto SG, Immke DC, Moyer BD.

Int J Neurosci. 2016;126(2):182-92. doi: 10.3109/00207454.2015.1004172. Epub 2015 Apr 7.

PMID:
25562420
13.

Development of novel azabenzofuran TRPA1 antagonists as in vivo tools.

Copeland KW, Boezio AA, Cheung E, Lee J, Olivieri P, Schenkel LB, Wan Q, Wang W, Wells MC, Youngblood B, Gavva NR, Lehto SG, Geuns-Meyer S.

Bioorg Med Chem Lett. 2014 Aug 1;24(15):3464-8. doi: 10.1016/j.bmcl.2014.05.069. Epub 2014 Jun 6.

PMID:
24953819
14.

Transient receptor potential channel ankyrin-1 is not a cold sensor for autonomic thermoregulation in rodents.

de Oliveira C, Garami A, Lehto SG, Pakai E, Tekus V, Pohoczky K, Youngblood BD, Wang W, Kort ME, Kym PR, Pinter E, Gavva NR, Romanovsky AA.

J Neurosci. 2014 Mar 26;34(13):4445-52. doi: 10.1523/JNEUROSCI.5387-13.2014.

15.

Optimization of potency and pharmacokinetic properties of tetrahydroisoquinoline transient receptor potential melastatin 8 (TRPM8) antagonists.

Horne DB, Tamayo NA, Bartberger MD, Bo Y, Clarine J, Davis CD, Gore VK, Kaller MR, Lehto SG, Ma VV, Nishimura N, Nguyen TT, Tang P, Wang W, Youngblood BD, Zhang M, Gavva NR, Monenschein H, Norman MH.

J Med Chem. 2014 Apr 10;57(7):2989-3004. doi: 10.1021/jm401955h. Epub 2014 Mar 19.

PMID:
24597733
16.

Transient receptor potential melastatin 8 (TRPM8) channels are involved in body temperature regulation.

Gavva NR, Davis C, Lehto SG, Rao S, Wang W, Zhu DX.

Mol Pain. 2012 May 9;8:36. doi: 10.1186/1744-8069-8-36.

17.

Fused piperidines as a novel class of potent and orally available transient receptor potential melastatin type 8 (TRPM8) antagonists.

Tamayo NA, Bo Y, Gore V, Ma V, Nishimura N, Tang P, Deng H, Klionsky L, Lehto SG, Wang W, Youngblood B, Chen J, Correll TL, Bartberger MD, Gavva NR, Norman MH.

J Med Chem. 2012 Feb 23;55(4):1593-611. doi: 10.1021/jm2013634. Epub 2012 Feb 13.

PMID:
22329507
18.

Chromenones as potent bradykinin B1 antagonists.

Bryan MC, Biswas K, Peterkin TA, Rzasa RM, Arik L, Lehto SG, Sun H, Hsieh FY, Xu C, Fremeau RT, Allen JR.

Bioorg Med Chem Lett. 2012 Jan 1;22(1):619-22. doi: 10.1016/j.bmcl.2011.10.068. Epub 2011 Oct 28.

PMID:
22088753
19.

Discovery of potent, orally bioavailable phthalazinone bradykinin B1 receptor antagonists.

Biswas K, Peterkin TA, Bryan MC, Arik L, Lehto SG, Sun H, Hsieh FY, Xu C, Fremeau RT, Allen JR.

J Med Chem. 2011 Oct 27;54(20):7232-46. doi: 10.1021/jm200808v. Epub 2011 Sep 26.

PMID:
21902230
20.

A review of current animal models of osteoarthritis pain.

D'Souza WN, Ng GY, Youngblood BD, Tsuji W, Lehto SG.

Curr Pharm Biotechnol. 2011 Oct;12(10):1596-612. Review.

PMID:
21466452
21.

Pharmacological effects of nonselective and subtype-selective nicotinic acetylcholine receptor agonists in animal models of persistent pain.

Gao B, Hierl M, Clarkin K, Juan T, Nguyen H, Valk Mv, Deng H, Guo W, Lehto SG, Matson D, McDermott JS, Knop J, Gaida K, Cao L, Waldon D, Albrecht BK, Boezio AA, Copeland KW, Harmange JC, Springer SK, Malmberg AB, McDonough SI.

Pain. 2010 Apr;149(1):33-49. doi: 10.1016/j.pain.2010.01.007. Epub 2010 Feb 18.

PMID:
20167427
22.

Antihyperalgesic effects of (R,E)-N-(2-hydroxy-2,3-dihydro-1H-inden-4-yl)-3-(2-(piperidin-1-yl)-4-(trifluoromethyl)phenyl)-acrylamide (AMG8562), a novel transient receptor potential vanilloid type 1 modulator that does not cause hyperthermia in rats.

Lehto SG, Tamir R, Deng H, Klionsky L, Kuang R, Le A, Lee D, Louis JC, Magal E, Manning BH, Rubino J, Surapaneni S, Tamayo N, Wang T, Wang J, Wang J, Wang W, Youngblood B, Zhang M, Zhu D, Norman MH, Gavva NR.

J Pharmacol Exp Ther. 2008 Jul;326(1):218-29. doi: 10.1124/jpet.107.132233. Epub 2008 Apr 17. Erratum in: J Pharmacol Exp Ther. 2008 Sep;326(3):999.

PMID:
18420600
23.

Central pituitary adenylate cyclase 1 receptors modulate nociceptive behaviors in both inflammatory and neuropathic pain states.

Davis-Taber R, Baker S, Lehto SG, Zhong C, Surowy CS, Faltynek CR, Scott VE, Honore P.

J Pain. 2008 May;9(5):449-56. doi: 10.1016/j.jpain.2008.01.329. Epub 2008 Mar 12.

PMID:
18337184
24.

Analgesic activity of metabotropic glutamate receptor 1 antagonists on spontaneous post-operative pain in rats.

Zhu CZ, Baker S, EI-Kouhen O, Lehto SG, Hollingsworth PR, Gauvin DM, Hernandez G, Zheng G, Chang R, Moreland RB, Stewart AO, Brioni JD, Honore P.

Eur J Pharmacol. 2008 Feb 12;580(3):314-21. Epub 2007 Nov 13.

PMID:
18054908
25.

Repeated administration of vanilloid receptor TRPV1 antagonists attenuates hyperthermia elicited by TRPV1 blockade.

Gavva NR, Bannon AW, Hovland DN Jr, Lehto SG, Klionsky L, Surapaneni S, Immke DC, Henley C, Arik L, Bak A, Davis J, Ernst N, Hever G, Kuang R, Shi L, Tamir R, Wang J, Wang W, Zajic G, Zhu D, Norman MH, Louis JC, Magal E, Treanor JJ.

J Pharmacol Exp Ther. 2007 Oct;323(1):128-37. Epub 2007 Jul 25.

PMID:
17652633
26.

The vanilloid receptor TRPV1 is tonically activated in vivo and involved in body temperature regulation.

Gavva NR, Bannon AW, Surapaneni S, Hovland DN Jr, Lehto SG, Gore A, Juan T, Deng H, Han B, Klionsky L, Kuang R, Le A, Tamir R, Wang J, Youngblood B, Zhu D, Norman MH, Magal E, Treanor JJ, Louis JC.

J Neurosci. 2007 Mar 28;27(13):3366-74.

27.

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.

28.

Correlation between brain/plasma ratios and efficacy in neuropathic pain models of selective metabotropic glutamate receptor 1 antagonists.

Zheng GZ, Bhatia P, Kolasa T, Patel M, El Kouhen OF, Chang R, Uchic ME, Miller L, Baker S, Lehto SG, Honore P, Wetter JM, Marsh KC, Moreland RB, Brioni JD, Stewart AO.

Bioorg Med Chem Lett. 2006 Sep 15;16(18):4936-40. Epub 2006 Jun 30.

PMID:
16809035
29.

Influence of genotype, dose and sex on pruritogen-induced scratching behavior in the mouse.

Green AD, Young KK, Lehto SG, Smith SB, Mogil JS.

Pain. 2006 Sep;124(1-2):50-8. Epub 2006 May 11.

PMID:
16697529
30.

Structure-activity relationship of triazafluorenone derivatives as potent and selective mGluR1 antagonists.

Zheng GZ, Bhatia P, Daanen J, Kolasa T, Patel M, Latshaw S, El Kouhen OF, Chang R, Uchic ME, Miller L, Nakane M, Lehto SG, Honore MP, Moreland RB, Brioni JD, Stewart AO.

J Med Chem. 2005 Nov 17;48(23):7374-88.

PMID:
16279797
31.

Variable sensitivity to noxious heat is mediated by differential expression of the CGRP gene.

Mogil JS, Miermeister F, Seifert F, Strasburg K, Zimmermann K, Reinold H, Austin JS, Bernardini N, Chesler EJ, Hofmann HA, Hordo C, Messlinger K, Nemmani KV, Rankin AL, Ritchie J, Siegling A, Smith SB, Sotocinal S, Vater A, Lehto SG, Klussmann S, Quirion R, Michaelis M, Devor M, Reeh PW.

Proc Natl Acad Sci U S A. 2005 Sep 6;102(36):12938-43. Epub 2005 Aug 23.

32.

Electrophysiological and in vivo characterization of A-317567, a novel blocker of acid sensing ion channels.

Dubé GR, Lehto SG, Breese NM, Baker SJ, Wang X, Matulenko MA, Honoré P, Stewart AO, Moreland RB, Brioni JD.

Pain. 2005 Sep;117(1-2):88-96. Erratum in: Pain. 2005 Nov;118(1-2):281.

PMID:
16061325

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