Format
Sort by
Items per page

Send to

Choose Destination

Links from PubMed

Items: 1 to 20 of 97

1.

Pyrido[2,3-b]pyrazines, discovery of TRPV1 antagonists with reduced potential for the formation of reactive metabolites.

Hodgetts KJ, Blum CA, Caldwell T, Bakthavatchalam R, Zheng X, Capitosti S, Krause JE, Cortright D, Crandall M, Murphy BA, Boyce S, Brian Jones A, Chenard BL.

Bioorg Med Chem Lett. 2010 Aug 1;20(15):4359-63. doi: 10.1016/j.bmcl.2010.06.069. Epub 2010 Jun 17.

PMID:
20615696
2.

Discovery of novel 6,6-heterocycles as transient receptor potential vanilloid (TRPV1) antagonists.

Blum CA, Caldwell T, Zheng X, Bakthavatchalam R, Capitosti S, Brielmann H, De Lombaert S, Kershaw MT, Matson D, Krause JE, Cortright D, Crandall M, Martin WJ, Murphy BA, Boyce S, Jones AB, Mason G, Rycroft W, Perrett H, Conley R, Burnaby-Davies N, Chenard BL, Hodgetts KJ.

J Med Chem. 2010 Apr 22;53(8):3330-48. doi: 10.1021/jm100051g.

PMID:
20307063
3.

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.

4.
5.

The effects of the TRPV1 antagonist SB-705498 on TRPV1 receptor-mediated activity and inflammatory hyperalgesia in humans.

Chizh BA, O'Donnell MB, Napolitano A, Wang J, Brooke AC, Aylott MC, Bullman JN, Gray EJ, Lai RY, Williams PM, Appleby JM.

Pain. 2007 Nov;132(1-2):132-41. Epub 2007 Jul 30.

PMID:
17659837
6.

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.

7.

Eriodictyol: a flavonoid antagonist of the TRPV1 receptor with antioxidant activity.

Rossato MF, Trevisan G, Walker CI, Klafke JZ, de Oliveira AP, Villarinho JG, Zanon RB, Royes LF, Athayde ML, Gomez MV, Ferreira J.

Biochem Pharmacol. 2011 Feb 15;81(4):544-51. doi: 10.1016/j.bcp.2010.11.004. Epub 2010 Nov 16.

8.

Design and characterization of a noncompetitive antagonist of the transient receptor potential vanilloid subunit 1 channel with in vivo analgesic and anti-inflammatory activity.

García-Martínez C, Fernández-Carvajal A, Valenzuela B, Gomis A, Van Den Nest W, Ferroni S, Carreño C, Belmonte C, Ferrer-Montiel A.

J Pain. 2006 Oct;7(10):735-46.

PMID:
17018334
9.

Identification of (R)-1-(5-tert-butyl-2,3-dihydro-1H-inden-1-yl)-3-(1H-indazol-4-yl)urea (ABT-102) as a potent TRPV1 antagonist for pain management.

Gomtsyan A, Bayburt EK, Schmidt RG, Surowy CS, Honore P, Marsh KC, Hannick SM, McDonald HA, Wetter JM, Sullivan JP, Jarvis MF, Faltynek CR, Lee CH.

J Med Chem. 2008 Feb 14;51(3):392-5. doi: 10.1021/jm701007g. Epub 2008 Jan 10.

PMID:
18183945
10.

Design of potent, orally available antagonists of the transient receptor potential vanilloid 1. Structure-activity relationships of 2-piperazin-1-yl-1H-benzimidazoles.

Ognyanov VI, Balan C, Bannon AW, Bo Y, Dominguez C, Fotsch C, Gore VK, Klionsky L, Ma VV, Qian YX, Tamir R, Wang X, Xi N, Xu S, Zhu D, Gavva NR, Treanor JJ, Norman MH.

J Med Chem. 2006 Jun 15;49(12):3719-42.

PMID:
16759115
11.

TRPV1 antagonists as a potential treatment for hyperalgesia.

Roberts LA, Connor M.

Recent Pat CNS Drug Discov. 2006 Jan;1(1):65-76. Review.

PMID:
18221192
12.

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.

14.
15.

(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.

16.

Novel vanilloid receptor-1 antagonists: 1. Conformationally restricted analogues of trans-cinnamides.

Norman MH, Zhu J, Fotsch C, Bo Y, Chen N, Chakrabarti P, Doherty EM, Gavva NR, Nishimura N, Nixey T, Ognyanov VI, Rzasa RM, Stec M, Surapaneni S, Tamir R, Viswanadhan VN, Treanor JJ.

J Med Chem. 2007 Jul 26;50(15):3497-514. Epub 2007 Jun 22.

PMID:
17585749
17.

A-425619 [1-isoquinolin-5-yl-3-(4-trifluoromethyl-benzyl)-urea], a novel transient receptor potential type V1 receptor antagonist, relieves pathophysiological pain associated with inflammation and tissue injury in rats.

Honore P, Wismer CT, Mikusa J, Zhu CZ, Zhong C, Gauvin DM, Gomtsyan A, El Kouhen R, Lee CH, Marsh K, Sullivan JP, Faltynek CR, Jarvis MF.

J Pharmacol Exp Ther. 2005 Jul;314(1):410-21. Epub 2005 Apr 18.

18.

Discovery of potent, soluble and orally active TRPV1 antagonists. Structure-activity relationships of a series of isoxazoles.

Ratcliffe P, Abernethy L, Ansari N, Cameron K, Clarkson T, Dempster M, Dunn D, Easson AM, Edwards D, Everett K, Feilden H, Ho KK, Kultgen S, Littlewood P, Maclean J, McArthur D, McGregor D, McLuskey H, Neagu I, Nimz O, Nisbet LA, Ohlmeyer M, Palin R, Pham Q, Rong Y, Roughton A, Sammons M, Swanson R, Tracey H, Walker G.

Bioorg Med Chem Lett. 2011 Aug 1;21(15):4652-7. doi: 10.1016/j.bmcl.2011.01.051. Epub 2011 Jan 26.

PMID:
21723725
19.

Identification and synthesis of 2,7-diamino-thiazolo[5,4-d]pyrimidine derivatives as TRPV1 antagonists.

Lebsack AD, Branstetter BJ, Hack MD, Xiao W, Peterson ML, Nasser N, Maher MP, Ao H, Bhattacharya A, Kansagara M, Scott BP, Luo L, Rynberg R, Rizzolio M, Chaplan SR, Wickenden AD, Guy Breitenbucher J.

Bioorg Med Chem Lett. 2009 Jan 1;19(1):40-6. doi: 10.1016/j.bmcl.2008.11.024. Epub 2008 Nov 13.

PMID:
19038548
20.

Characterization of 2-(2,6-dichloro-benzyl)-thiazolo[5,4-d]pyrimidin-7-yl]-(4-trifluoromethyl-phenyl)-amine (JNJ-39729209) as a novel TRPV1 antagonist.

Maher MP, Bhattacharya A, Ao H, Swanson N, Wu NT, Freedman J, Kansagara M, Scott B, Li DH, Eckert WA 3rd, Liu Y, Sepassi K, Rizzolio M, Fitzgerald A, Liu J, Branstetter BJ, Rech JC, Lebsack AD, Breitenbucher JG, Wickenden AD, Chaplan SR.

Eur J Pharmacol. 2011 Aug 1;663(1-3):40-50. doi: 10.1016/j.ejphar.2011.05.001. Epub 2011 May 10.

PMID:
21575625

Supplemental Content

Support Center