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Items: 1 to 20 of 71

1.

Silicon switch approach in TRPV1 antagonist MK-056 and its analogues.

Chang M, Park SR, Kim J, Jang M, Park JH, Park JE, Park HG, Suh YG, Jeong YS, Park YH, Kim HD.

Bioorg Med Chem. 2010 Jan 1;18(1):111-6. doi: 10.1016/j.bmc.2009.11.014. Epub 2009 Nov 10.

PMID:
19931463
2.

(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.

PMID:
18515644
3.

Clinically useful vanilloid receptor TRPV1 antagonists: just around the corner (or too early to tell)?

Appendino G, Szallasi A.

Prog Med Chem. 2006;44:145-80. Review. No abstract available.

PMID:
16697897
4.

Design, synthesis, and biological evaluation of novel diarylalkyl amides as TRPV1 antagonists.

Li FN, Kim NJ, Paek SM, Kwon DY, Min KH, Jeong YS, Kim SY, Park YH, Kim HD, Park HG, Suh YG.

Bioorg Med Chem. 2009 May 15;17(10):3557-67. doi: 10.1016/j.bmc.2009.04.010. Epub 2009 Apr 11.

PMID:
19398205
5.

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.

PMID:
18755179
6.

Synthesis and structural optimization of multiple H-bonding region of diarylalkyl (thio)amides as novel TRPV1 antagonists.

Li FN, Kim NJ, Chang DJ, Jang J, Jang H, Jung JW, Min KH, Jeong YS, Kim SY, Park YH, Kim HD, Park HG, Suh YG.

Bioorg Med Chem. 2009 Dec 15;17(24):8149-60. doi: 10.1016/j.bmc.2009.10.043. Epub 2009 Oct 27.

PMID:
19897373
7.

Chain branching approach in structure modification of TRPV1 receptor antagonist MK056 and its analogs.

Jang M, Ryu CH, Park YH, Kim HD.

Arch Pharm Res. 2012 Feb;35(2):321-6. doi: 10.1007/s12272-012-0212-x. Epub 2012 Feb 28.

PMID:
22370786
8.

Analysis of structure-activity relationships for the 'A-region' of N-(4-t-butylbenzyl)-N'-[4-(methylsulfonylamino)benzyl]thiourea analogues as TRPV1 antagonists.

Lee J, Kang SU, Kil MJ, Shin M, Lim JO, Choi HK, Jin MK, Kim SY, Kim SE, Lee YS, Min KH, Kim YH, Ha HJ, Tran R, Welter JD, Wang Y, Szabo T, Pearce LV, Lundberg DJ, Toth A, Pavlyukovets VA, Morgan MA, Blumberg PM.

Bioorg Med Chem Lett. 2005 Sep 15;15(18):4136-42.

PMID:
16005215
9.

Novel compounds that interact with both leukotriene B4 receptors and vanilloid TRPV1 receptors.

McHugh D, McMaster RS, Pertwee RG, Roy S, Mahadevan A, Razdan RK, Ross RA.

J Pharmacol Exp Ther. 2006 Feb;316(2):955-65. Epub 2005 Oct 5.

PMID:
16207832
10.

Structure-activity studies of a novel series of 5,6-fused heteroaromatic ureas as TRPV1 antagonists.

Drizin I, Gomtsyan A, Bayburt EK, Schmidt RG, Zheng GZ, Perner RJ, DiDomenico S, Koenig JR, Turner SC, Jinkerson TK, Brown BS, Keddy RG, McDonald HA, Honore P, Wismer CT, Marsh KC, Wetter JM, Polakowski JS, Segreti JA, Jarvis MF, Faltynek CR, Lee CH.

Bioorg Med Chem. 2006 Jul 15;14(14):4740-9. Epub 2006 Apr 18.

PMID:
16621571
11.

Design, synthesis, and biological evaluation of phenylpropanamides as novel transient receptor potential vanilloid 1 antagonists.

Li FN, Kim NJ, Nam YH, Kim SH, Seo SY, Jeong YS, Kim SY, Park YH, Suh YG.

Arch Pharm Res. 2009 Sep;32(9):1201-10. doi: 10.1007/s12272-009-1903-9. Epub 2009 Sep 26.

PMID:
19784574
12.

[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.

PMID:
17660385
13.

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
14.

Trisubstituted pyrimidines as transient receptor potential vanilloid 1 (TRPV1) antagonists with improved solubility.

Wang X, Chakrabarti PP, Ognyanov VI, Pettus LH, Tamir R, Tan H, Tang P, Treanor JJ, Gavva NR, Norman MH.

Bioorg Med Chem Lett. 2007 Dec 1;17(23):6539-45. Epub 2007 Oct 15.

PMID:
17937985
15.

Substituted aryl pyrimidines as potent and soluble TRPV1 antagonists.

Stec MM, Bo Y, Chakrabarti PP, Liao L, Ncube M, Tamayo N, Tamir R, Gavva NR, Treanor JJ, Norman MH.

Bioorg Med Chem Lett. 2008 Sep 15;18(18):5118-22. doi: 10.1016/j.bmcl.2008.07.112. Epub 2008 Jul 31.

PMID:
18722118
16.

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.

17.

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
18.

Synthesis and biological evaluation of 5-substituted and 4,5-disubstituted-2-arylamino oxazole TRPV1 antagonists.

Perner RJ, Koenig JR, Didomenico S, Gomtsyan A, Schmidt RG, Lee CH, Hsu MC, McDonald HA, Gauvin DM, Joshi S, Turner TM, Reilly RM, Kym PR, Kort ME.

Bioorg Med Chem. 2010 Jul 1;18(13):4821-9. doi: 10.1016/j.bmc.2010.04.099. Epub 2010 May 10.

PMID:
20570528
19.

Synthesis of benzamide derivatives as TRPV1 antagonists.

Shishido Y, Jinno M, Ikeda T, Ito F, Sudo M, Makita N, Ohta A, Iki-Taki A, Ohmi T, Kanai Y, Tamura T, Shimojo M.

Bioorg Med Chem Lett. 2008 Feb 1;18(3):1072-8. Epub 2007 Dec 10.

PMID:
18155908
20.

Analysis of structure-activity relationships for the 'B-region' of N-(4-t-butylbenzyl)-N'-[4-(methylsulfonylamino)benzyl]-thiourea analogues as TRPV1 antagonists.

Lee J, Jin MK, Kang SU, Kim SY, Lee J, Shin M, Hwang J, Cho S, Choi YS, Choi HK, Kim SE, Suh YG, Lee YS, Kim YH, Ha HJ, Toth A, Pearce LV, Tran R, Szabo T, Welter JD, Lundberg DJ, Wang Y, Lazar J, Pavlyukovets VA, Morgan MA, Blumberg PM.

Bioorg Med Chem Lett. 2005 Sep 15;15(18):4143-50.

PMID:
15993063

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