192 related articles for article (PubMed ID: 16621571)
1. 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; 14(14):4740-9. PubMed ID: 16621571
[TBL] [Abstract][Full Text] [Related]
2. Chroman and tetrahydroquinoline ureas as potent TRPV1 antagonists.
Schmidt RG; Bayburt EK; Latshaw SP; Koenig JR; Daanen JF; McDonald HA; Bianchi BR; Zhong C; Joshi S; Honore P; Marsh KC; Lee CH; Faltynek CR; Gomtsyan A
Bioorg Med Chem Lett; 2011 Mar; 21(5):1338-41. PubMed ID: 21315587
[TBL] [Abstract][Full Text] [Related]
3. 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. PubMed ID: 19135797
[TBL] [Abstract][Full Text] [Related]
4. In vitro structure-activity relationship and in vivo characterization of 1-(aryl)-3-(4-(amino)benzyl)urea transient receptor potential vanilloid 1 antagonists.
Perner RJ; DiDomenico S; Koenig JR; Gomtsyan A; Bayburt EK; Schmidt RG; Drizin I; Zheng GZ; Turner SC; Jinkerson T; Brown BS; Keddy RG; Lukin K; McDonald HA; Honore P; Mikusa J; Marsh KC; Wetter JM; George KS; Jarvis MF; Faltynek CR; Lee CH
J Med Chem; 2007 Jul; 50(15):3651-60. PubMed ID: 17583335
[TBL] [Abstract][Full Text] [Related]
5. Heteroaryl beta-tetralin ureas as novel antagonists of human TRPV1.
Jetter MC; Youngman MA; McNally JJ; McDonnell ME; Zhang SP; Dubin AE; Nasser N; Codd EE; Flores CM; Dax SL
Bioorg Med Chem Lett; 2007 Nov; 17(22):6160-3. PubMed ID: 17892935
[TBL] [Abstract][Full Text] [Related]
6. 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; 51(3):392-5. PubMed ID: 18183945
[TBL] [Abstract][Full Text] [Related]
7. (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. PubMed ID: 18515644
[TBL] [Abstract][Full Text] [Related]
8. Discovery of SB-705498: a potent, selective and orally bioavailable TRPV1 antagonist suitable for clinical development.
Rami HK; Thompson M; Stemp G; Fell S; Jerman JC; Stevens AJ; Smart D; Sargent B; Sanderson D; Randall AD; Gunthorpe MJ; Davis JB
Bioorg Med Chem Lett; 2006 Jun; 16(12):3287-91. PubMed ID: 16580202
[TBL] [Abstract][Full Text] [Related]
9. Novel transient receptor potential vanilloid 1 receptor antagonists for the treatment of pain: structure-activity relationships for ureas with quinoline, isoquinoline, quinazoline, phthalazine, quinoxaline, and cinnoline moieties.
Gomtsyan A; Bayburt EK; Schmidt RG; Zheng GZ; Perner RJ; Didomenico S; Koenig JR; Turner S; Jinkerson T; Drizin I; Hannick SM; Macri BS; McDonald HA; Honore P; Wismer CT; Marsh KC; Wetter J; Stewart KD; Oie T; Jarvis MF; Surowy CS; Faltynek CR; Lee CH
J Med Chem; 2005 Feb; 48(3):744-52. PubMed ID: 15689158
[TBL] [Abstract][Full Text] [Related]
10. 6,6-Fused heterocyclic ureas as highly potent TRPV1 antagonists.
Sun W; Kim HS; Lee S; Jung A; Kim SE; Ann J; Yoon S; Choi S; Lee JH; Blumberg PM; Frank-Foltyn R; Bahrenberg G; Schiene K; Stockhausen H; Christoph T; Frormann S; Lee J
Bioorg Med Chem Lett; 2015 Feb; 25(4):803-6. PubMed ID: 25597011
[TBL] [Abstract][Full Text] [Related]
11. From arylureas to biarylamides to aminoquinazolines: discovery of a novel, potent TRPV1 antagonist.
Zheng X; Hodgetts KJ; Brielmann H; Hutchison A; Burkamp F; Brian Jones A; Blurton P; Clarkson R; Chandrasekhar J; Bakthavatchalam R; De Lombaert S; Crandall M; Cortright D; Blum CA
Bioorg Med Chem Lett; 2006 Oct; 16(19):5217-21. PubMed ID: 16870426
[TBL] [Abstract][Full Text] [Related]
12. Effects of the transient receptor potential vanilloid 1 antagonist A-425619 on body temperature and thermoregulation in the rat.
Mills C; McMackin M; Jaffe R; Yu J; Zininberg E; Slee D; Gogas K; Bradbury M
Neuroscience; 2008 Sep; 156(1):165-74. PubMed ID: 18706981
[TBL] [Abstract][Full Text] [Related]
13. Alpha-methylation at benzylic fragment of N-aryl-N'-benzyl ureas provides TRPV1 antagonists with better pharmacokinetic properties and higher efficacy in inflammatory pain model.
Gomtsyan A; Bayburt EK; Keddy R; Turner SC; Jinkerson TK; Didomenico S; Perner RJ; Koenig JR; Drizin I; McDonald HA; Surowy CS; Honore P; Mikusa J; Marsh KC; Wetter JM; Faltynek CR; Lee CH
Bioorg Med Chem Lett; 2007 Jul; 17(14):3894-9. PubMed ID: 17507218
[TBL] [Abstract][Full Text] [Related]
14. Design and synthesis of peripherally restricted transient receptor potential vanilloid 1 (TRPV1) antagonists.
Tamayo N; Liao H; Stec MM; Wang X; Chakrabarti P; Retz D; Doherty EM; Surapaneni S; Tamir R; Bannon AW; Gavva NR; Norman MH
J Med Chem; 2008 May; 51(9):2744-57. PubMed ID: 18386885
[TBL] [Abstract][Full Text] [Related]
15. Discovery of TRPV1 antagonist ABT-116.
Brown BS; Keddy R; Perner RJ; DiDomenico S; Koenig JR; Jinkerson TK; Hannick SM; McDonald HA; Bianchi BR; Honore P; Puttfarcken PS; Moreland RB; Marsh KC; Faltynek CR; Lee CH
Bioorg Med Chem Lett; 2010 Jun; 20(11):3291-4. PubMed ID: 20457518
[TBL] [Abstract][Full Text] [Related]
16. 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; 49(12):3719-42. PubMed ID: 16759115
[TBL] [Abstract][Full Text] [Related]
17. Discovery and synthesis of 6,7,8,9-tetrahydro-5H-pyrimido-[4,5-d]azepines as novel TRPV1 antagonists.
Hawryluk NA; Merit JE; Lebsack AD; Branstetter BJ; Hack MD; Swanson N; Ao H; Maher MP; Bhattacharya A; Wang Q; Freedman JM; Scott BP; Wickenden AD; Chaplan SR; Breitenbucher JG
Bioorg Med Chem Lett; 2010 Dec; 20(23):7137-41. PubMed ID: 20947352
[TBL] [Abstract][Full Text] [Related]
18. Analgesic potential of TRPV1 antagonists.
Kym PR; Kort ME; Hutchins CW
Biochem Pharmacol; 2009 Aug; 78(3):211-6. PubMed ID: 19481638
[TBL] [Abstract][Full Text] [Related]
19. [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. PubMed ID: 17660385
[TBL] [Abstract][Full Text] [Related]
20. 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; 50(15):3497-514. PubMed ID: 17585749
[TBL] [Abstract][Full Text] [Related]
[Next] [New Search]
