| Name | transient receptor potential vanilloid 1 |
|---|---|
| Synonyms | Capsaicin receptor; OTRPC 1; Osm 9 like TRP channel 1; TRP vanilloid 1; TRPV 1; TRPV1; Transient receptor potential cation channel subfamily V member 1… |
| Name | piperazine |
|---|---|
| CAS | piperazine |
| PubMed | Abstract | RScore(About this table) | |
|---|---|---|---|
| 15664844 | Shao B, Huang J, Sun Q, Valenzano KJ, Schmid L, Nolan S: 4-(2-Pyridyl) piperazine-1-benzimidazoles as potent TRPV1 antagonists. . Bioorg Med Chem Lett. 2005 Feb 1;15(3):719-23. A series of 4-(2-pyridyl) piperazine-1-benzimidazole analogues based on compound 1 was synthesized and evaluated for TRPV1 antagonist activity in -induced (CAP) and pH5.5-induced (pH) FLIPR assays in a human TRPV1-expressing HEK293 cell line. |
113(1,2,2,3) | Details |
| 15771431 | Swanson DM, Dubin AE, Shah C, Nasser N, Chang L, Dax SL, Jetter M, Breitenbucher JG, Liu C, Mazur C, Lord B, Gonzales L, Hoey K, Rizzolio M, Bogenstaetter M, Codd EE, Lee DH, Zhang SP, Chaplan SR, Carruthers NI: Identification and biological evaluation of 4-(3-trifluoromethylpyridin-2-yl) piperazine-1-carboxylic acid (5-trifluoromethylpyridin-2-yl) amide, a high affinity TRPV1 (VR1) vanilloid receptor antagonist. J Med Chem. 2005 Mar 24;48(6):1857-72. |
83(1,1,1,3) | Details |
| 17690251 | Bhattacharya A, Scott BP, Nasser N, Ao H, Maher MP, Dubin AE, Swanson DM, Shankley NP, Wickenden AD, Chaplan SR: Pharmacology and antitussive efficacy of 4-(3-trifluoromethyl-pyridin-2-yl)-piperazine-1-carboxylic acid (5-trifluoromethyl-pyridin-2-yl)-amide (JNJ17203212), a transient receptor potential vanilloid 1 antagonist in guinea pigs. J Pharmacol Exp Ther. 2007 Nov;323(2):665-74. Epub 2007 Aug 9. |
68(0,2,2,8) | Details |
| 14505681 | Sun Q, Tafesse L, Islam K, Zhou X, Victory SF, Zhang C, Hachicha M, Schmid LA, Patel A, Rotshteyn Y, Valenzano KJ, Kyle DJ: 4-(2-pyridyl) piperazine-1-carboxamides: potent vanilloid receptor 1 antagonists. Bioorg Med Chem Lett. 2003 Oct 20;13(20):3611-6. |
31(0,1,1,1) | Details |
| 19539322 | Cefalu JS, Guillon MA, Burbach LR, Zhu QM, Hu DQ, Ho MJ, Ford AP, Nunn PA, Cockayne DA: Selective pharmacological blockade of the TRPV1 receptor suppresses sensory reflexes of the rodent bladder. J Urol. 2009 Aug;182(2):776-85. Epub 2009 Jun 18. |
5(0,0,0,5) | Details |
| 19275664 | Pal M, Angaru S, Kodimuthali A, Dhingra N: Vanilloid receptor antagonists: emerging class of novel anti-inflammatory agents for pain management. Curr Pharm Des. 2009;15(9):1008-26. Initially, the focus was on the development of TRPV1 agonists e.g. and resiniferatoxin (RTX) as analgesic agents through the desensitization/denervation approach. However, depending on their chemical structures all these agents can be grouped as benzenesulfonamides, cinnamides, ureas, thio-ureas, amides, benzimidazoles, and piperazine carboxamides, N-aryl-cinnamides etc. |
3(0,0,0,3) | Details |
| 18351744 | Thiel OR, Bernard C, King T, Dilmeghani-Seran M, Bostick T, Larsen RD, Faul MM: Practical synthesis of a vanilloid receptor-1 antagonist. . J Org Chem. 2008 May 2;73(9):3508-15. Epub 2008 Mar 20. Highlights of our approach include a practical route to a substituted benzothiazole, a scalable synthesis of an enantiopure piperazine fragment, and identification of conditions for selective coupling reactions on 2,6-dichloropyrimidine, to access the active pharmaceutical ingredient in high purity and overall yield. |
2(0,0,0,2) | Details |
| 16870426 | 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: From arylureas to biarylamides to aminoquinazolines: discovery of a novel, potent TRPV1 antagonist. Bioorg Med Chem Lett. 2006 Oct 1;16(19):5217-21. Epub 2006 Jul 25. Bioisosteric replacement of piperazine with an aryl ring in lead VR1 antagonist 1 led to the biarylamide series. |
1(0,0,0,1) | Details |
| 19091963 | Huang SM, Lee H, Chung MK, Park U, Yu YY, Bradshaw HB, Coulombe PA, Walker JM, Caterina MJ: Overexpressed transient receptor potential vanilloid 3 ion channels in skin keratinocytes modulate pain sensitivity via J Neurosci. 2008 Dec 17;28(51):13727-37. Upon selective pharmacological inhibition of TRPV1 with JNJ-17203212 [corrected], however, the keratinocyte-specific TRPV3 transgenic mice showed increased escape responses to noxious heat relative to their wild-type littermates. |
1(0,0,0,1) | Details |
| 16697897 | Appendino G, Szallasi A: Clinically useful vanilloid receptor TRPV1 antagonists: just around the corner (or too early to tell)? Prog Med Chem. 2006;44:145-80. |
1(0,0,0,1) | Details |