Detalhe da pesquisa
1.
Synthesis and preliminary biological evaluation of potent and selective 2-(3-alkoxy-1-azetidinyl) quinolines as novel PDE10A inhibitors with improved solubility.
Bioorg Med Chem
; 22(23): 6570-6585, 2014 Dec 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-25456383
2.
Discovery of selective biaryl ethers as PDE10A inhibitors: improvement in potency and mitigation of Pgp-mediated efflux.
Bioorg Med Chem Lett
; 22(24): 7371-5, 2012 Dec 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-23149228
3.
Nonthermal activation of transient receptor potential vanilloid-1 channels in abdominal viscera tonically inhibits autonomic cold-defense effectors.
J Neurosci
; 27(28): 7459-68, 2007 Jul 11.
Artigo
em Inglês
| MEDLINE | ID: mdl-17626206
4.
The vanilloid receptor TRPV1 is tonically activated in vivo and involved in body temperature regulation.
J Neurosci
; 27(13): 3366-74, 2007 Mar 28.
Artigo
em Inglês
| MEDLINE | ID: mdl-17392452
5.
4-Aminopyrimidine tetrahydronaphthols: a series of novel vanilloid receptor-1 antagonists with improved solubility properties.
Bioorg Med Chem Lett
; 18(6): 1830-4, 2008 Mar 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-18299195
6.
Substituted aryl pyrimidines as potent and soluble TRPV1 antagonists.
Bioorg Med Chem Lett
; 18(18): 5118-22, 2008 Sep 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-18722118
7.
Novel vanilloid receptor-1 antagonists: 1. Conformationally restricted analogues of trans-cinnamides.
J Med Chem
; 50(15): 3497-514, 2007 Jul 26.
Artigo
em Inglês
| MEDLINE | ID: mdl-17585749
8.
Novel vanilloid receptor-1 antagonists: 2. Structure-activity relationships of 4-oxopyrimidines leading to the selection of a clinical candidate.
J Med Chem
; 50(15): 3515-27, 2007 Jul 26.
Artigo
em Inglês
| MEDLINE | ID: mdl-17585750
9.
Novel vanilloid receptor-1 antagonists: 3. The identification of a second-generation clinical candidate with improved physicochemical and pharmacokinetic properties.
J Med Chem
; 50(15): 3528-39, 2007 Jul 26.
Artigo
em Inglês
| MEDLINE | ID: mdl-17585751
10.
Trisubstituted pyrimidines as transient receptor potential vanilloid 1 (TRPV1) antagonists with improved solubility.
Bioorg Med Chem Lett
; 17(23): 6539-45, 2007 Dec 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-17937985
11.
Design of potent, orally available antagonists of the transient receptor potential vanilloid 1. Structure-activity relationships of 2-piperazin-1-yl-1H-benzimidazoles.
J Med Chem
; 49(12): 3719-42, 2006 Jun 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-16759115
12.
Discovery of potent, orally available vanilloid receptor-1 antagonists. Structure-activity relationship of N-aryl cinnamides.
J Med Chem
; 48(1): 71-90, 2005 Jan 13.
Artigo
em Inglês
| MEDLINE | ID: mdl-15634002
13.
Pharmacological blockade of the vanilloid receptor TRPV1 elicits marked hyperthermia in humans.
Pain
; 136(1-2): 202-10, 2008 May.
Artigo
em Inglês
| MEDLINE | ID: mdl-18337008
14.
Structure-activity relationship (SAR) investigations of substituted imidazole analogs as TRPV1 antagonists.
Bioorg Med Chem Lett
; 17(21): 5825-30, 2007 Nov 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-17851073
15.
Repeated administration of vanilloid receptor TRPV1 antagonists attenuates hyperthermia elicited by TRPV1 blockade.
J Pharmacol Exp Ther
; 323(1): 128-37, 2007 Oct.
Artigo
em Inglês
| MEDLINE | ID: mdl-17652633
16.
A polyclonal antibody to the prepore loop of transient receptor potential vanilloid type 1 blocks channel activation.
J Pharmacol Exp Ther
; 319(1): 192-8, 2006 Oct.
Artigo
em Inglês
| MEDLINE | ID: mdl-16844842
17.
Proton activation does not alter antagonist interaction with the capsaicin-binding pocket of TRPV1.
Mol Pharmacol
; 68(6): 1524-33, 2005 Dec.
Artigo
em Inglês
| MEDLINE | ID: mdl-16135784
18.
Synthesis and evaluation of thiazole carboxamides as vanilloid receptor 1 (TRPV1) antagonists.
Bioorg Med Chem Lett
; 15(23): 5211-7, 2005 Dec 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-16203144
19.
AMG 9810 [(E)-3-(4-t-butylphenyl)-N-(2,3-dihydrobenzo[b][1,4] dioxin-6-yl)acrylamide], a novel vanilloid receptor 1 (TRPV1) antagonist with antihyperalgesic properties.
J Pharmacol Exp Ther
; 313(1): 474-84, 2005 Apr.
Artigo
em Inglês
| MEDLINE | ID: mdl-15615864
20.
Molecular determinants of vanilloid sensitivity in TRPV1.
J Biol Chem
; 279(19): 20283-95, 2004 May 07.
Artigo
em Inglês
| MEDLINE | ID: mdl-14996838