Search Results - "Tamir, Rami"
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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
Published in The Journal of pharmacology and experimental therapeutics (01-07-2008)“…Antagonists of the vanilloid receptor TRPV1 (transient receptor potential vanilloid type 1) have been reported to produce antihyperalgesic effects in animal…”
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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
Published in The Journal of pharmacology and experimental therapeutics (01-04-2005)“…The vanilloid receptor 1 (VR1 or TRPV1) is a membrane-bound, nonselective cation channel expressed by peripheral sensory neurons. TRPV1 antagonists produce…”
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Species-Specific Pharmacology of Trichloro(Sulfanyl)ethyl Benzamides as Transient Receptor Potential Ankyrin 1 (TRPA1) Antagonists
Published in Molecular pain (17-12-2007)“…Agonists of TRPA1 such as mustard oil and its key component AITC cause pain and neurogenic inflammation in humans and pain behavior in rodents. TRPA1 is…”
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Molecular Determinants of Vanilloid Sensitivity in TRPV1
Published in The Journal of biological chemistry (07-05-2004)“…Vanilloid receptor 1 (TRPV1), a membrane-associated cation channel, is activated by the pungent vanilloid from chili peppers, capsaicin, and the ultra potent…”
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Repeated administration of vanilloid receptor TRPV1 antagonists attenuates hyperthermia elicited by TRPV1 blockade
Published in The Journal of pharmacology and experimental therapeutics (01-10-2007)“…Capsaicin, the active ingredient in some pain-relieving creams, is an agonist of a nonselective cation channel known as the transient receptor potential…”
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Proton activation does not alter antagonist interaction with the capsaicin-binding pocket of TRPV1
Published in Molecular pharmacology (01-12-2005)“…Vanilloid receptor 1 (TRPV1) is activated by chemical ligands (e.g., capsaicin and protons) and heat. In this study, we show that…”
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A polyclonal antibody to the prepore loop of transient receptor potential vanilloid type 1 blocks channel activation
Published in The Journal of pharmacology and experimental therapeutics (01-10-2006)“…Transient receptor potential vanilloid type 1 (TRPV1) can be activated by multiple chemical and physical stimuli such as capsaicin, anandamide, protons, and…”
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Design of Potent, Orally Available Antagonists of the Transient Receptor Potential Vanilloid 1. Structure−Activity Relationships of 2-Piperazin-1-yl-1H-benzimidazoles
Published in Journal of medicinal chemistry (15-06-2006)“…The vanilloid receptor-1 (VR1 or TRPV1) is a membrane-bound, nonselective cation channel that is predominantly expressed by peripheral neurons sensing painful…”
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KTP/532 YAG laser treatment for allergic rhinitis
Published in American journal of rhinology & allergy (01-09-2009)“…The purpose of this study was to investigate the efficacy of the KTP/532 YAG laser to reduce nasal congestion and discharge in patients with allergic rhinitis…”
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The Vanilloid Receptor TRPV1 Is Tonically Activated In Vivo and Involved in Body Temperature Regulation
Published in The Journal of neuroscience (28-03-2007)“…The vanilloid receptor TRPV1 (transient receptor potential vanilloid 1) is a cation channel that serves as a polymodal detector of pain-producing stimuli such…”
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Generation of suppressor cells in atopic patients during immunotherapy that modulate IgE synthesis
Published in Journal of allergy and clinical immunology (01-04-1987)“…We prospectively studied the effect of ragweed immunotherapy on the generation of suppressor T cells that modulate total and antiragweed IgE production in five…”
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Design and Synthesis of Peripherally Restricted Transient Receptor Potential Vanilloid 1 (TRPV1) Antagonists
Published in Journal of medicinal chemistry (08-05-2008)“…Transient receptor potential vanilloid 1 (TRPV1) channel antagonists may have clinical utility for the treatment of chronic nociceptive and neuropathic pain…”
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Novel Vanilloid Receptor-1 Antagonists: 2. Structure−Activity Relationships of 4-Oxopyrimidines Leading to the Selection of a Clinical Candidate
Published in Journal of medicinal chemistry (26-07-2007)“…A series of novel 4-oxopyrimidine TRPV1 antagonists was evaluated in assays measuring the blockade of capsaicin or acid-induced influx of calcium into CHO…”
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GDNF–Induced Activation of the Ret Protein Tyrosine Kinase Is Mediated by GDNFR-α, a Novel Receptor for GDNF
Published in Cell (28-06-1996)“…We report the expression cloning and characterization of GDNFR-α, a novel glycosylphosphatidylinositol-linked cell surface receptor for glial cell line–derived…”
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Abstract 2058: Translational regulation of SPARC by the microRNAs mir29a, b, and c
Published in Cancer research (Chicago, Ill.) (15-04-2010)“…Abstract Background: SPARC (Secreted Protein Acidic and Rich in Cysteine) is overexpressed in most cancers, including breast, prostate, lung, brain,…”
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Discovery of Potent, Orally Available Vanilloid Receptor-1 Antagonists. Structure−Activity Relationship of N-Aryl Cinnamides
Published in Journal of medicinal chemistry (13-01-2005)“…The vanilloid receptor-1 (TRPV1 or VR1) is a member of the transient receptor potential (TRP) family of ion channels and plays a role in regulating the…”
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Novel Vanilloid Receptor-1 Antagonists: 3. The Identification of a Second-Generation Clinical Candidate with Improved Physicochemical and Pharmacokinetic Properties
Published in Journal of medicinal chemistry (26-07-2007)“…Based on the previously reported clinical candidate, AMG 517 (compound 1), a series of related piperazinylpyrimidine analogues were synthesized and evaluated…”
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Novel Vanilloid Receptor-1 Antagonists: 1. Conformationally Restricted Analogues of trans-Cinnamides
Published in Journal of medicinal chemistry (26-07-2007)“…The vanilloid receptor-1 (VR1 or TRPV1) is a member of the transient receptor potential (TRP) family of ion channels and plays a role as an integrator of…”
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Structure–activity relationship (SAR) investigations of substituted imidazole analogs as TRPV1 antagonists
Published in Bioorganic & medicinal chemistry letters (01-11-2007)“…A novel series of 4,5-biarylimidazoles as TRPV1 antagonists were designed based on the previously reported 4,6-disubstituted benzimidazole series. The analogs…”
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Substituted aryl pyrimidines as potent and soluble TRPV1 antagonists
Published in Bioorganic & medicinal chemistry (15-09-2008)“…Analogs with various substituents at the R region of 3 were prepared to improve the solubility while maintaining the potent TRPV1 activity of clinical…”
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