标题
Advances in TRP channel drug discovery: from target validation to clinical studies
作者
关键词
-
出版物
NATURE REVIEWS DRUG DISCOVERY
Volume -, Issue -, Pages -
出版商
Springer Science and Business Media LLC
发表日期
2021-09-15
DOI
10.1038/s41573-021-00268-4
参考文献
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注意：仅列出部分参考文献，下载原文获取全部文献信息。- TRPM3 channels play roles in heat hypersensitivity and spontaneous pain after nerve injury
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- TRPM7 is the central gatekeeper of intestinal mineral absorption essential for postnatal survival
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- Knockout of TRPC6 promotes insulin resistance and exacerbates glomerular injury in Akita mice
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- Increased lysosomal exocytosis induced by lysosomal Ca2+ channel agonists protects human dopaminergic neurons from α-synuclein toxicity
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- In vivo selective inhibition of TRPC6 by antagonist BI 749327 ameliorates fibrosis and dysfunction in cardiac and renal disease
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- TRPM 2 participates the transformation of acute pain to chronic pain during injury‐induced neuropathic pain
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- Cutaneous TRPV1+ Neurons Trigger Protective Innate Type 17 Anticipatory Immunity
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- The structure of TRPC ion channels
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- De novo substitutions of TRPM3 cause intellectual disability and epilepsy
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- Pharmacology of JNJ-28583113: A novel TRPM2 antagonist
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- Trpc5 deficiency causes hypoprolactinemia and altered function of oscillatory dopamine neurons in the arcuate nucleus
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- Reversal of Global Ischemia-Induced Cognitive Dysfunction by Delayed Inhibition of TRPM2 Ion Channels
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- Methylglyoxal-Derived Advanced Glycation Endproducts Accumulate in Multiple Sclerosis Lesions
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- Important regulatory function of transient receptor potential ankyrin 1 receptors in age-related learning and memory alterations of mice
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- A Cell-Penetrating Scorpion Toxin Enables Mode-Specific Modulation of TRPA1 and Pain
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- Dimethyl fumarate alters intracellular Ca2+ handling in immune cells by redox-mediated pleiotropic effects
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- Intravenous Glibenclamide Reduces Lesional Water Uptake in Large Hemispheric Infarction
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- Ultrasonic Neuromodulation via Astrocytic TRPA1
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- TRPV4 receptor as a functional sensory molecule in bladder urothelium: Stretch‐independent, tissue‐specific actions and pathological implications
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- Transient receptor potential (TRP) channels: Biosensors for redox environmental stimuli and cellular status
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- Discovery of Nonpungent Transient Receptor Potential Vanilloid 1 (TRPV1) Agonist as Strong Topical Analgesic
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- Phosphorylation of TRPV1 S801 Contributes to Modality-Specific Hyperalgesia in Mice
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- TRPC5 channel instability induced by depalmitoylation protects striatal neurons against oxidative stress in Huntington's disease
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- Eucalyptol alleviates inflammation and pain responses in a mouse model of gout arthritis
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- A structural overview of the ion channels of the TRPM family
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- Ca2+-permeable TRPV1 pain receptor knockout rescues memory deficits and reduces amyloid-β and tau in a mouse model of Alzheimer’s disease
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- Reduced TRPM8 expression underpins reduced migraine risk and attenuated cold pain sensation in humans
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- Transient receptor potential ankyrin 1 promoter methylation and peripheral pain sensitivity in Crohn’s disease
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- Intravesical Activation of the Cation Channel TRPV4 Improves Bladder Function in a Rat Model for Detrusor Underactivity
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- The regulatory mechanism of mammalian TRPMLs revealed by cryo-EM
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- The role of TRPV4 in fibrosis
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- Mechanistic link between diesel exhaust particles and respiratory reflexes
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- Transient receptor potential vanilloid 4–expressing macrophages and keratinocytes contribute differentially to allergic and nonallergic chronic itch
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- Deletion of the Cold Thermoreceptor TRPM8 Increases Heat Loss and Food Intake Leading to Reduced Body Temperature and Obesity in Mice
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- Inflammation Induces Epac Protein Kinase Alpha and Epsilon Signaling in TRPV1-Mediated Hyperalgesia
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- Activation of TRPV3 inhibits lipogenesis and stimulates production of inflammatory mediators in human sebocytes – a putative contributor to dry skin dermatoses
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- Discovery of TRPM8 Antagonist (S)-6-(((3-Fluoro-4-(trifluoromethoxy)phenyl)(3-fluoropyridin-2-yl)methyl)carbamoyl)nicotinic Acid (AMG 333), a Clinical Candidate for the Treatment of Migraine
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- A TRP channel trio mediates acute noxious heat sensing
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- TRPV1 mediates inflammation and hyperplasia in imiquimod (IMQ)-induced psoriasiform dermatitis (PsD) in mice
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- Antinociceptive Effects of Isosakuranetin in a Rat Model of Peripheral Neuropathy
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- The Role of Transient Receptor Potential Vanilloid 4 in Pulmonary Inflammatory Diseases
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- Loss of TRPV4 Function Suppresses Inflammatory Fibrosis Induced by Alkali-Burning Mouse Corneas
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- TRPV1-mediated Pharmacological Hypothermia Promotes Improved Functional Recovery Following Ischemic Stroke
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- Detrimental or beneficial: the role of TRPM2 in ischemia/reperfusion injury
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- Emerging roles of calcium-activated K channels and TRPV4 channels in lung oedema and pulmonary circulatory collapse
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- TRPA1 deficiency is protective in cuprizone-induced demyelination-A new target against oligodendrocyte apoptosis
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- TRPC6 G757D Loss-of-Function Mutation Associates with FSGS
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- Loss of Transient Receptor Potential Ankyrin 1 Channel Deregulates Emotion, Learning and Memory, Cognition, and Social Behavior in Mice
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- Proton-gated Ca2+-permeable TRP channels damage myelin in conditions mimicking ischaemia
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- Coding and Plasticity in the Mammalian Thermosensory System
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- TRPV1 Antagonist Suppresses Allergic Conjunctivitis in a Murine Model
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- TRPA1gene polymorphisms and childhood asthma
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- Increased activity of TRPV3 in keratinocytes in hypertrophic burn scars with postburn pruritus
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- Small molecule dual-inhibitors of TRPV4 and TRPA1 for attenuation of inflammation and pain
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- Epigenetic Regulation of Genes That Modulate Chronic Stress-Induced Visceral Pain in the Peripheral Nervous System
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- Pharmacologically-Induced Neurovascular Uncoupling is Associated with Cognitive Impairment in Mice
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- Involvement of TRPV1 and TRPA1 in Incisional Intraoral and Extraoral Pain
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- TRPM2, a Susceptibility Gene for Bipolar Disorder, Regulates Glycogen Synthase Kinase-3 Activity in the Brain
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- P2X3 receptor antagonist (AF-219) in refractory chronic cough: a randomised, double-blind, placebo-controlled phase 2 study
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- Regulation of neuropathic pain behavior by amygdaloid TRPC4/C5 channels
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- Up-regulation of lysosomal TRPML1 channels is essential for lysosomal adaptation to nutrient starvation
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- Ablation of TRPM5 in Mice Results in Reduced Body Weight Gain and Improved Glucose Tolerance and Protects from Excessive Consumption of Sweet Palatable Food when Fed High Caloric Diets
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- TRPV4 inhibition counteracts edema and inflammation and improves pulmonary function and oxygen saturation in chemically induced acute lung injury
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- The blockade of transient receptor potential ankirin 1 (TRPA1) signalling mediates antidepressant- and anxiolytic-like actions in mice
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- Transient receptor potential vanilloid 1 (TRPV1) antagonism in patients with refractory chronic cough: A double-blind randomized controlled trial
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- TRPV4 mediates myofibroblast differentiation and pulmonary fibrosis in mice
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- Decreased Anxiety-Like Behavior and G q/11-Dependent Responses in the Amygdala of Mice Lacking TRPC4 Channels
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- A rat knockout model implicates TRPC4 in visceral pain sensation
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- Transient Receptor Potential Ankyrin 1 Receptor Activation In Vitro and In Vivo by Pro-tussive Agents: GRC 17536 as a Promising Anti-Tussive Therapeutic
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- Role of transient receptor potential and pannexin channels in cigarette smoke-triggered ATP release in the lung
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- Increased Severity of Inflammation Correlates with Elevated Expression of TRPV1 Nerve Fibers and Nerve Growth Factor on Interstitial Cystitis/Bladder Pain Syndrome
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- TRPA1 channels mediate acute neurogenic inflammation and pain produced by bacterial endotoxins
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- Differential methylation of the TRPA1 promoter in pain sensitivity
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- A NewTRPV3Missense Mutation in a Patient With Olmsted Syndrome and Erythromelalgia
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- Transient receptor potential (TRP) channels in the airway: role in airway disease
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- Increased expression of bronchial epithelial transient receptor potential vanilloid 1 channels in patients with severe asthma
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- The role of trigeminal nasal TRPM8-expressing afferent neurons in the antitussive effects of menthol
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- TRPV1 and TRPA1 Antagonists Prevent the Transition of Acute to Chronic Inflammation and Pain in Chronic Pancreatitis
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- TRPA1 Channels Are Regulators of Astrocyte Basal Calcium Levels and Long-Term Potentiation via Constitutive D-Serine Release
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- TRPM4 inhibition promotes angiogenesis after ischemic stroke
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- Participation of the TRPV1 receptor in the development of acute gout attacks
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- Exome Sequencing Reveals Mutations in TRPV3 as a Cause of Olmsted Syndrome
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- TRPV1 induction in airway vagal low-threshold mechanosensory neurons by allergen challenge and neurotrophic factors
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- Crucial Role of Transient Receptor Potential Ankyrin 1 and Mast Cells in Induction of Nonallergic Airway Hyperreactivity in Mice
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- Quantitative analysis of TRP channel genes in mouse organs
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- Inhibition of airway hyper-responsiveness by TRPV1 antagonists (SB-705498 and PF-04065463) in the unanaesthetized, ovalbumin-sensitized guinea pig
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- The functions of TRPA1 and TRPV1: moving away from sensory nerves
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- Role of TRPV1 and TRPA1 in visceral hypersensitivity to colorectal distension during experimental colitis in rats
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- Regulation of Particulate Matter-Induced Mucin Secretion by Transient Receptor Potential Vanilloid 1 Receptors
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- The Sulfonylurea Receptor 1 (Sur1)-Transient Receptor Potential Melastatin 4 (Trpm4) Channel
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- Methylglyoxal Activates Nociceptors through Transient Receptor Potential Channel A1 (TRPA1)
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- TRPM2 Contributes to Inflammatory and Neuropathic Pain through the Aggravation of Pronociceptive Inflammatory Responses in Mice
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- Methylglyoxal activates the human transient receptor potential ankyrin 1 channel
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- TRPM4 cation channel mediates axonal and neuronal degeneration in experimental autoimmune encephalomyelitis and multiple sclerosis
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- Neural precursor cells induce cell death of high-grade astrocytomas through stimulation of TRPV1
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- Redox signal-mediated sensitization of transient receptor potential melastatin 2 (TRPM2) to temperature affects macrophage functions
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- Sweet taste and menthol increase cough reflex thresholds
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- Transient receptor potential genes, smoking, occupational exposures and cough in adults
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- An Orally Active TRPV4 Channel Blocker Prevents and Resolves Pulmonary Edema Induced by Heart Failure
- (2012) Kevin S. Thorneloe et al. Science Translational Medicine
- Transient receptor potential channels mediate the tussive response to prostaglandin E2and bradykinin
- (2012) Megan Grace et al. THORAX
- Therapeutic Targeting of TRP Channels - The TR(i)P to Pain Relief
- (2011) Samer R. Eid CURRENT TOPICS IN MEDICINAL CHEMISTRY
- Identification of ML204, a Novel Potent Antagonist That Selectively Modulates Native TRPC4/C5 Ion Channels
- (2011) Melissa Miller et al. JOURNAL OF BIOLOGICAL CHEMISTRY
- Rho Signaling Regulates Pannexin 1-mediated ATP Release from Airway Epithelia
- (2011) Lucia Seminario-Vidal et al. JOURNAL OF BIOLOGICAL CHEMISTRY
- Activation of Transient Receptor Potential Vanilloid-3 Inhibits Human Hair Growth
- (2011) István Borbíró et al. JOURNAL OF INVESTIGATIVE DERMATOLOGY
- Expression of functional TRPA1 receptor on human lung fibroblast and epithelial cells
- (2011) Indranil Mukhopadhyay et al. JOURNAL OF RECEPTORS AND SIGNAL TRANSDUCTION
- Transient receptor potential channels as therapeutic targets
- (2011) Magdalene M. Moran et al. NATURE REVIEWS DRUG DISCOVERY
- TRPM3 Is a Nociceptor Channel Involved in the Detection of Noxious Heat
- (2011) Joris Vriens et al. NEURON
- Oxaliplatin elicits mechanical and cold allodynia in rodents via TRPA1 receptor stimulation
- (2011) Romina Nassini et al. PAIN
- Inhibiting TRPA1 ion channel reduces loss of cutaneous nerve fiber function in diabetic animals: Sustained activation of the TRPA1 channel contributes to the pathogenesis of peripheral diabetic neuropathy
- (2011) Ari Koivisto et al. PHARMACOLOGICAL RESEARCH
- Evaluation of exhaled breath condensate pH as a biomarker for COPD
- (2011) William MacNee et al. RESPIRATORY MEDICINE
- A role for sensory nerves in the late asthmatic response
- (2011) Kristof Raemdonck et al. THORAX
- TRPV4 channels augment macrophage activation and ventilator-induced lung injury
- (2010) Kazutoshi Hamanaka et al. AMERICAN JOURNAL OF PHYSIOLOGY-LUNG CELLULAR AND MOLECULAR PHYSIOLOGY
- Extracellular ATP Is a Danger Signal Activating P2X7Receptor in Lung Inflammation and Fibrosis
- (2010) Nicolas Riteau et al. AMERICAN JOURNAL OF RESPIRATORY AND CRITICAL CARE MEDICINE
- TRP Channel Regulates EGFR Signaling in Hair Morphogenesis and Skin Barrier Formation
- (2010) Xiping Cheng et al. CELL
- TRPV1-lineage neurons are required for thermal sensation
- (2010) Santosh K Mishra et al. EMBO JOURNAL
- Motor impairment in Alzheimer’s disease and transgenic Alzheimer’s disease mouse models
- (2010) O. Wirths et al. GENES BRAIN AND BEHAVIOR
- Loss of Function of Transient Receptor Potential Vanilloid 1 (TRPV1) Genetic Variant Is Associated with Lower Risk of Active Childhood Asthma
- (2010) Gerard Cantero-Recasens et al. JOURNAL OF BIOLOGICAL CHEMISTRY
- A Gain-of-Function Mutation in TRPA1 Causes Familial Episodic Pain Syndrome
- (2010) Barbara Kremeyer et al. NEURON
- TRPM8, but not TRPA1, is required for neural and behavioral responses to acute noxious cold temperatures and cold-mimetics in vivo
- (2010) Wendy M. Knowlton et al. PAIN
- International Union of Basic and Clinical Pharmacology. LXXVI. Current Progress in the Mammalian TRP Ion Channel Family
- (2010) L.-J. Wu et al. PHARMACOLOGICAL REVIEWS
- Inhibition of the cation channel TRPV4 improves bladder function in mice and rats with cyclophosphamide-induced cystitis
- (2010) W. Everaerts et al. PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA
- TRPA1 Agonists Evoke Coughing in Guinea Pig and Human Volunteers
- (2009) Mark A. Birrell et al. AMERICAN JOURNAL OF RESPIRATORY AND CRITICAL CARE MEDICINE
- Transient receptor potential ankyrin receptor 1 is a novel target for pro-tussive agents
- (2009) E Andrè et al. BRITISH JOURNAL OF PHARMACOLOGY
- Essential Role for TRPC5 in Amygdala Function and Fear-Related Behavior
- (2009) Antonio Riccio et al. CELL
- Association of TRPV4 gene polymorphisms with chronic obstructive pulmonary disease
- (2009) G. Zhu et al. HUMAN MOLECULAR GENETICS
- Role of TRPV3 in immune response to development of dermatitis
- (2009) Kinichi Imura et al. Journal of Inflammation-London
- De novo expression of Trpm4 initiates secondary hemorrhage in spinal cord injury
- (2009) Volodymyr Gerzanich et al. NATURE MEDICINE
- The Transient Receptor Potential Vanilloid-1 Channel in Thermoregulation: A Thermosensor It Is Not
- (2009) A. A. Romanovsky et al. PHARMACOLOGICAL REVIEWS
- A sensory neuronal ion channel essential for airway inflammation and hyperreactivity in asthma
- (2009) A. I. Caceres et al. PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA
- Transient Receptor Potential Ankyrin 1 Mediates Toluene Diisocyanate–Evoked Respiratory Irritation
- (2008) Thomas E. Taylor-Clark et al. AMERICAN JOURNAL OF RESPIRATORY CELL AND MOLECULAR BIOLOGY
- Transient Receptor Potential Vanilloid-4 Has a Major Role in Visceral Hypersensitivity Symptoms
- (2008) Nicolas Cenac et al. GASTROENTEROLOGY
- TRPA1 is a major oxidant sensor in murine airway sensory neurons
- (2008) Bret F. Bessac et al. JOURNAL OF CLINICAL INVESTIGATION
- Impact of the Gly573Ser Substitution in TRPV3 on the Development of Allergic and Pruritic Dermatitis in Mice
- (2008) Takeshi Yoshioka et al. JOURNAL OF INVESTIGATIVE DERMATOLOGY
- N-((1S)-1- -3-hydroxypropanoyl)-1-piperazinyl]carbonyl}-3-methylbutyl)-1-benzothiophene-2-carboxamide (GSK1016790A), a Novel and Potent Transient Receptor Potential Vanilloid 4 Channel Agonist Induces Urinary Bladder Contraction and Hyperactivity: Part I
- (2008) K. S. Thorneloe et al. JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS
- Altered expression of TRPV1 and sensitivity to capsaicin in pulmonary myelinated afferents following chronic airway inflammation in the rat
- (2008) Guangfan Zhang et al. JOURNAL OF PHYSIOLOGY-LONDON
- GRC-6211, a New Oral Specific TRPV1 Antagonist, Decreases Bladder Overactivity and Noxious Bladder Input in Cystitis Animal Models
- (2008) Ana Charrua et al. JOURNAL OF UROLOGY
- A primer on ankyrin repeat function in TRP channels and beyond
- (2008) Rachelle Gaudet Molecular BioSystems
- Transient receptor potential channels: targeting pain at the source
- (2008) Ardem Patapoutian et al. NATURE REVIEWS DRUG DISCOVERY
- Pharmacological blockade of the vanilloid receptor TRPV1 elicits marked hyperthermia in humans
- (2008) Narender R. Gavva et al. PAIN
- Breathtaking TRP Channels: TRPA1 and TRPV1 in Airway Chemosensation and Reflex Control
- (2008) Bret F. Bessac et al. PHYSIOLOGY
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