Medicinal Chemistry, Pharmacology, and Clinical Implications of TRPV1 Receptor Antagonists

A Synergistic Antiobesity Effect by a Combination of Capsinoids and Cold Temperature Through Promoting Beige Adipocyte Biogenesis

(2016) Kana Ohyama et al.   DIABETES

Tyrosine Residue in the TRPV1 Vanilloid Binding Pocket Regulates Deactivation Kinetics

(2016) Rakesh Kumar et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Harnessing the Therapeutic Potential of Capsaicin and Its Analogues in Pain and Other Diseases

(2016) Shaherin Basith et al.   MOLECULES

Capsaicin, Nociception and Pain

(2016) Bárbara Frias et al.   MOLECULES

TRPV1 structures in nanodiscs reveal mechanisms of ligand and lipid action

(2016) Yuan Gao et al.   NATURE

Opioids and TRPV1 in the peripheral control of neuropathic pain – Defining a target site in the injured nerve

(2016) Dominika Labuz et al.   NEUROPHARMACOLOGY

TRP functions in the broncho-pulmonary system

(2016) Francesco De Logu et al.   Seminars in Immunopathology

TRPV1 function is modulated by Cdk5-mediated phosphorylation: insights into the molecular mechanism of nociception

(2016) Thomas Jendryke et al.   Scientific Reports

TRPV1 is crucial for proinflammatory STAT3 signaling and thermoregulation-associated pathways in the brain during inflammation

(2016) Ayaka Yoshida et al.   Scientific Reports

A combination of exercise and capsinoid supplementation additively suppresses diet-induced obesity by increasing energy expenditure in mice

(2015) Kana Ohyama et al.   AMERICAN JOURNAL OF PHYSIOLOGY-ENDOCRINOLOGY AND METABOLISM

6,6-Fused heterocyclic ureas as highly potent TRPV1 antagonists

(2015) Wei Sun et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

α-Substituted 2-(3-fluoro-4-methylsulfonamidophenyl)acetamides as potent TRPV1 antagonists

(2015) Phuong-Thao Tran et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Transient receptor potential channel modulators as pharmacological treatments for lower urinary tract symptoms (LUTS): myth or reality?

(2015) Yves Deruyver et al.   BJU INTERNATIONAL

Urinary bladder inflammation induces changes in urothelial nerve growth factor and TRPV1 channels

(2015) A Coelho et al.   BRITISH JOURNAL OF PHARMACOLOGY

Biological Activities of Red Pepper (Capsicum annuum) and Its Pungent Principle Capsaicin: A Review

(2015) Krishnapura Srinivasan   CRITICAL REVIEWS IN FOOD SCIENCE AND NUTRITION

TRPV1 Channel: A Potential Drug Target for Treating Epilepsy

(2015) Mustafa Nazıroglu   Current Neuropharmacology

TRP channels

(2015) Silvia Benemei et al.   CURRENT OPINION IN PHARMACOLOGY

Transient receptor potential vanilloid type 1 antagonists: a patent review (2011 – 2014)

(2015) Yoonji Lee et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

Transient receptor potential vanilloid type-1 channel regulates diet-induced obesity, insulin resistance, and leptin resistance

(2015) Eunjung Lee et al.   FASEB JOURNAL

Role of the Outer Pore Domain in Transient Receptor Potential Vanilloid 1 Dynamic Permeability to Large Cations

(2015) Clare H. Munns et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Benzo[d]imidazole Transient Receptor Potential Vanilloid 1 Antagonists for the Treatment of Pain: Discovery of trans-2-(2-{2-[2-(4-Trifluoromethyl-phenyl)-vinyl]-1H-benzimidazol-5-yl}-phenyl)-propan-2-ol (Mavatrep)

(2015) William H. Parsons et al.   JOURNAL OF MEDICINAL CHEMISTRY

α-Spinasterol, a TRPV1 receptor antagonist, elevates the seizure threshold in three acute seizure tests in mice

(2015) Katarzyna Socała et al.   JOURNAL OF NEURAL TRANSMISSION

Binding of Capsaicin to the TRPV1 Ion Channel

(2015) Leonardo Darré et al.   MOLECULAR PHARMACEUTICS

Structural mechanism underlying capsaicin binding and activation of the TRPV1 ion channel

(2015) Fan Yang et al.   Nature Chemical Biology

Analysis in conditional cannabinoid 1 receptor-knockout mice reveals neuronal subpopulation-specific effects on epileptogenesis in the kindling paradigm

(2015) E.L. von Rüden et al.   NEUROBIOLOGY OF DISEASE

Understanding TRPV1 activation by ligands: Insights from the binding modes of capsaicin and resiniferatoxin

(2015) Khaled Elokely et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Potential therapeutic value of TRPV1 and TRPA1 in diabetes mellitus and obesity

(2015) Andrei V. Derbenev et al.   Seminars in Immunopathology

TRPs and pain

(2015) Yi Dai   Seminars in Immunopathology

Nonpsychotropic Plant Cannabinoids, Cannabidivarin (CBDV) and Cannabidiol (CBD), Activate and Desensitize Transient Receptor Potential Vanilloid 1 (TRPV1) Channels in Vitro: Potential for the Treatment of Neuronal Hyperexcitability

(2014) Fabio Arturo Iannotti et al.   ACS Chemical Neuroscience

2-Aryl substituted pyridine C-region analogues of 2-(3-fluoro-4-methylsulfonylaminophenyl)propanamides as highly potent TRPV1 antagonists

(2014) HyungChul Ryu et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

2-Alkyl/alkenyl substituted pyridine C-region analogues of 2-(3-fluoro-4-methylsulfonylaminophenyl)propanamides as highly potent TRPV1 antagonists

(2014) HyungChul Ryu et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

α-Methylated simplified resiniferatoxin (sRTX) thiourea analogues as potent and stereospecific TRPV1 antagonists

(2014) Ho Shin Kim et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Experiences with an adaptive design for a dose-finding study in patients with osteoarthritis

(2014) Frank Miller et al.   Contemporary Clinical Trials

Tiotropium modulates transient receptor potential V1 (TRPV1) in airway sensory nerves: A beneficial off-target effect?⋆

(2014) Mark A. Birrell et al.   JOURNAL OF ALLERGY AND CLINICAL IMMUNOLOGY

Transient receptor potential vanilloid 1 (TRPV1) antagonism in patients with refractory chronic cough: A double-blind randomized controlled trial

(2014) Saifudin Khalid et al.   JOURNAL OF ALLERGY AND CLINICAL IMMUNOLOGY

Bioavailability of capsaicin and its implications for drug delivery

(2014) William D. Rollyson et al.   JOURNAL OF CONTROLLED RELEASE

Structure–Activity Relationship Studies and Discovery of a Potent Transient Receptor Potential Vanilloid (TRPV1) Antagonist 4-[3-Chloro-5-[(1S)-1,2-dihydroxyethyl]-2-pyridyl]-N-[5-(trifluoromethyl)-2-pyridyl]-3,6-dihydro-2H-pyridine-1-carboxamide (V116517) as a Clinical Candidate for Pain Management

(2014) Laykea Tafesse et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of (R)-1-(7-Chloro-2,2-bis(fluoromethyl)chroman-4-yl)-3-(3-methylisoquinolin-5-yl)urea (A-1165442): A Temperature-Neutral Transient Receptor Potential Vanilloid-1 (TRPV1) Antagonist with Analgesic Efficacy

(2014) Eric A. Voight et al.   JOURNAL OF MEDICINAL CHEMISTRY

Cannabinoid 1 and Transient Receptor Potential Vanilloid 1 Receptors Discretely Modulate Evoked Glutamate Separately from Spontaneous Glutamate Transmission

(2014) J. A. Fawley et al.   JOURNAL OF NEUROSCIENCE

Involvement of central TRPV1 receptors in pentylenetetrazole and amygdala-induced kindling in male rats

(2014) Mohsen Shirazi et al.   NEUROLOGICAL SCIENCES

A Randomised Trial Evaluating the Effects of the TRPV1 Antagonist SB705498 on Pruritus Induced by Histamine, and Cowhage Challenge in Healthy Volunteers

(2014) Rachel A. Gibson et al.   PLoS One

αCGRP is essential for algesic exocytotic mobilization of TRPV1 channels in peptidergic nociceptors

(2014) Isabel Devesa et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

TRPV1: A Potential Drug Target for Treating Various Diseases

(2014) Rafael Brito et al.   Cells

Increased function of pronociceptive TRPV1 at the level of the joint in a rat model of osteoarthritis pain

(2013) S Kelly et al.   ANNALS OF THE RHEUMATIC DISEASES

Role of CXCR2 and TRPV1 in functional, inflammatory and behavioural changes in the rat model of cyclophosphamide-induced haemorrhagic cystitis

(2013) Fabiana N Dornelles et al.   BRITISH JOURNAL OF PHARMACOLOGY

Transient receptor potential (TRP) channels in the airway: role in airway disease

(2013) M S Grace et al.   BRITISH JOURNAL OF PHARMACOLOGY

Transient receptor potential (TRP) channels: a clinical perspective

(2013) Yosuke Kaneko et al.   BRITISH JOURNAL OF PHARMACOLOGY

2-(3-Fluoro-4-methylsulfonylaminophenyl)propanamides as potent TRPV1 antagonists: Structure activity relationships of the 2-oxy pyridine C-region

(2013) Shivaji A. Thorat et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Enhanced function of TRPV1 via up-regulation by insulin-like growth factor-1 in a rat model of bone cancer pain

(2013) Y. Li et al.   EUROPEAN JOURNAL OF PAIN

TRPV1 antagonist capsazepine suppresses 4-AP-induced epileptiform activity in vitro and electrographic seizures in vivo

(2013) Luis E. Gonzalez-Reyes et al.   EXPERIMENTAL NEUROLOGY

Transient receptor potential vanilloid 1 as a therapeutic target in analgesia

(2013) János Szolcsányi et al.   EXPERT OPINION ON THERAPEUTIC TARGETS

Ethanol contributes to neurogenic pancreatitis by activation of TRPV1

(2013) Steven R. Vigna et al.   FASEB JOURNAL

Upper airway cough syndrome in children and two inflammatory factors: TRPV1 and TGF-β2

(2013) Ying-Xia Lu et al.   INTERNATIONAL JOURNAL OF PEDIATRIC OTORHINOLARYNGOLOGY

Increased expression of bronchial epithelial transient receptor potential vanilloid 1 channels in patients with severe asthma

(2013) Lorcan P. McGarvey et al.   JOURNAL OF ALLERGY AND CLINICAL IMMUNOLOGY

Promiscuous Activation of Transient Receptor Potential Vanilloid 1 (TRPV1) Channels by Negatively Charged Intracellular Lipids

(2013) Viktor Lukacs et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Vanilloid receptors—do they have a role in whole body metabolism? Evidence from TRPV1

(2013) Andrea Zsombok   JOURNAL OF DIABETES AND ITS COMPLICATIONS

Cyclophosphamide-induced cystitis reduces ASIC channel but enhances TRPV1 receptor function in rat bladder sensory neurons

(2013) Khoa Dang et al.   JOURNAL OF NEUROPHYSIOLOGY

The Orally Administered Selective TRPV1 Antagonist, JTS-653, Attenuates Chronic Pain Refractory to Non-steroidal Anti-inflammatory Drugs in Rats and Mice Including Post-herpetic Pain

(2013) Yoshihiro Kitagawa et al.   JOURNAL OF PHARMACOLOGICAL SCIENCES

Structure of the TRPV1 ion channel determined by electron cryo-microscopy

(2013) Maofu Liao et al.   NATURE

Could TRPV1-targeted analgesia of OA pain still be feasible?

(2013) David Killock   Nature Reviews Rheumatology

Oleoylethanolamide reduces L-DOPA-induced dyskinesia via TRPV1 receptor in a mouse model of Parkinson´s disease

(2013) Ramiro González-Aparicio et al.   NEUROBIOLOGY OF DISEASE

TRPV1 Channels Are Intrinsically Heat Sensitive and Negatively Regulated by Phosphoinositide Lipids

(2013) Erhu Cao et al.   NEURON

Topical application of capsaicin reduces visceral adipose fat by affecting adipokine levels in high-fat diet-induced obese mice

(2013) Gong-Rak Lee et al.   Obesity

Osteoarthritis pain mechanisms: basic studies in animal models

(2013) R.-X. Zhang et al.   OSTEOARTHRITIS AND CARTILAGE

TRPV1 antagonistic analgesic effect: A randomized study of AZD1386 in pain after third molar extraction

(2013) Hans Quiding et al.   PAIN

Effect of paclitaxel on transient receptor potential vanilloid 1 in rat dorsal root ganglion

(2013) Tomomi Hara et al.   PAIN

Randomized clinical trial: inhibition of the TRPV1 system in patients with nonerosive gastroesophageal reflux disease and a partial response to PPI treatment is not associated with analgesia to esophageal experimental pain

(2013) Anne Lund Krarup et al.   SCANDINAVIAN JOURNAL OF GASTROENTEROLOGY

Rhinovirus upregulates transient receptor potential channels in a human neuronal cell line: implications for respiratory virus-induced cough reflex sensitivity

(2013) H Abdullah et al.   THORAX

Alteration in TRPV1 and Muscarinic (M3) receptor expression and function in idiopathic overactive bladder urothelial cells

(2012) L. A. Birder et al.   Acta Physiologica

Transient receptor potential channels in bladder function

(2012) A. Avelino et al.   Acta Physiologica

Development of PAC-14028, a novel transient receptor potential vanilloid type 1 (TRPV1) channel antagonist as a new drug for refractory skin diseases

(2012) Kyung-Min Lim et al.   ARCHIVES OF PHARMACAL RESEARCH

Tetrahydro-naphthols as orally available TRPV1 inhibitors

(2012) Klaus Urbahns et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Potent and orally efficacious benzothiazole amides as TRPV1 antagonists

(2012) Yevgeni Besidski et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Discovery of novel pyrrolopyridazine scaffolds as transient receptor potential vanilloid (TRPV1) antagonists

(2012) Ismet Dorange et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Effect of analgesic therapy on clinical outcome measures in a randomized controlled trial using client-owned dogs with hip osteoarthritis

(2012) Sarah Malek et al.   BMC Veterinary Research

Effects of the TRPV1 antagonist ABT-102 on body temperature in healthy volunteers: pharmacokinetic/ pharmacodynamic analysis of three phase 1 trials

(2012) Ahmed A. Othman et al.   BRITISH JOURNAL OF CLINICAL PHARMACOLOGY

The functions of TRPA1 and TRPV1: moving away from sensory nerves

(2012) ES Fernandes et al.   BRITISH JOURNAL OF PHARMACOLOGY

Transient Receptor Potential Vanilloid Type 1-Dependent Regulation of Liver-Related Neurons in the Paraventricular Nucleus of the Hypothalamus Diminished in the Type 1 Diabetic Mouse

(2012) H. Gao et al.   DIABETES

Transient Receptor Potential Vanilloid 1 Activation Enhances Gut Glucagon-Like Peptide-1 Secretion and Improves Glucose Homeostasis

(2012) P. Wang et al.   DIABETES

Agonist- and Ca2+-dependent Desensitization of TRPV1 Channel Targets the Receptor to Lysosomes for Degradation

(2012) Lucía Sanz-Salvador et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Ischemic Neuroprotection by TRPV1 Receptor-Induced Hypothermia

(2012) Mirko Muzzi et al.   JOURNAL OF CEREBRAL BLOOD FLOW AND METABOLISM

Discovery of Novel 5,5-Diarylpentadienamides as Orally Available Transient Receptor Potential Vanilloid 1 (TRPV1) Antagonists

(2012) Osamu Saku et al.   JOURNAL OF MEDICINAL CHEMISTRY

2-(3-Fluoro-4-methylsulfonylaminophenyl)propanamides as Potent Transient Receptor Potential Vanilloid 1 (TRPV1) Antagonists: Structure–Activity Relationships of 2-Amino Derivatives in the N-(6-Trifluoromethylpyridin-3-ylmethyl) C-Region

(2012) Myeong Seop Kim et al.   JOURNAL OF MEDICINAL CHEMISTRY

Increased Expression of TRPV1 in the Cortex and Hippocampus from Patients with Mesial Temporal Lobe Epilepsy

(2012) Fei-Ji Sun et al.   JOURNAL OF MOLECULAR NEUROSCIENCE

JTS-653 Blocks Afferent Nerve Firing and Attenuates Bladder Overactivity Without Affecting Normal Voiding Function

(2012) Yoshihiro Kitagawa et al.   JOURNAL OF UROLOGY

Antiepileptic action of N-palmitoylethanolamine through CB1 and PPAR-α receptor activation in a genetic model of absence epilepsy

(2012) Rita Citraro et al.   NEUROPHARMACOLOGY

Transient receptor potential genes, smoking, occupational exposures and cough in adults

(2012) Lidwien AM Smit et al.   RESPIRATORY RESEARCH

Multisteric TRPV1 nocisensor: a target for analgesics

(2012) János Szolcsányi et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Urothelial TRPV1: TRPV1-Reporter Mice, a Way to Clarify the Debate?

(2012) Mathieu Boudes et al.   Frontiers in Physiology

Efficacy of ABT-116, an antagonist of transient receptor potential vanilloid type 1, in providing analgesia for dogs with chemically induced synovitis

(2011) Curtis J. Cathcart et al.   AMERICAN JOURNAL OF VETERINARY RESEARCH

The Ile585Val TRPV1 variant is involved in risk of painful knee osteoarthritis

(2011) A. M. Valdes et al.   ANNALS OF THE RHEUMATIC DISEASES

N-4-t-Butylbenzyl 2-(4-methylsulfonylaminophenyl) propanamide TRPV1 antagonists: Structure–activity relationships in the A-region

(2011) Yong Soo Kim et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Naphthol derivatives as TRPV1 inhibitors for the treatment of urinary incontinence

(2011) Klaus Urbahns et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Chroman and tetrahydroquinoline ureas as potent TRPV1 antagonists

(2011) Robert G. Schmidt et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Identification of potent, soluble, and orally active TRPV1 antagonists

(2011) Paul Ratcliffe et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

An investigation of the safety and pharmacokinetics of the novel TRPV1 antagonist XEN-D0501 in healthy subjects

(2011) Patrick Round et al.   BRITISH JOURNAL OF CLINICAL PHARMACOLOGY

TRPV1-Dependent and -Independent Alterations in the Limbic Cortex of Neuropathic Mice: Impact on Glial Caspases and Pain Perception

(2011) Catia Giordano et al.   CEREBRAL CORTEX

Transient receptor potential vanilloid type 1 and pain development

(2011) Enza Palazzo et al.   CURRENT OPINION IN PHARMACOLOGY

Therapeutic Targeting of TRP Channels - The TR(i)P to Pain Relief

(2011) Samer R. Eid   CURRENT TOPICS IN MEDICINAL CHEMISTRY

Characterization of Dental Nociceptive Neurons

(2011) H.Y. Kim et al.   JOURNAL OF DENTAL RESEARCH

Triazine-Based Vanilloid 1 Receptor Open Channel Blockers: Design, Synthesis, Evaluation, and SAR Analysis

(2011) Miquel Vidal-Mosquera et al.   JOURNAL OF MEDICINAL CHEMISTRY

Dietary Capsaicin Attenuates Metabolic Dysregulation in Genetically Obese Diabetic Mice

(2011) Ji-Hye Kang et al.   JOURNAL OF MEDICINAL FOOD

Functional Plasticity of Central TRPV1 Receptors in Brainstem Dorsal Vagal Complex Circuits of Streptozotocin-Treated Hyperglycemic Mice

(2011) A. Zsombok et al.   JOURNAL OF NEUROSCIENCE

Trpv1 Reporter Mice Reveal Highly Restricted Brain Distribution and Functional Expression in Arteriolar Smooth Muscle Cells

(2011) D. J. Cavanaugh et al.   JOURNAL OF NEUROSCIENCE

AKAP150-Mediated TRPV1 Sensitization is Disrupted by Calcium/Calmodulin

(2011) Sraboni Chaudhury et al.   Molecular Pain

The Blockade of the Transient Receptor Potential Vanilloid Type 1 and Fatty Acid Amide Hydrolase Decreases Symptoms and Central Sequelae in the Medial Prefrontal Cortex of Neuropathic Rats

(2011) Vito de Novellis et al.   Molecular Pain

Peripheral sensitization caused by insulin-like growth factor 1 contributes to pain hypersensitivity after tissue injury

(2011) Mayumi Miura et al.   PAIN

Oral and cutaneous thermosensory profile of selective TRPV1 inhibition by ABT-102 in a randomized healthy volunteer trial

(2011) Michael C. Rowbotham et al.   PAIN

Transient receptor potential (TRP) channels as drug targets for diseases of the digestive system

(2011) Peter Holzer   PHARMACOLOGY & THERAPEUTICS

TRP channels: Emerging targets for respiratory disease

(2011) Katharine Helen Banner et al.   PHARMACOLOGY & THERAPEUTICS

Synthesis and biological evaluation of 5-substituted and 4,5-disubstituted-2-arylamino oxazole TRPV1 antagonists

(2010) Richard J. Perner et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Discovery and synthesis of 6,7,8,9-tetrahydro-5H-pyrimido-[4,5-d]azepines as novel TRPV1 antagonists

(2010) Natalie A. Hawryluk et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

1,2-Diamino-ethane-substituted-6,7,8,9-tetrahydro-5H-pyrimido[4,5-d]azepines as TRPV1 antagonists with improved properties

(2010) Alec D. Lebsack et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Discovery of TRPV1 antagonist ABT-116

(2010) Brian S. Brown et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Structure–activity studies of a novel series of isoxazole-3-carboxamide derivatives as TRPV1 antagonists

(2010) Ronald Palin et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Drug-induced mild therapeutic hypothermia obtained by administration of a transient receptor potential vanilloid type 1 agonist

(2010) Keld Fosgerau et al.   BMC Cardiovascular Disorders

TRPV1-related modulation of spinal neuronal activity and behavior in a rat model of osteoarthritic pain

(2010) Katharine L. Chu et al.   BRAIN RESEARCH

Activation of TRPV1 by Dietary Capsaicin Improves Endothelium-Dependent Vasorelaxation and Prevents Hypertension

(2010) Dachun Yang et al.   Cell Metabolism

Binding of [3H]A-778317 to native transient receptor potential vanilloid-1 (TRPV1) channels in rat dorsal root ganglia and spinal cord

(2010) Bruce R. Bianchi et al.   EUROPEAN JOURNAL OF PHARMACOLOGY

Pre-treatment with capsaicin in a rat osteoarthritis model reduces the symptoms of pain and bone damage induced by monosodium iodoacetate

(2010) Karel-Martijn Kalff et al.   EUROPEAN JOURNAL OF PHARMACOLOGY

Effects of TRPV1 activation on synaptic excitation in the dentate gyrus of a mouse model of temporal lobe epilepsy

(2010) Muthu D. Bhaskaran et al.   EXPERIMENTAL NEUROLOGY

Expression of the TRPV1 receptor differs in quiescent inflammatory bowel disease with or without abdominal pain

(2010) A. Akbar et al.   GUT

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

Thermally Active TRPV1 Tonically Drives Central Spontaneous Glutamate Release

(2010) K. Shoudai et al.   JOURNAL OF NEUROSCIENCE

TRPV1 activation by endogenous anandamide triggers postsynaptic long-term depression in dentate gyrus

(2010) Andrés E Chávez et al.   NATURE NEUROSCIENCE

Postsynaptic TRPV1 triggers cell type–specific long-term depression in the nucleus accumbens

(2010) Brad A Grueter et al.   NATURE NEUROSCIENCE

A-995662 [(R)-8-(4-methyl-5-(4-(trifluoromethyl)phenyl)oxazol-2-ylamino)-1,2,3,4-tetrahydronaphthalen-2-ol], a novel, selective TRPV1 receptor antagonist, reduces spinal release of glutamate and CGRP in a rat knee joint pain model

(2010) Pamela S. Puttfarcken et al.   PAIN

Murine models of human neuropathic pain

(2009) Mariapia Colleoni et al.   BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR BASIS OF DISEASE

Capsaicin (TRPV1 Agonist) Therapy for Pain Relief

(2009) Helena Knotkova et al.   CLINICAL JOURNAL OF PAIN

Cerebrospinal fluid levels of the endocannabinoid anandamide are reduced in patients with untreated newly diagnosed temporal lobe epilepsy

(2009) Andrea Romigi et al.   EPILEPSIA

The acute effects of a lunch containing capsaicin on energy and substrate utilisation, hormones, and satiety

(2009) Astrid J. Smeets et al.   EUROPEAN JOURNAL OF NUTRITION

Differential contribution of SNARE-dependent exocytosis to inflammatory potentiation of TRPV1 in nociceptors

(2009) M. Camprubí-Robles et al.   FASEB JOURNAL

Functional Transient Receptor Potential Vanilloid 1 is Expressed in Human Urothelial Cells

(2009) Ana Charrua et al.   JOURNAL OF UROLOGY

Selective Pharmacological Blockade of the TRPV1 Receptor Suppresses Sensory Reflexes of the Rodent Bladder

(2009) Joseph S. Cefalu et al.   JOURNAL OF UROLOGY

TRPV1: A potential target for antiepileptogenesis

(2009) Min Fu et al.   MEDICAL HYPOTHESES

Pharmacology of Vanilloid Transient Receptor Potential Cation Channels

(2009) J. Vriens et al.   MOLECULAR PHARMACOLOGY

Behavioral assessment and identification of a molecular marker in a salicylate-induced tinnitus in rats

(2009) K. Kizawa et al.   NEUROSCIENCE

Dietary Capsaicin Reduces Obesity-induced Insulin Resistance and Hepatic Steatosis in Obese Mice Fed a High-fat Diet

(2009) Ji-Hye Kang et al.   Obesity

Repeated dosing of ABT-102, a potent and selective TRPV1 antagonist, enhances TRPV1-mediated analgesic activity in rodents, but attenuates antagonist-induced hyperthermia

(2009) Prisca Honore et al.   PAIN

Cough and gastroesophageal reflux: Insights from animal models

(2009) Marian Kollarik et al.   PULMONARY PHARMACOLOGY & THERAPEUTICS

Discovery of piperidine carboxamide TRPV1 antagonists

(2008) Wing S. Cheung et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Therapeutic potential of vanilloid receptor TRPV1 agonists and antagonists as analgesics: Recent advances and setbacks

(2008) Gilbert Y. Wong et al.   BRAIN RESEARCH REVIEWS

Identification of molecular determinants of channel gating in the transient receptor potential box of vanilloid receptor I

(2008) Pierluigi Valente et al.   FASEB JOURNAL

TRPV1-null mice are protected from diet-induced obesity

(2008) Arianne L. Motter et al.   FEBS LETTERS

Immunohistochemical Localization of Transient Receptor Potential Vanilloid Subtype 1 in the Trachea of Ovalbumin-Sensitized Guinea Pigs

(2008) Naoto Watanabe et al.   INTERNATIONAL ARCHIVES OF ALLERGY AND IMMUNOLOGY

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

(2008) Arthur Gomtsyan et al.   JOURNAL OF MEDICINAL CHEMISTRY

The TRPV1 receptor is associated with preferential stress in large dorsal root ganglion neurons in early diabetic sensory neuropathy

(2008) Shuangsong Hong et al.   JOURNAL OF NEUROCHEMISTRY

Short Interfering RNA against Transient Receptor Potential Vanilloid 1 Attenuates Cisplatin-Induced Hearing Loss in the Rat

(2008) D. Mukherjea et al.   JOURNAL OF NEUROSCIENCE

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

(2008) S. G. Lehto et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

(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

(2008) C. S. Surowy et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

Influence of TRPV1 on Diabetes-Induced Alterations in Thermal Pain Sensitivity

(2008) Reddy M Pabbidi et al.   Molecular Pain

TRPV1 shows dynamic ionic selectivity during agonist stimulation

(2008) Man-Kyo Chung et al.   NATURE NEUROSCIENCE

Proinflammatory Mediators Modulate the Heat-Activated Ion Channel TRPV1 via the Scaffolding Protein AKAP79/150

(2008) Xuming Zhang et al.   NEURON

Lack of TRPV1 inhibits cystitis-induced increased mechanical sensitivity in mice

(2008) Zun-Yi Wang et al.   PAIN

Structure of TRPV1 channel revealed by electron cryomicroscopy

(2008) V. Y. Moiseenkova-Bell et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Body-temperature maintenance as the predominant function of the vanilloid receptor TRPV1

(2008) Narender R. Gavva   TRENDS IN PHARMACOLOGICAL SCIENCES

Stereospecific High-affinity TRPV1 Antagonists: ChiralN-(2-Benzyl-3-pivaloyloxypropyl) 2-[4-(methylsulfonylamino)phenyl]propionamide Analogues

(2007) HyungChul Ryu et al.   JOURNAL OF MEDICINAL CHEMISTRY

Homologous and heterologous desensitization of capsaicin and mustard oil responses utilize different cellular pathways in nociceptors

(2007) Nikita B. Ruparel et al.   PAIN

The emerging role of TRPV1 in diabetes and obesity

(2007) Anish Suri et al.   TRENDS IN PHARMACOLOGICAL SCIENCES