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Vol. 51, Issue 2, 159-212, June 1999

Vanilloid (Capsaicin) Receptors and Mechanisms

Arpad Szallasi1 and Peter M. Blumberg

Molecular Mechanisms of Tumor Promotion Section, Laboratory of Cellular Carcinogenesis and Tumor Promotion, National Cancer Institute, Bethesda, Maryland

I. Foreword: A Brief History of a Really "Hot" Aspect of Pharmacology
II. Introduction
    A. Overview
    B. Capsaicin: Targets and Actions
    C. Early, Indirect Evidence for and against a Vanilloid (Capsaicin) Receptor VR
III. Direct Evidence for a Vanilloid (Capsaicin) Receptor
    A. Specific Binding of resiniferatoxin (RTX), a Naturally Occurring Ultrapotent Agonist
    B. Development of Capsazepine, a Competitive Vanilloid Antagonist
    C. Cloning of the First VR, Termed VR1
IV. Anatomical Localization and Tissue Specificity of VRs
    A. VRs in Primary Sensory Neurons; Colocalization with Other Receptors, Neuropeptides, and the Isolectin B4
    B. VRs in Vagal (Nodose Ganglion) Neurons
    C. VRs in Brain
    D. Possible Presence of VRs in Nonneuronal Tissues Such as Mast Cells and Glia
V. Evidence for Multiple VRs
VI. Biochemical Pharmacology of VRs
    A. The Cloned VR Is a Nonselective Cation Channel with a Limited Selectivity for Calcium
    B. Role of Calcium in Modulating VR Functions
    C. Where Is the Vanilloid Binding Site on VRs?
    D. VR1 Is Activated by Noxious Heat and Low pH (Protons): the VR as an Integrator of Painful Chemical and Physical Stimuli
    E. Ruthenium Red Blocks VRs by an Unknown Mechanism
    F. VRs Are Sensitized by Inflammatory Mediators and Proinflammatory Cytokines
    G. Aspirin and Related Drugs May in Part Exert Their Analgesic Actions by Blocking VRs
    H. Proposed Role of Phosphorylation Sites in Modulating VR1 Activity
    I. Regulation of VR Expression
    J. VRs Are Thiol Proteins Displaying Positive Cooperativity
VII. Requirements for Ligand Recognition by VRs: Typical and Novel Vanilloids
    A. Structure-Activity Relations for Capsaicinoids
    B. Structure-Activity Relations for Resiniferanoids for Inducing Calcium Uptake by Sensory Neurons
    C. Differences in Structure-Activity Relationships of Vanilloids for Receptor Binding and Calcium Uptake
    D. Why Is RTX Ultrapotent as a Vanilloid?
    E. Novel Vanilloids Lacking 3-Hydroxy 4-methoxyphenyl (Vanillyl) Functionality
        1. Sesquiterpene Unsaturated 1,4-Dialdehydes and Related Bioactive Terpenoids.
        2. Triprenyl Phenols as Vanilloids.
        3. Implications of the Discovery of Novel Vanilloids Lacking a Vanillyl-Like Functionality.
VIII. Vanilloid Mechanisms
    A. Excitation by Vanilloids
        1. Stimulation of Vanilloid-Sensitive Neurons and Its Consequences.
        2. Hyperalgesia and Allodynia Following Vanilloid Administration.
    B. Desensitization to Vanilloids
        1. Desensitization.
        2. Tachyphylaxis.
        3. Is Lasting Tachyphylaxis Possible Without Prior Excitation?
        4. Impairment of Neuronal Functions after Vanilloid Treatment.
        4. Down-Regulation of VRs as a Mechanism of Long-Term Desensitization to Vanilloids.
        6. Messenger Plasticity by Vanilloids as a Novel Mechanism of Analgesia.
    C. Neurotoxicity by Vanilloids
IX. Diverse Biological Actions of Vanilloids; VR-Mediated and Independent Mechanism
X. Species-Related Differences in Vanilloid Actions
    A. Species-Related Differences in VR Expression
    B. Species-Related Differences in Expression of Sensory Neuropeptides and Their Receptors
    C. Human VRs
XI. Endogenous Vanilloids: Do They Exist?
XII. Vanilloids in Clinical Practice: Current Uses and Future Perspectives
    A. Counterirritation with Capsaicin
    B. Desensitization to Capsaicin
    C. Adverse Effects of Topical Capsaicin
    D. Novel, Innovative Clinical Uses
    E. RTX, an Improved Vanilloid Drug Undergoing Clinical Trials
XIII. Vanilloids: Carcinogens, Anticarcinogens, or Neither?
    A. Capsaicin
        1. Mutagenesis by Capsaicin.
        2. Carcinogenesis by Capsaicin: Animal Experiments.
        3. May Culinary Hot Pepper Consumption Be a Risk Factor for Stomach Cancer in Humans?
        4. Capsaicin: A Potential Antitumor Agent?
    B. RTX
XIV. Concluding Remarks, Emerging Principles, and Future Perspectives
Appendix
Acknowledgments
Note Added in Proof.
References


1   Address for correspondence: Arpad Szallasi, Department of Pathology, St. Louis University, 1402 South Grand Blvd., St. Louis, MO 63104. E-mail: arpads{at}thalamus.wustl.edu


0031-6997/99/5102-0159$03.00/0
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Copyright © 1999 by The American Society for Pharmacology and Experimental Therapeutics



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[Abstract] [Full Text] [PDF]


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[Abstract] [Full Text] [PDF]


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Home page
J. Neurophysiol.Home page
F. Mercado, I. A. Lopez, D. Acuna, R. Vega, and E. Soto
Acid-Sensing Ionic Channels in the Rat Vestibular Endorgans and Ganglia
J Neurophysiol, September 1, 2006; 96(3): 1615 - 1624.
[Abstract] [Full Text] [PDF]


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Anesth. Analg.Home page
I. Kissin, C. F. Freitas, and E. L. Bradley Jr
Memory of pain: the effect of perineural resiniferatoxin.
Anesth. Analg., September 1, 2006; 103(3): 721 - 728.
[Abstract] [Full Text] [PDF]


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J. Appl. Physiol.Home page
T. Ruan, Y. S. Lin, K.-S. Lin, and Y. R. Kou
Mediator mechanisms involved in TRPV1 and P2X receptor-mediated, ROS-evoked bradypneic reflex in anesthetized rats
J Appl Physiol, August 1, 2006; 101(2): 644 - 654.
[Abstract] [Full Text] [PDF]


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Endocr. Rev.Home page
H. Wang, S. K. Dey, and M. Maccarrone
Jekyll and Hyde: Two Faces of Cannabinoid Signaling in Male and Female Fertility
Endocr. Rev., August 1, 2006; 27(5): 427 - 448.
[Abstract] [Full Text] [PDF]


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J. Neurophysiol.Home page
S. Valencia-de Ita, N. B. Lawand, Q. Lin, G. Castaneda-Hernandez, and W. D. Willis
Role of the Na+-K+-2Cl- Cotransporter in the Development of Capsaicin-Induced Neurogenic Inflammation
J Neurophysiol, June 1, 2006; 95(6): 3553 - 3561.
[Abstract] [Full Text] [PDF]


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Cardiovasc ResHome page
D. Gazzieri, M. Trevisani, F. Tarantini, P. Bechi, G. Masotti, G. F. Gensini, S. Castellani, N. Marchionni, P. Geppetti, and S. Harrison
Ethanol dilates coronary arteries and increases coronary flow via transient receptor potential vanilloid 1 and calcitonin gene-related peptide
Cardiovasc Res, June 1, 2006; 70(3): 589 - 599.
[Abstract] [Full Text] [PDF]


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J. Neurophysiol.Home page
S.-R. Chen and H.-L. Pan
Loss of TRPV1-Expressing Sensory Neurons Reduces Spinal {micro} Opioid Receptors But Paradoxically Potentiates Opioid Analgesia
J Neurophysiol, May 1, 2006; 95(5): 3086 - 3096.
[Abstract] [Full Text] [PDF]


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GutHome page
M Hartel, F F di Mola, F Selvaggi, G Mascetta, M N Wente, K Felix, N A Giese, U Hinz, P Di Sebastiano, M W Buchler, et al.
Vanilloids in pancreatic cancer: potential for chemotherapy and pain management
Gut, April 1, 2006; 55(4): 519 - 528.
[Abstract] [Full Text] [PDF]


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Cancer Res.Home page
A. Mori, S. Lehmann, J. O'Kelly, T. Kumagai, J. C. Desmond, M. Pervan, W. H. McBride, M. Kizaki, and H. P. Koeffler
Capsaicin, a Component of Red Peppers, Inhibits the Growth of Androgen-Independent, p53 Mutant Prostate Cancer Cells.
Cancer Res., March 15, 2006; 66(6): 3222 - 3229.
[Abstract] [Full Text] [PDF]


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J. Pharmacol. Exp. Ther.Home page
S. Maione, T. Bisogno, V. de Novellis, E. Palazzo, L. Cristino, M. Valenti, S. Petrosino, V. Guglielmotti, F. Rossi, and V. D. Marzo
Elevation of Endocannabinoid Levels in the Ventrolateral Periaqueductal Grey through Inhibition of Fatty Acid Amide Hydrolase Affects Descending Nociceptive Pathways via Both Cannabinoid Receptor Type 1 and Transient Receptor Potential Vanilloid Type-1 Receptors
J. Pharmacol. Exp. Ther., March 1, 2006; 316(3): 969 - 982.
[Abstract] [Full Text] [PDF]


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Mol. Pharmacol.Home page
E. Lizanecz, Z. Bagi, E. T. Pasztor, Z. Papp, I. Edes, N. Kedei, P. M. Blumberg, and A. Toth
Phosphorylation-Dependent Desensitization by Anandamide of Vanilloid Receptor-1 (TRPV1) Function in Rat Skeletal Muscle Arterioles and in Chinese Hamster Ovary Cells Expressing TRPV1
Mol. Pharmacol., March 1, 2006; 69(3): 1015 - 1023.
[Abstract] [Full Text] [PDF]


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HypertensionHome page
Y. Wang and D. H. Wang
A Novel Mechanism Contributing to Development of Dahl Salt-Sensitive Hypertension: Role of the Transient Receptor Potential Vanilloid Type 1
Hypertension, March 1, 2006; 47(3): 609 - 614.
[Abstract] [Full Text] [PDF]


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J. Neurosci.Home page
F. Wei, K. I. Vadakkan, H. Toyoda, L.-J. Wu, M.-G. Zhao, H. Xu, F. W.F. Shum, Y. H. Jia, and M. Zhuo
Calcium Calmodulin-Stimulated Adenylyl Cyclases Contribute to Activation of Extracellular Signal-Regulated Kinase in Spinal Dorsal Horn Neurons in Adult Rats and Mice
J. Neurosci., January 18, 2006; 26(3): 851 - 861.
[Abstract] [Full Text] [PDF]


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Mol. Pharmacol.Home page
N. R. Gavva, R. Tamir, L. Klionsky, M. H. Norman, J.-C. Louis, K. D. Wild, and J. J. S. Treanor
Proton Activation Does Not Alter Antagonist Interaction with the Capsaicin-Binding Pocket of TRPV1
Mol. Pharmacol., December 1, 2005; 68(6): 1524 - 1533.
[Abstract] [Full Text] [PDF]


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J. Biol. Chem.Home page
P. Movahed, B. A. G. Jonsson, B. Birnir, J. A. Wingstrand, T. D. Jorgensen, A. Ermund, O. Sterner, P. M. Zygmunt, and E. D. Hogestatt
Endogenous Unsaturated C18 N-Acylethanolamines Are Vanilloid Receptor (TRPV1) Agonists
J. Biol. Chem., November 18, 2005; 280(46): 38496 - 38504.
[Abstract] [Full Text] [PDF]


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Anesth. Analg.Home page
E. Y. Kissin, C. F. Freitas, and I. Kissin
The Effects of Intraarticular Resiniferatoxin in Experimental Knee-Joint Arthritis
Anesth. Analg., November 1, 2005; 101(5): 1433 - 1439.
[Abstract] [Full Text] [PDF]


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J. Physiol.Home page
I. M Poblete, M. L. Orliac, R. Briones, E. Adler-Graschinsky, and J. P. Huidobro-Toro
Anandamide elicits an acute release of nitric oxide through endothelial TRPV1 receptor activation in the rat arterial mesenteric bed
J. Physiol., October 15, 2005; 568(2): 539 - 551.
[Abstract] [Full Text] [PDF]


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J. Appl. Physiol.Home page
M. Tartas, P. Bouye, A. Koitka, V. Jaquinandi, L. Tan, J. L. Saumet, and P. Abraham
Cathodal current-induced vasodilation to single application and the amplified response to repeated application in humans rely on aspirin-sensitive mechanisms
J Appl Physiol, October 1, 2005; 99(4): 1538 - 1544.
[Abstract] [Full Text] [PDF]


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Mol. Pharmacol.Home page
H. Yamamura, S. Ugawa, T. Ueda, M. Nagao, and S. Shimada
Icilin Activates the {delta}-Subunit of the Human Epithelial Na+ Channel
Mol. Pharmacol., October 1, 2005; 68(4): 1142 - 1147.
[Abstract] [Full Text] [PDF]


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J. Biol. Chem.Home page
E. D. Hogestatt, B. A. G. Jonsson, A. Ermund, D. A. Andersson, H. Bjork, J. P. Alexander, B. F. Cravatt, A. I. Basbaum, and P. M. Zygmunt
Conversion of Acetaminophen to the Bioactive N-Acylphenolamine AM404 via Fatty Acid Amide Hydrolase-dependent Arachidonic Acid Conjugation in the Nervous System
J. Biol. Chem., September 9, 2005; 280(36): 31405 - 31412.
[Abstract] [Full Text] [PDF]


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JDRHome page
M.H. Lee, K.-Y. Yeon, C.-K. Park, H.-Y. Li, Z. Fang, M.S. Kim, S.-Y. Choi, S.J. Lee, S. Lee, K. Park, et al.
Eugenol Inhibits Calcium Currents in Dental Afferent Neurons
Journal of Dental Research, September 1, 2005; 84(9): 848 - 851.
[Abstract] [Full Text] [PDF]


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Eur Respir JHome page
N. Frossard, E. Naline, C. Olgart Hoglund, O. Georges, and C. Advenier
Nerve growth factor is released by IL-1{beta} and induces hyperresponsiveness of the human isolated bronchus
Eur. Respir. J., July 1, 2005; 26(1): 15 - 20.
[Abstract] [Full Text] [PDF]


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J. Pharmacol. Exp. Ther.Home page
M. R. Brandt, T. A. Cummons, L. Potestio, S. J. Sukoff, and S. Rosenzweig-Lipson
Effects of the N-Methyl-D-aspartate Receptor Antagonist Perzinfotel [EAA-090; [2-(8,9-Dioxo-2,6-diazabicyclo[5.2.0]non-1(7)-en-2-yl)-ethyl]phosphonic Acid] on Chemically Induced Thermal Hypersensitivity
J. Pharmacol. Exp. Ther., June 1, 2005; 313(3): 1379 - 1386.
[Abstract] [Full Text] [PDF]


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J. Physiol.Home page
T. Ruan, Y. S. Lin, K.-S. Lin, and Y. R. Kou
Sensory transduction of pulmonary reactive oxygen species by capsaicin-sensitive vagal lung afferent fibres in rats
J. Physiol., June 1, 2005; 565(2): 563 - 578.
[Abstract] [Full Text] [PDF]


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J. Neurosci.Home page
B. Liu, C. Zhang, and F. Qin
Functional Recovery from Desensitization of Vanilloid Receptor TRPV1 Requires Resynthesis of Phosphatidylinositol 4,5-Bisphosphate
J. Neurosci., May 11, 2005; 25(19): 4835 - 4843.
[Abstract] [Full Text] [PDF]


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Mol. Endocrinol.Home page
I. Ben-Shlomo and A. J. W. Hsueh
Three's Company: Two or More Unrelated Receptors Pair with the Same Ligand
Mol. Endocrinol., May 1, 2005; 19(5): 1097 - 1109.
[Abstract] [Full Text] [PDF]


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Br J AnaesthHome page
P. M. W. Lam, J. McDonald, and D. G. Lambert
Characterization and comparison of recombinant human and rat TRPV1 receptors: effects of exo- and endocannabinoids
Br. J. Anaesth., May 1, 2005; 94(5): 649 - 656.
[Abstract] [Full Text] [PDF]


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J. Physiol.Home page
X. Wang, R. L. Miyares, and G. P Ahern
Oleoylethanolamide excites vagal sensory neurones, induces visceral pain and reduces short-term food intake in mice via capsaicin receptor TRPV1
J. Physiol., April 15, 2005; 564(2): 541 - 547.
[Abstract] [Full Text] [PDF]


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J. Biol. Chem.Home page
D. P. Mohapatra and C. Nau
Regulation of Ca2+-dependent Desensitization in the Vanilloid Receptor TRPV1 by Calcineurin and cAMP-dependent Protein Kinase
J. Biol. Chem., April 8, 2005; 280(14): 13424 - 13432.
[Abstract] [Full Text] [PDF]


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GutHome page
M Domenicali, J Ros, G Fernandez-Varo, P Cejudo-Martin, M Crespo, M Morales-Ruiz, A M Briones, J-M Campistol, V Arroyo, E Vila, et al.
Increased anandamide induced relaxation in mesenteric arteries of cirrhotic rats: role of cannabinoid and vanilloid receptors
Gut, April 1, 2005; 54(4): 522 - 527.
[Abstract] [Full Text] [PDF]


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Am. J. Pathol.Home page
E. Bodo, T. Biro, A. Telek, G. Czifra, Z. Griger, B. I. Toth, A. Mescalchin, T. Ito, A. Bettermann, L. Kovacs, et al.
A Hot New Twist to Hair Biology: Involvement of Vanilloid Receptor-1 (VR1/TRPV1) Signaling in Human Hair Growth Control
Am. J. Pathol., April 1, 2005; 166(4): 985 - 998.
[Abstract] [Full Text] [PDF]


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J. Biol. Chem.Home page
M. Bari, N. Battista, F. Fezza, A. Finazzi-Agro, and M. Maccarrone
Lipid Rafts Control Signaling of Type-1 Cannabinoid Receptors in Neuronal Cells: IMPLICATIONS FOR ANANDAMIDE-INDUCED APOPTOSIS
J. Biol. Chem., April 1, 2005; 280(13): 12212 - 12220.
[Abstract] [Full Text] [PDF]


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Am. J. Physiol. Heart Circ. Physiol.Home page
M. Tartas, P. Bouye, A. Koitka, S. Durand, Y. Gallois, J. L. Saumet, and P. Abraham
Early vasodilator response to anodal current application in human is not impaired by cyclooxygenase-2 blockade
Am J Physiol Heart Circ Physiol, April 1, 2005; 288(4): H1668 - H1673.
[Abstract] [Full Text] [PDF]


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Anesth. Analg.Home page
I. Kissin, N. Davison, and E. L. Bradley Jr
Perineural Resiniferatoxin Prevents Hyperalgesia in a Rat Model of Postoperative Pain
Anesth. Analg., March 1, 2005; 100(3): 774 - 780.
[Abstract] [Full Text] [PDF]


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Toxicol SciHome page
J. B. Morris, W. S. Wilkie, and D. J. Shusterman
Acute Respiratory Responses of the Mouse to Chlorine
Toxicol. Sci., February 1, 2005; 83(2): 380 - 387.
[Abstract] [Full Text] [PDF]


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J. Neurophysiol.Home page
Y. Ren, X. Zou, L. Fang, and Q. Lin
Sympathetic Modulation of Activity in A{delta}- and C-Primary Nociceptive Afferents After Intradermal Injection of Capsaicin in Rats
J Neurophysiol, January 1, 2005; 93(1): 365 - 377.
[Abstract] [Full Text] [PDF]


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Chem SensesHome page
M. Tominaga
Molecular Mechanisms of Trigeminal Nociception and Sensation of Pungency
Chem Senses, January 1, 2005; 30(suppl_1): i191 - i192.
[Full Text] [PDF]


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J. Physiol.Home page
S Durand, M Tartas, P Bouye, A Koitka, J. L Saumet, and P Abraham
Prostaglandins participate in the late phase of the vascular response to acetylcholine iontophoresis in humans
J. Physiol., December 15, 2004; 561(3): 811 - 819.
[Abstract] [Full Text] [PDF]


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Circ. Res.Home page
R. S. Scotland, S. Chauhan, C. Davis, C. De Felipe, S. Hunt, J. Kabir, P. Kotsonis, U. Oh, and A. Ahluwalia
Vanilloid Receptor TRPV1, Sensory C-Fibers, and Vascular Autoregulation: A Novel Mechanism Involved in Myogenic Constriction
Circ. Res., November 12, 2004; 95(10): 1027 - 1034.
[Abstract] [Full Text] [PDF]


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J. Pharmacol. Exp. Ther.Home page
S.-C. Chen, T.-J. Chang, and F.-S. Wu
Competitive Inhibition of the Capsaicin Receptor-Mediated Current by Dehydroepiandrosterone in Rat Dorsal Root Ganglion Neurons
J. Pharmacol. Exp. Ther., November 1, 2004; 311(2): 529 - 536.
[Abstract] [Full Text] [PDF]


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J. Biol. Chem.Home page
H. Yamamura, S. Ugawa, T. Ueda, M. Nagao, and S. Shimada
Capsazepine Is a Novel Activator of the {delta} Subunit of the Human Epithelial Na+ Channel
J. Biol. Chem., October 22, 2004; 279(43): 44483 - 44489.
[Abstract] [Full Text] [PDF]


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CirculationHome page
H.-L. Pan and S.-R. Chen
Sensing Tissue Ischemia: Another New Function for Capsaicin Receptors?
Circulation, September 28, 2004; 110(13): 1826 - 1831.
[Abstract] [Full Text] [PDF]


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ThoraxHome page
M Trevisani, A Milan, R Gatti, A Zanasi, S Harrison, G Fontana, A H Morice, and P Geppetti
Antitussive activity of iodo-resiniferatoxin in guinea pigs
Thorax, September 1, 2004; 59(9): 769 - 772.
[Abstract] [Full Text] [PDF]




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