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1
المؤلفون: Kathy Sarris, Philip J. Hajduk, Ihle David C, Diana L. Donnelly-Roberts, Arthur Gomtsyan, Christian Goess, David B. Duignan, Danying Song, Chaohong Sun, Andrea Mcclure, Adrian D. Hobson, Robert H. Stoffel, Anil Vasudevan, John A. Mankovich, Sanjay C. Panchal, A. Chris Krueger, Steven L. Swann, Kenneth M. Comess, Andrew M. Petros, Wilson Noel S, Jill M. Wetter, Paul G. Richardson, Kenton L. Longenecker, Paul M. Jung, Vincent S. Stoll, Amanda W. Dombrowski, Suzanne Mathieu, Justin D. Dietrich, Philip B. Cox
المصدر: Journal of Medicinal Chemistry. 64:417-429
مصطلحات موضوعية: Drug, media_common.quotation_subject, medicine.medical_treatment, Allosteric regulation, Administration, Oral, Arthritis, Pharmacology, Ligands, 01 natural sciences, Autoimmune Diseases, Arthritis, Rheumatoid, Mice, 03 medical and health sciences, Allosteric Regulation, In vivo, Drug Discovery, medicine, Animals, 030304 developmental biology, media_common, Biological Products, 0303 health sciences, Tumor Necrosis Factor-alpha, Chemistry, Drug discovery, medicine.disease, Small molecule, 0104 chemical sciences, 010404 medicinal & biomolecular chemistry, Cytokine, Drug Design, Molecular Medicine, Tumor necrosis factor alpha
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2
المؤلفون: Jill-Desiree Brederson, Michael J. Dart, Robert G. Schmidt, Steve McGaraughty, Philip R. Kym, Arthur Gomtsyan, Laura Leys, Katharine L. Chu, Richard J. Radek, Jun Xu
المصدر: Journal of Neurophysiology. 118:904-916
مصطلحات موضوعية: Male, Nociception, 0301 basic medicine, TRPV3, Physiology, Action Potentials, TRPV Cation Channels, Nociceptive Pain, Rats, Sprague-Dawley, Tissue Culture Techniques, 03 medical and health sciences, 0302 clinical medicine, Ganglia, Spinal, Membrane Transport Modulators, Afferent, Animals, Medicine, Pain modulation, business.industry, General Neuroscience, Brain, Nociceptors, Analgesics, Non-Narcotic, Peripheral, Disease Models, Animal, Electrophysiology, 030104 developmental biology, Spinal Cord, Rostral ventromedial medulla, Sleep, business, Neuroscience, 030217 neurology & neurosurgery, Research Article
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3
المؤلفون: Philip R. Kym, Arthur Gomtsyan, Gregory A. Gfesser, Bin Li, Regina M. Reilly, Bruce Clapham, Jerome F. Daanen, Rodger F. Henry, Torben R. Neelands, Pamela S. Puttfarcken, Susan M. Huang, Robert G. Schmidt, Robert J. Altenbach, S.K. Joshi, Huaqing Liu, Marlon D. Cowart, David N. Whittern, Phil B. Cox, Jill-Desiree Brederson, Michael J. Dart, Anurupa Shrestha, Donna Gauvin, Michael E. Kort, Erol K. Bayburt, Ping Song, Steve McGaraughty, Connie R. Faltynek, Heath A. McDonald, Patricia N. Banfor, Diana Schmidt, Eric A. Voight, Mohamad Shebley, Jason A. Segreti
المصدر: Journal of Medicinal Chemistry. 59:4926-4947
مصطلحات موضوعية: TRPV3, Pyridines, Molecular Conformation, TRPV Cation Channels, Pharmacology, 010402 general chemistry, 01 natural sciences, Structure-Activity Relationship, Transient receptor potential channel, Drug Discovery, medicine, Humans, Structure–activity relationship, Selective receptor modulator, ADME, Dose-Response Relationship, Drug, 010405 organic chemistry, Chemistry, Antagonist, Reserpine, 0104 chemical sciences, HEK293 Cells, Neuropathic pain, Molecular Medicine, Calcium, Cyclobutanes, medicine.drug
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4
المؤلفون: Arthur Gomtsyan, Kort Michael E, Michael J. Dart, Regina M. Reilly, Jason A. Segreti, Heath A. McDonald, Philip R. Kym, Pamela S. Puttfarcken, Robert G. Schmidt, Jerome F. Daanen, Voight Eric
المصدر: Temperature: Multidisciplinary Biomedical Journal
مصطلحات موضوعية: Hyperthermia, Compound 3, (R)-1-(2,2-dimethyl-8-(trifluoromethoxy)chroman-4-yl)-3-(3-methylisoquinolin-5-yl)urea, Physiology, TRPV1, Context (language use), Partial agonist, Transient receptor potential channel, FLIPR, fluorometric imaging plate reader, Compound 2, (R)-1-(2,2-dimethyl-7-(trifluoromethyl)chroman-4-yl)-3-(3-methylisoquinolin-5-yl)urea, Physiology (medical), TRPV1, transient receptor potential vanilloid 1, medicine, 5′-iodo-RTX, Ion channel, Compound 1, (R)-1-(2,2-dimethyl-7-(trifluoromethyl)chroman-4-yl)-3-(3,6-dimethylisoquinolin-5-yl)urea, thermoregulation, Drug discovery, Chemistry, TRPV1 agonists, Thermoregulation, hyperthermia, 5′-I-RTX, 5′-iodo-resiniferatoxi, medicine.disease, TRPV1 antagonists, chromanyl ureas, Biochemistry, Biophysics, OA, osteoarthritis, hypothermia, Research Paper
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5Stereoselective Synthesis of a Dipyridyl Transient Receptor Potential Vanilloid-3 (TRPV3) Antagonist
المؤلفون: Robert G. Schmidt, Jerome F. Daanen, Arthur Gomtsyan, Philip R. Kym, Michael J. Dart, Eric A. Voight
المصدر: The Journal of organic chemistry. 81(23)
مصطلحات موضوعية: chemistry.chemical_classification, TRPV3, Spectrometry, Mass, Electrospray Ionization, Ketone, 010405 organic chemistry, Hydrosilylation, Alkene, Stereochemistry, Pyridines, Proton Magnetic Resonance Spectroscopy, Organic Chemistry, Antagonist, Enantioselective synthesis, TRPV Cation Channels, Nanotechnology, Stereoisomerism, 010402 general chemistry, 01 natural sciences, 0104 chemical sciences, chemistry.chemical_compound, chemistry, Humans, Stereoselectivity, Carbon-13 Magnetic Resonance Spectroscopy
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6
المؤلفون: Jerome F. Daanen, Joseph P. Mikusa, Chih Hung Lee, Chengmin Zhong, Jason A. Segreti, Patrick W. Mantyh, Torben R. Neelands, Patricia N. Banfor, Michael F. Jarvis, Arthur Gomtsyan, Prasant Chandran, Molly A. Sevcik, Philip R. Kym, Donna M. Gauvin, Regina M. Reilly, Kennan C. Marsh, Michael E. Kort, Connie R. Faltynek, James P. Sullivan, Erol K. Bayburt, Carol S. Surowy, Joseph R. Ghilardi, Prisca Honore, Gricelda Hernandez, Ryan M. Fryer, Shailen K. Joshi
المصدر: Pain. 142:27-35
مصطلحات موضوعية: Male, Pain Threshold, Hyperthermia, Indazoles, Fever, Analgesic, TRPV1, Pain, TRPV Cation Channels, Bone Neoplasms, Motor Activity, Pharmacology, Body Temperature, Rats, Sprague-Dawley, Mice, Transient receptor potential channel, chemistry.chemical_compound, Osteoarthritis, Threshold of pain, Animals, Urea, Medicine, Drug Interactions, Pain Measurement, Inflammation, Analgesics, Mice, Inbred C3H, business.industry, Antagonist, medicine.disease, Rats, Disease Models, Animal, Anesthesiology and Pain Medicine, Nociception, Neurology, chemistry, Capsaicin, Calcium, Neurology (clinical), business
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7
المؤلفون: Carol S. Surowy, Katharine L. Chu, Prisca Honore, Rachid El Kouhen, Connie R. Faltynek, Bruce R. Bianchi, Ping Han, James P. Sullivan, Steve McGaraughty, Wende Niforatos, Arthur Gomtsyan, Erol K. Bayburt, Chih-Hung Lee, Torben R. Neelands, Heath A. McDonald, Melissa H. Vos, Michael F. Jarvis
المصدر: Journal of Pharmacology and Experimental Therapeutics. 326:879-888
مصطلحات موضوعية: Male, Agonist, Hot Temperature, Indazoles, medicine.drug_class, TRPV1, Action Potentials, TRPV Cation Channels, Pharmacology, TRPV, Cell Line, Rats, Sprague-Dawley, Transient receptor potential channel, chemistry.chemical_compound, Dorsal root ganglion, medicine, Animals, Humans, Urea, Receptor, Cells, Cultured, Dose-Response Relationship, Drug, Rats, Posterior Horn Cells, medicine.anatomical_structure, nervous system, chemistry, Competitive antagonist, Capsaicin, Molecular Medicine
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8
المؤلفون: Prisca Honore, Connie R. Faltynek, James P. Sullivan, Jill M. Wetter, Arthur Gomtsyan, Michael F. Jarvis, Carol S. Surowy, Steven M. Hannick, Robert G. Schmidt, Erol K. Bayburt, Chih-Hung Lee, Kennan C. Marsh, Heath A. McDonald
المصدر: Journal of Medicinal Chemistry. 51:392-395
مصطلحات موضوعية: Indazoles, Stereochemistry, Analgesic, TRPV1, Administration, Oral, Biological Availability, Pain, TRPV Cation Channels, In Vitro Techniques, Chemical synthesis, Structure-Activity Relationship, chemistry.chemical_compound, Dogs, Drug Discovery, Animals, Humans, Urea, Structure–activity relationship, Analgesics, musculoskeletal, neural, and ocular physiology, Antagonist, Stereoisomerism, Biological activity, Haplorhini, Rats, Indenes, nervous system, chemistry, Discovery and development of TRPV1 antagonists, Capsaicin, Microsomes, Liver, Molecular Medicine
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9
المؤلفون: Sriajan N. Vaidyanathan, Bruce R. Bianchi, Torben R. Neelands, Robert B. Moreland, Bruce Surber, Carol S. Surowy, Rachid El Kouhen, Michael F. Jarvis, Chih-Hung Lee, Shirish N. Raja, Connie R. Faltynek, Arthur Gomtsyan, Heath A. McDonald, Pamela S. Puttfarcken
المصدر: Journal of Pharmacology and Experimental Therapeutics. 323:285-293
مصطلحات موضوعية: Stereochemistry, TRPV1, TRPV Cation Channels, CHO Cells, Ligands, Transfection, Tritium, Binding, Competitive, Calcium in biology, Radioligand Assay, Cricetulus, Cricetinae, Ganglia, Spinal, Radioligand, Animals, Humans, Urea, Calcium Signaling, Neurons, Afferent, Binding site, Receptor, Pharmacology, Molecular Structure, Chemistry, Chinese hamster ovary cell, Cell Membrane, Antagonist, Stereoisomerism, Isoquinolines, Recombinant Proteins, Rats, Competitive antagonist, Molecular Medicine
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10
المؤلفون: Connie R. Faltynek, Joe Mikusa, Richard J. Perner, Jill M. Wetter, Stanley Didomenico, Tammie K. Jinkerson, Kennan C. Marsh, Chih-Hung Lee, John R. Koenig, Heath A. McDonald, Sean C. Turner, Arthur Gomtsyan, Erol K. Bayburt, Carol S. Surowy, Irene Drizin, Ryan G. Keddy, Prisca Honore
المصدر: Bioorganic & Medicinal Chemistry Letters. 17:3894-3899
مصطلحات موضوعية: Stereochemistry, Clinical Biochemistry, TRPV1, Pain, TRPV Cation Channels, Pharmaceutical Science, Alkylation, Methylation, Models, Biological, Biochemistry, chemistry.chemical_compound, Drug Discovery, Animals, Urea, Potency, Isoquinoline, Molecular Biology, Inflammation, Analgesics, Indazole, Aryl, Organic Chemistry, In vitro, Rats, chemistry, Molecular Medicine, lipids (amino acids, peptides, and proteins), Enantiomer
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11
المؤلفون: Kurill Lukin, Jill M. Wetter, Michael F. Jarvis, Guo Zhu Zheng, Joe Mikusa, Richard J. Perner, Erol K. Bayburt, Ryan G. Keddy, Robert G. Schmidt, Tammie K. Jinkerson, Connie R. Faltynek, Prisca Honore, John R. Koenig, Chih-Hung Lee, Arthur Gomtsyan, Stanley Didomenico, Irene Drizin, Heath A. McDonald, Sean C. Turner, Kennan C. Marsh, Karen St. George, Brian S. Brown
المصدر: Journal of Medicinal Chemistry. 50:3651-3660
مصطلحات موضوعية: Indazoles, Stereochemistry, TRPV1, Administration, Oral, Biological Availability, TRPV Cation Channels, In Vitro Techniques, Chemical synthesis, Structure-Activity Relationship, chemistry.chemical_compound, Dogs, Drug Stability, In vivo, Drug Discovery, Animals, Humans, Urea, Structure–activity relationship, Isoquinoline, Analgesics, Indazole, Phenylurea Compounds, Aryl, Isoquinolines, Rats, chemistry, Microsomes, Liver, Benzyl group, Molecular Medicine
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12
المؤلفون: Steven W. Muchmore, Elizabeth A. Kowaluk, Kennan C. Marsh, Steve McGaraughty, Haixia Yu, Arthur Gomtsyan, Andrew O. Stewart, Shripad S. Bhagwat, Michael F. Jarvis, Karen M. Alexander, Kathy L. Kohlhaas, Clarissa L. Jakob, Chih-Hung Lee, Robin R. Frey, Mark A. Matulenko, Ernest S. Paight, Joseph P. Mikusa, Meiqun Jiang, Stanley Didomenico
المصدر: Bioorganic & Medicinal Chemistry. 15:1586-1605
مصطلحات موضوعية: Protein Conformation, Stereochemistry, Morpholines, Clinical Biochemistry, Pharmaceutical Science, Adenosine kinase, Crystallography, X-Ray, Biochemistry, Rats, Sprague-Dawley, Inhibitory Concentration 50, Mice, Structure-Activity Relationship, chemistry.chemical_compound, Drug Discovery, medicine, Animals, Structure–activity relationship, Binding site, Adenosine Kinase, Molecular Biology, Binding Sites, biology, Chemistry, Aryl, Organic Chemistry, Active site, Ligand (biochemistry), Adenosine, Rats, Pyrimidines, biology.protein, Molecular Medicine, Nucleoside, Protein Binding, medicine.drug
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13
المؤلفون: Torben R. Neelands, C. Zhong, Erol K. Bayburt, B. Brown, Prisca Honore, Joseph P. Mikusa, W. Niforatos, Donna M. Gauvin, Gricelda Hernandez, H. McDonald, Michael W. Decker, Robert B. Moreland, Arthur Gomtsyan, Kennan C. Marsh, B. Bianchi, Prasant Chandran, Connie R. Faltynek, James P. Sullivan, C.-H. Lee, M. Cui
المصدر: The Journal of Neuroscience. 26:9385-9393
مصطلحات موضوعية: Central Nervous System, Male, Indazoles, Pyridines, Analgesic, TRPV1, Administration, Oral, Pain, TRPV Cation Channels, Pharmacology, Cell Line, Rats, Sprague-Dawley, chemistry.chemical_compound, Oral administration, Animals, Humans, Urea, Potency, Sulfones, Receptor, Cells, Cultured, Injections, Spinal, Analgesics, Chemistry, General Neuroscience, Antagonist, Nociceptors, Articles, Arthralgia, Rats, Disease Models, Animal, Treatment Outcome, Nociception, Hyperalgesia, Capsaicin, Calcium, Inflammation Mediators
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14
المؤلفون: Erol K. Bayburt, Prisca Honore, Tammie K. Jinkerson, Chih-Hung Lee, Heath A. McDonald, Sean C. Turner, Brian S. Brown, Irene Drizin, Kennan C. Marsh, James S. Polakowski, Jason A. Segreti, Michael F. Jarvis, John R. Koenig, Stanley Didomenico, Richard J. Perner, Jill M. Wetter, Guo Zhu Zheng, Carol T. Wismer, Ryan G. Keddy, Robert G. Schmidt, Connie R. Faltynek, Arthur Gomtsyan
المصدر: Bioorganic & Medicinal Chemistry. 14:4740-4749
مصطلحات موضوعية: Male, Stereochemistry, Clinical Biochemistry, TRPV Cation Channels, Pharmaceutical Science, In Vitro Techniques, Motor Activity, Biochemistry, Chemical synthesis, Rats, Sprague-Dawley, Mice, Structure-Activity Relationship, chemistry.chemical_compound, Therapeutic index, In vivo, Drug Discovery, Animals, Urea, Structure–activity relationship, Molecular Biology, Pain Measurement, Indazole, Bicyclic molecule, Chemistry, Organic Chemistry, Rats, Kinetics, Molecular Medicine, Linker
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15
المؤلفون: Meiqun Jiang, Stanley Didomenico, Ronald D. Snyder, Karen M. Alexander, Shripad S. Bhagwat, Guo Zhu Zheng, Carol T. Wismer, Haixia Yu, Andrew O. Stewart, Marilyn S. Diehl, Gregory A. Gfesser, Kennan C. Marsh, Erol K. Bayburt, Robin R. Frey, Mark A. Matulenko, Marlon D. Cowart, Jeffery A. McKie, Arthur Gomtsyan, Kathy L. Kohlhaas, Michael F. Jarvis, Elizabeth A. Kowaluk, Joseph P. Mikusa, Steve McGaraughty, Chih-Hung Lee
المصدر: Bioorganic & Medicinal Chemistry. 13:3705-3720
مصطلحات موضوعية: Male, Magnetic Resonance Spectroscopy, Stereochemistry, Morpholines, Clinical Biochemistry, Pharmaceutical Science, Adenosine kinase, Ring (chemistry), Biochemistry, Mass Spectrometry, Cell Line, Ames test, Rats, Sprague-Dawley, Structure-Activity Relationship, In vivo, Drug Discovery, Animals, Structure–activity relationship, Enzyme Inhibitors, Adenosine Kinase, Molecular Biology, chemistry.chemical_classification, biology, Organic Chemistry, Rats, Pyrimidines, Enzyme, chemistry, Enzyme inhibitor, biology.protein, Molecular Medicine, Nucleoside
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16
المؤلفون: Connie R. Faltynek, Chih-Hung Lee, Wende Niforatos, James P. Sullivan, Michael F. Jarvis, Bruce R. Bianchi, Prisca Honore, Arthur Gomtsyan, Rachid El Kouhen, Carol S. Surowy, Heath A. McDonald, Torben R. Neelands
المصدر: Journal of Pharmacology and Experimental Therapeutics. 314:400-409
مصطلحات موضوعية: Male, Hot Temperature, Drug Evaluation, Preclinical, TRPV1, TRPV Cation Channels, Pharmacology, Ion Channels, Vanilloids, Rats, Sprague-Dawley, chemistry.chemical_compound, Transient receptor potential channel, Dorsal root ganglion, Ganglia, Spinal, Calcium flux, medicine, Animals, Humans, Urea, Receptor, Cells, Cultured, Antagonist, Isoquinolines, Recombinant Proteins, Rats, Electrophysiology, medicine.anatomical_structure, nervous system, chemistry, Molecular Medicine, Calcium, lipids (amino acids, peptides, and proteins), Capsazepine, Acids
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17
المؤلفون: Chengmin Zhong, Donna M. Gauvin, Arthur Gomtsyan, Prisca Honore, Connie R. Faltynek, James P. Sullivan, Rachid El Kouhen, Chang Z. Zhu, Joseph P. Mikusa, Michael F. Jarvis, Kennan C. Marsh, Carol T. Wismer, Chih-Hung Lee
المصدر: Journal of Pharmacology and Experimental Therapeutics. 314:410-421
مصطلحات موضوعية: Male, Hot Temperature, Receptors, Drug, Freund's Adjuvant, TRPV1, Pain, Inflammation, Motor Activity, Pharmacology, Carrageenan, Rats, Sprague-Dawley, chemistry.chemical_compound, Formaldehyde, Osteoarthritis, medicine, Animals, Edema, Urea, Receptor, Ligation, Postural Balance, Pain Measurement, Analgesics, Pain, Postoperative, Dose-Response Relationship, Drug, business.industry, Antagonist, Isoquinolines, Sciatic Nerve, Rats, Spinal Nerves, Nociception, chemistry, Hyperalgesia, Capsaicin, Freund's adjuvant, Acute Disease, Chronic Disease, Neuropathic pain, Molecular Medicine, medicine.symptom, business
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18
المؤلفون: Arthur Gomtsyan, Arpad Szallasi
المصدر: Naunyn-Schmiedeberg's archives of pharmacology. 388(4)
مصطلحات موضوعية: Pharmacology, TRPV4, TRPV1, Icilin, Chronic pain, General Medicine, medicine.disease, Transient receptor potential channel, chemistry.chemical_compound, Allodynia, Transient Receptor Potential Channels, chemistry, TRPM8, medicine, Animals, Humans, medicine.symptom, Receptor
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19
المؤلفون: M. Allen McAlexander, Ganesan Baranidharan, Ralf Baron, Arun K. Bhaskar, Mahendra Bishnoi, Jill-Desiree Brederson, Dorothy Cimino Brown, Nigel W. Bunnett, Ingolf Cascorbi, Michael J. Caterina, Ana Charrua, Francisco Cruz, Matthew A.J. Duncton, Madeleine Ennis, Susan Fleetwood-Walker, Ehud Goldin, Arthur Gomtsyan, Huizhen Huang, Gerald Hunsberger, Michael J. Iadarola, Neelima Khairatkar Joshi, Pragyanshu Khare, Kirill Kiselyov, Ari Koivisto, Kanthi K. Kondepudi, Artem Kondratskyi, Ina Kraus-Stojanowic, TinaMarie Lieu, Daoyan Liu, Nancy Luo, Lorcan McGarvey, Rory Mitchell, Magdalene Moran, Christopher Neipp, Bernd Nilius, James C. Parker, Antti Pertovaara, Koenraad Philippaert, Daniel P. Poole, Louis S. Premkumar, Natalia Prevarskaya, Pradeep Rajasekhar, Paul Rosenberg, Sarah E. Ross, Kavisha Singh, Lindsey M. Snyder, Martin Steinhoff, Mathias Sulk, Arpad Szallasi, Jessica Tan, Balázs István Tóth, Mary I. Townsley, Nicholas A. Veldhuis, Kartik Venkatachalam, Rudi Vennekens, Donald G. Welsh, Shiqiang Xiong, Anil Zechariah, Alexander Zholos, Zhiming Zhu
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20
المؤلفون: Arthur Gomtsyan, Jill-Desiree Brederson
مصطلحات موضوعية: business.industry, Analgesic, TRPV1, Sensory system, Pharmacology, Transient receptor potential channel, chemistry.chemical_compound, medicine.anatomical_structure, Nociception, nervous system, Discovery and development of TRPV1 antagonists, chemistry, Capsaicin, medicine, lipids (amino acids, peptides, and proteins), business, Sensitization