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C. Fowler, G. Tiger, M. López-Rodríguez, A. Viso, S. Ortega‐Gutiérrez, J. Ramos (2003)
Inhibition of Fatty Acid Amidohydrolase, the Enzyme Responsible for the Metabolism of the Endocannabinoid Anandamide, by Analogues of Arachidonoyl-serotoninJournal of Enzyme Inhibition and Medicinal Chemistry, 18
Ben Paylor, S. Holt, C. Fowler (2006)
The potency of the fatty acid amide hydrolase inhibitor URB597 is dependent upon the assay pH.Pharmacological research, 54 6
Masashi Kohno, H. Hasegawa, A. Inoue, M. Muraoka, T. Miyazaki, Keizo Oka, M. Yasukawa (2006)
Identification of N-arachidonylglycine as the endogenous ligand for orphan G-protein-coupled receptor GPR18.Biochemical and biophysical research communications, 347 3
A. Szallasi, G. Appendino (2004)
Vanilloid receptor TRPV1 antagonists as the next generation of painkillers. Are we putting the cart before the horse?Journal of medicinal chemistry, 47 11
J. Sawynok, X. Liu (2003)
The Formalin Test: Characteristics and Usefulness of the ModelReviews in Analgesia, 7
A. Jayamanne, R. Greenwood, V. Mitchell, S. Aslan, D. Piomelli, C. Vaughan (2006)
Actions of the FAAH inhibitor URB597 in neuropathic and inflammatory chronic pain modelsBritish Journal of Pharmacology, 147
T. Bisogno, D. Melck, L. Petrocellis, M. Bobrov, N. Gretskaya, V. Bezuglov, N. Sitachitta, W. Gerwick, V. Marzo (1998)
Arachidonoylserotonin and other novel inhibitors of fatty acid amide hydrolase.Biochemical and biophysical research communications, 248 3
J. Idänpään-Heikkilä, G. Guilbaud (1999)
Pharmacological studies on a rat model of trigeminal neuropathic pain: baclofen, but not carbamazepine, morphine or tricyclic antidepressants, attenuates the allodynia-like behaviourPAIN, 79
L. Petrocellis, T. Bisogno, John Davis, R. Pertwee, V. Marzo (2000)
Overlap between the ligand recognition properties of the anandamide transporter and the VR1 vanilloid receptor: inhibitors of anandamide uptake with negligible capsaicin‐like activityFEBS Letters, 483
M. Gonzalez, M. Field, J. Hughes, L. Singh (2000)
Evaluation of selective NK(1) receptor antagonist CI-1021 in animal models of inflammatory and neuropathic pain.The Journal of pharmacology and experimental therapeutics, 294 2
Z.-Z. Wu, S.-R. Chen, H. Pan (2006)
Signaling mechanisms of down-regulation of voltage-activated Ca2+ channels by transient receptor potential vanilloid type 1 stimulation with olvanil in primary sensory neuronsNeuroscience, 141
S. Kathuria, S. Gaetani, D. Fegley, F. Valiño, A. Duranti, A. Tontini, M. Mor, G. Tarzia, G. Rana, A. Calignano, A. Giustino, M. Tattoli, M. Palmery, V. Cuomo, D. Piomelli (2003)
Modulation of anxiety through blockade of anandamide hydrolysisNature Medicine, 9
Y. Kanai, E. Nakazato, Akiyoshi Fujiuchi, Tomokazu Hara, A. Imai (2005)
Involvement of an increased spinal TRPV1 sensitization through its up-regulation in mechanical allodynia of CCI ratsNeuropharmacology, 49
K. Sufka, G. Watson, Rebeccah Nothdurft, J. Mogil (1998)
Scoring the mouse formalin test: Validation studyEuropean Journal of Pain, 2
E. Lizanecz, Z. Bagi, E. Pásztor, Z. Papp, I. Edes, N. Kedei, P. Blumberg, A. Tóth (2006)
Phosphorylation-Dependent Desensitization by Anandamide of Vanilloid Receptor-1 (TRPV1) Function in Rat Skeletal Muscle Arterioles and in Chinese Hamster Ovary Cells Expressing TRPV1Molecular Pharmacology, 69
S. Maione, T. Bisogno, V. Novellis, E. Palazzo, L. Cristino, M. Valenti, S. Petrosino, V. Guglielmotti, F. Rossi, V. Marzo (2006)
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 ReceptorsJournal of Pharmacology and Experimental Therapeutics, 316
D. Dubuisson, S. Dennis (1977)
The formalin test: A quantitative study of the analgesic effects of morphine, meperidine, and brain stem stimulation in rats and catsPain, 4
V. Marzo, P. Blumberg, A. Szallasi (2002)
Endovanilloid signaling in painCurrent Opinion in Neurobiology, 12
K. Walker, L. Urbán, S. Medhurst, Sadhana Patel, Mohanjit Panesar, A. Fox, P. McIntyre (2003)
The VR1 Antagonist Capsazepine Reverses Mechanical Hyperalgesia in Models of Inflammatory and Neuropathic PainJournal of Pharmacology and Experimental Therapeutics, 304
M. Caterina, A. Leffler, A. Malmberg, A. Malmberg, W. Martin, W. Martin, J. Trafton, K. Petersen-Zeitz, M. Koltzenburg, A. Basbaum, D. Julius (2000)
Impaired nociception and pain sensation in mice lacking the capsaicin receptor.Science, 288 5464
S. Joshi, G. Hernandez, J. Mikusa, C. Zhu, C. Zhong, A. Salyers, C. Wismer, P. Chandran, M. Decker, P. Honore (2006)
Comparison of antinociceptive actions of standard analgesics in attenuating capsaicin and nerve-injury-induced mechanical hypersensitivityNeuroscience, 143
J. Brooks, G. Pryce, T. Bisogno, S. Jaggar, D. Hankey, Peter Brown, D. Bridges, C. Ledent, M. Bifulco, A. Rice, V. Marzo, D. Baker (2002)
Arvanil-induced inhibition of spasticity and persistent pain: evidence for therapeutic sites of action different from the vanilloid VR1 receptor and cannabinoid CB(1)/CB(2) receptors.European journal of pharmacology, 439 1-3
M. Cui, P. Honore, C. Zhong, D. Gauvin, J. Mikusa, G. Hernandez, P. Chandran, A. Gomtsyan, B. Brown, E. Bayburt, K. Marsh, B. Bianchi, H. McDonald, W. Niforatos, T. Neelands, R. Moreland, M. Decker, C. Lee, J. Sullivan, C. Faltynek (2006)
TRPV1 Receptors in the CNS Play a Key Role in Broad-Spectrum Analgesia of TRPV1 AntagonistsThe Journal of Neuroscience, 26
Giovanni Re, R. Barbero, A. Miolo, V. Marzo (2007)
Palmitoylethanolamide, endocannabinoids and related cannabimimetic compounds in protection against tissue inflammation and pain: potential use in companion animals.Veterinary journal, 173 1
S. McGaraughty, K. Chu, R. Bitner, Brenda Martino, R. Kouhen, P. Han, A. Nikkel, E. Burgard, C. Faltynek, M. Jarvis (2003)
Capsaicin infused into the PAG affects rat tail flick responses to noxious heat and alters neuronal firing in the RVM.Journal of neurophysiology, 90 4
N. Otsuka, Y. Kiuchi, Fumiko Yokogawa, Yutaka Masuda, K. Oguchi, A. Hosoyamada (2001)
Antinociceptive efficacy of antidepressants: assessment of five antidepressants and four monoamine receptors in ratsJournal of Anesthesia, 15
G. Paxinos, Charles Watson (1983)
The Rat Brain in Stereotaxic Coordinates
S. Petrosino, E. Palazzo, V. Novellis, T. Bisogno, F. Rossi, S. Maione, V. Marzo (2007)
Changes in spinal and supraspinal endocannabinoid levels in neuropathic ratsNeuropharmacology, 52
Paxinos (1986)
10.1126/science.283.5400.401
G. Bennett, Y. Xie (1988)
A peripheral mononeuropathy in rat that produces disorders of pain sensation like those seen in manPain, 33
Lie-ju Liu, S. Simon (1996)
Capsaicin-induced currents with distinct desensitization and Ca2+ dependence in rat trigeminal ganglion cells.Journal of neurophysiology, 75 4
L. Iversen, V. Chapman (2002)
Cannabinoids: a real prospect for pain relief?Current opinion in pharmacology, 2 1
R. Lan, Qian Liu, P. Fan, Sonyuan Lin, S. Fernando, D. McCallion, R. Pertwee, A. Makriyannis (1999)
Structure-activity relationships of pyrazole derivatives as cannabinoid receptor antagonists.Journal of medicinal chemistry, 42 4
R. Suplita, Jesse Farthing, T. Gutierrez, A. Hohmann (2005)
Inhibition of fatty-acid amide hydrolase enhances cannabinoid stress-induced analgesia: Sites of action in the dorsolateral periaqueductal gray and rostral ventromedial medullaNeuropharmacology, 49
S. Holt, J. Nilsson, R. Omeir, G. Tiger, C. Fowler (2001)
Effects of pH on the inhibition of fatty acid amidohydrolase by ibuprofenBritish Journal of Pharmacology, 133
A. Lichtman, C. Shelton, Tushar Advani, B. Cravatt (2004)
Mice lacking fatty acid amide hydrolase exhibit a cannabinoid receptor-mediated phenotypic hypoalgesiaPain, 109
Pierre Beaulieu, T. Bisogno, Shahid Punwar, W. Farquhar-Smith, Gerolmina Ambrosino, V. Marzo, Andrew Rice (2000)
Role of the endogenous cannabinoid system in the formalin test of persistent pain in the rat.European journal of pharmacology, 396 2-3
A. Santos, J. Calixto (1997)
Ruthenium red and capsazepine antinociceptive effect in formalin and capsaicin models of pain in miceNeuroscience Letters, 235
Mark Brown, Sonia Flores, R. Dubner, Margaret Hargreaves, P. Joris (1987)
A new and sensitive method for measuring thermal nociception in cutaneous hyperalgesiaPain, 32
C. Gill, A. Randall, S. Bates, K. Hill, D. Owen, P. Larkman, W. Cairns, S. Yusaf, P. Murdock, Paul Strijbos, A. Powell, C. Benham, C. Davies (2004)
Characterization of the human HCN1 channel and its inhibition by capsazepineBritish Journal of Pharmacology, 143
Eva Lago, S. Petrosino, M. Valenti, E. Morera, S. Ortega‐Gutiérrez, J. Fernández-Ruiz, V. Marzo (2005)
Effect of repeated systemic administration of selective inhibitors of endocannabinoid inactivation on rat brain endocannabinoid levels.Biochemical pharmacology, 70 3
H. Bradshaw, J. Walker (2005)
The expanding field of cannabimimetic and related lipid mediatorsBritish Journal of Pharmacology, 144
Mario Stelt, M. Trevisani, V. Vellani, L. Petrocellis, A. Moriello, B. Campi, P. McNaughton, P. Geppetti, V. Marzo (2005)
Anandamide acts as an intracellular messenger amplifying Ca2+ influx via TRPV1 channelsThe EMBO Journal, 24
A. Baamonde, A. Lastra, Lucía Juárez, A. Hidalgo, L. Menéndez (2005)
TRPV1 desensitisation and endogenous vanilloid involvement in the enhanced analgesia induced by capsaicin in inflamed tissuesBrain Research Bulletin, 67
S. Holt, F. Comelli, B. Costa, Christopher Fowler (2005)
Inhibitors of fatty acid amide hydrolase reduce carrageenan‐induced hind paw inflammation in pentobarbital‐treated mice: comparison with indomethacin and possible involvement of cannabinoid receptorsBritish Journal of Pharmacology, 146
L. Petrocellis, T. Bisogno, M. Maccarrone, John Davis, A. Finazzi-Agrò, V. Marzo (2001)
The Activity of Anandamide at Vanilloid VR1 Receptors Requires Facilitated Transport across the Cell Membrane and Is Limited by Intracellular Metabolism*The Journal of Biological Chemistry, 276
R. Almasi, G. Pethö, K. Bölcskei, J. Szolcsányi (2003)
Effect of resiniferatoxin on the noxious heat threshold temperature in the rat: a novel heat allodynia model sensitive to analgesicsBritish Journal of Pharmacology, 139
Y. Kanai, Tomokazu Hara, A. Imai (2006)
Participation of the spinal TRPV1 receptors in formalin‐evoked pain transduction: a study using a selective TRPV1 antagonist, iodo‐resiniferatoxinJournal of Pharmacy and Pharmacology, 58
A. Lichtman, D. Leung, C. Shelton, A. Saghatelian, C. Hardouin, D. Boger, B. Cravatt (2004)
Reversible Inhibitors of Fatty Acid Amide Hydrolase That Promote Analgesia: Evidence for an Unprecedented Combination of Potency and SelectivityJournal of Pharmacology and Experimental Therapeutics, 311
L. Kárai, D. Brown, A. Mannes, S. Connelly, Jacob Brown, M. Gandal, O. Wellisch, J. Neubert, Z. Oláh, M. Iadarola (2004)
Deletion of vanilloid receptor 1-expressing primary afferent neurons for pain control.The Journal of clinical investigation, 113 9
S. Jordt, D. Julius (2002)
Molecular Basis for Species-Specific Sensitivity to “Hot” Chili PeppersCell, 108
Background and purpose: N‐arachidonoyl‐serotonin (AA‐5‐HT) is an inhibitor of fatty acid amide hydrolase (FAAH)‐catalysed hydrolysis of the endocannabinoid/ endovanilloid compound, anandamide (AEA). We investigated if AA‐5‐HT antagonizes the transient receptor potential vanilloid‐1 (TRPV1) channel and, as FAAH and TRPV1 are targets for analgesic compounds, if it exerts analgesia in rodent models of hyperalgesia. Experimental approach: AA‐5‐HT was tested in vitro, on HEK‐293 cells overexpressing the human or the rat recombinant TRPV1 receptor, and in vivo, in rats and mice treated with formalin and in rats with chronic constriction injury of the sciatic nerve. The levels of the endocannabinoids, AEA and 2‐arachidonoylglycerol, in supraspinal (periaqueductal grey, rostral ventromedial medulla), spinal or peripheral (skin) tissues were measured. Key results: AA‐5‐HT behaved as an antagonist at both rat and human TRPV1 receptors (IC50=37‐40 nM against 100 nM capsaicin). It exerted strong analgesic activity in all pain models used here. This activity was partly due to FAAH inhibition, elevation of AEA tissue levels and indirect activation of cannabinoid CB1 receptors, as it was reversed by AM251, a CB1 antagonist. AA‐5‐HT also appeared to act either via activation/desensitization of TRPV1, following elevation of AEA, or as a direct TRPV1 antagonist, as suggested by the fact that its effects were either reversed by capsazepine and 5′‐iodo‐resiniferatoxin, two TRPV1 antagonists, or mimicked by these compounds administered alone. Conclusions and implications: Possibly due to its dual activity as a FAAH inhibitor and TRPV1 antagonist, AA‐5‐HT was highly effective against both acute and chronic peripheral pain. British Journal of Pharmacology (2007) 150, 766–781. doi:10.1038/sj.bjp.0707145
British Journal of Pharmacology – Wiley
Published: Mar 1, 2007
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