Effects of inhibition of fatty acid amide hydrolase vs. the anandamide membrane transporter on TRPV1‐mediated calcium responses in adult DRG neurons; the role of CB1 receptors

The aim of the present study was to investigate the relationship between TRPV1 stimulation and endocannabinoid‐driven CB1 receptor‐mediated inhibition of activity in adult rat dorsal root ganglion (DRG) neurons, a model of primary afferent nociceptors. Calcium‐imaging studies were performed to compare the effects of the fatty acid amide hydrolase (FAAH) inhibitor URB597 (1 µm) vs. the anandamide (AEA) uptake inhibitor UCM707 (1 µm) on capsaicin (100 nm) and N‐arachidonoyl dopamine (NADA; 1 µm)‐evoked changes in intracellular calcium [Ca2+]i in DRG neurons. The ability of the CB1 receptor antagonist AM251 (1 µm) to modulate the effects of URB597 and UCM707 was also determined.

[1]  Christian C. Felder,et al.  Pharmacological Characterization of Endocannabinoid Transport and Fatty Acid Amide Hydrolase Inhibitors , 2006, Cellular and Molecular Neurobiology.

[2]  D. Deutsch,et al.  Anandamide Uptake Is Consistent with Rate-limited Diffusion and Is Regulated by the Degree of Its Hydrolysis by Fatty Acid Amide Hydrolase* , 2006, Journal of Biological Chemistry.

[3]  D. Piomelli,et al.  Actions of the FAAH inhibitor URB597 in neuropathic and inflammatory chronic pain models , 2006, British journal of pharmacology.

[4]  I. Vetter,et al.  The μ opioid agonist morphine modulates potentiation of capsaicin-evoked TRPV1 responses through a cyclic AMP-dependent protein kinase A pathway , 2006, Molecular pain.

[5]  G. Nomikos,et al.  Identification of a high-affinity binding site involved in the transport of endocannabinoids. , 2005, Proceedings of the National Academy of Sciences of the United States of America.

[6]  V. Vellani,et al.  Anandamide acts as an intracellular messenger amplifying Ca2+ influx via TRPV1 channels , 2005, The EMBO journal.

[7]  K. Hargreaves,et al.  A role for the anandamide membrane transporter in TRPV1-mediated neurosecretion from trigeminal sensory neurons , 2005, Neuropharmacology.

[8]  B. Cravatt,et al.  The endogenous cannabinoid system and its role in nociceptive behavior. , 2004, Journal of neurobiology.

[9]  D. R. Sagar,et al.  TRPV1 and CB1 receptor‐mediated effects of the endovanilloid/endocannabinoid N‐arachidonoyl‐dopamine on primary afferent fibre and spinal cord neuronal responses in the rat , 2004, The European journal of neuroscience.

[10]  B. Cravatt,et al.  Comparison of anandamide transport in FAAH wild-type and knockout neurons: evidence for contributions by both FAAH and the CB1 receptor to anandamide uptake. , 2004, Biochemistry.

[11]  C. Fowler,et al.  Reversible, temperature-dependent, and AM404-inhibitable adsorption of anandamide to cell culture wells as a confounding factor in release experiments. , 2004, European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences.

[12]  B. Lutz,et al.  Further evidence for the existence of a specific process for the membrane transport of anandamide. , 2004, The Biochemical journal.

[13]  V. Di Marzo,et al.  Selective inhibition of anandamide cellular uptake versus enzymatic hydrolysis--a difficult issue to handle. , 2004, European journal of pharmacology.

[14]  V. Marzo,et al.  Endovanilloids. Putative endogenous ligands of transient receptor potential vanilloid 1 channels. , 2004 .

[15]  D. Piomelli The molecular logic of endocannabinoid signalling , 2003, Nature Reviews Neuroscience.

[16]  S. Bevan,et al.  Anandamide regulates neuropeptide release from capsaicin‐sensitive primary sensory neurons by activating both the cannabinoid 1 receptor and the vanilloid receptor 1 in vitro , 2003, The European journal of neuroscience.

[17]  J. Ramos,et al.  Design, synthesis and biological evaluation of new endocannabinoid transporter inhibitors. , 2003, European journal of medicinal chemistry.

[18]  L. Petrocellis,et al.  Dual effect of cannabinoid CB1 receptor stimulation on a vanilloid VR1 receptor-mediated response , 2003, Cellular and Molecular Life Sciences CMLS.

[19]  S. Gaetani,et al.  Modulation of anxiety through blockade of anandamide hydrolysis , 2003, Nature Medicine.

[20]  M. Connor,et al.  Anandamide is a partial agonist at native vanilloid receptors in acutely isolated mouse trigeminal sensory neurons , 2002, British journal of pharmacology.

[21]  J. Ramos,et al.  UCM707, a potent and selective inhibitor of endocannabinoid uptake, potentiates hypokinetic and antinociceptive effects of anandamide. , 2002, European journal of pharmacology.

[22]  Pierangelo Geppetti,et al.  An endogenous capsaicin-like substance with high potency at recombinant and native vanilloid VR1 receptors , 2002, Proceedings of the National Academy of Sciences of the United States of America.

[23]  R. Pertwee,et al.  The endogenous cannabinoid anandamide activates vanilloid receptors in the rat hippocampal slice , 2001, Neuropharmacology.

[24]  J. Ramos,et al.  Design, synthesis and biological evaluation of novel arachidonic acid derivatives as highly potent and selective endocannabinoid transporter inhibitors. , 2001, Journal of medicinal chemistry.

[25]  V. Di Marzo,et al.  Palmitoylethanolamide enhances anandamide stimulation of human vanilloid VR1 receptors , 2001, FEBS letters.

[26]  B. Cravatt,et al.  Supersensitivity to anandamide and enhanced endogenous cannabinoid signaling in mice lacking fatty acid amide hydrolase , 2001, Proceedings of the National Academy of Sciences of the United States of America.

[27]  A. Finazzi-Agro’,et al.  The Activity of Anandamide at Vanilloid VR1 Receptors Requires Facilitated Transport across the Cell Membrane and Is Limited by Intracellular Metabolism* , 2001, The Journal of Biological Chemistry.

[28]  V. Chapman,et al.  Cannabinoid inhibition of the capsaicin‐induced calcium response in rat dorsal root ganglion neurones , 2001, British journal of pharmacology.

[29]  L. Petrocellis,et al.  N-acyl-dopamines: novel synthetic CB(1) cannabinoid-receptor ligands and inhibitors of anandamide inactivation with cannabimimetic activity in vitro and in vivo. , 2000, The Biochemical journal.

[30]  D. Kendall,et al.  Inhibition of receptor-mediated calcium responses by corticotrophin-releasing hormone in the CATH.a cell line , 1999, Neuropharmacology.

[31]  S. Hwang,et al.  Capsaicin Binds to the Intracellular Domain of the Capsaicin-Activated Ion Channel , 1999, The Journal of Neuroscience.

[32]  T. Bisogno,et al.  Interactions between synthetic vanilloids and the endogenous cannabinoid system , 1998, FEBS letters.

[33]  Pascual Ferrara,et al.  Structural Features of the Central Cannabinoid CB1 Receptor Involved in the Binding of the Specific CB1 Antagonist SR 141716A (*) , 1996, The Journal of Biological Chemistry.

[34]  A. Yamashita,et al.  2-Arachidonoylglycerol: a possible endogenous cannabinoid receptor ligand in brain. , 1995, Biochemical and biophysical research communications.

[35]  D. Gibson,et al.  Isolation and structure of a brain constituent that binds to the cannabinoid receptor. , 1992, Science.

[36]  R. Lindsay,et al.  Nerve growth factors (NGF, BDNF) enhance axonal regeneration but are not required for survival of adult sensory neurons , 1988, The Journal of neuroscience : the official journal of the Society for Neuroscience.

[37]  C. Gauchy,et al.  Effects of some psychotropic drugs on tyrosine hydroxylase activity in different structures of the rat brain. , 1973, European journal of pharmacology.