Overdose of the histamine H3 inverse agonist pitolisant increases thermal pain thresholds

Inflammation Research

Volumn 61, Issue 11, 2012, Pages 1283-1291

  Zhang, Dong Dong ^a   Sisignano, Marco ^a   Schuh, Claus Dieter ^a   Sander, Kerstin ^b   Stark, Holger ^b   Scholich, Klaus ^a  

^a UNIVERSITY HOSPITAL FRANKFURT   (Germany)

^b GOETHE UNIVERSITY   (Germany)

Author keywords

Ciproxifan; Histamine receptor 3; Pain; Pitolisant; Thermal hyperalgesia

Indexed keywords

CALCIUM; CIPROXIFAN; HISTAMINE H3 RECEPTOR; HISTAMINE H3 RECEPTOR AGONIST; MORPHINE; PITOLISANT; ST 889; UNCLASSIFIED DRUG; VANILLOID RECEPTOR 1; ZYMOSAN;

ANIMAL BEHAVIOR; ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ANTINOCICEPTION; ARTICLE; BODY TEMPERATURE; CALCIUM CELL LEVEL; CELL LEVEL; CONTROLLED STUDY; DOSE RESPONSE; DRUG ANTAGONISM; DRUG MECHANISM; DRUG MEGADOSE; DRUG OVERDOSE; DRUG STRUCTURE; HYPOTHERMIA; INFLAMMATORY PAIN; MECHANICAL STIMULATION; MOUSE; NERVE CELL CULTURE; NERVE INJURY; NEUROIMAGING; NEUROPATHIC PAIN; NONHUMAN; PAIN THRESHOLD; SENSORY NERVE CELL; SPINAL GANGLION; STIMULUS RESPONSE; THERMAL STIMULATION;

ANIMALS; BEHAVIOR, ANIMAL; CALCIUM; CELLS, CULTURED; GANGLIA, SPINAL; HISTAMINE AGONISTS; HISTAMINE H3 ANTAGONISTS; HOT TEMPERATURE; HYPOTHERMIA; IMIDAZOLES; MICE; PAIN; PAIN THRESHOLD; PIPERIDINES; PSYCHOMOTOR PERFORMANCE;

EID: 84868132769     PISSN: 10233830     EISSN: 1420908X     Source Type: Journal    
DOI: 10.1007/s00011-012-0528-5     Document Type: Article

References (46)

1. Lieberman P. Histamine, antihistamines, and the central nervous system. Allergy Asthma Proc. 2009;30:482-6.
2. Jutel M, Akdis M, Akdis CA. Histamine, histamine receptors and their role in immune pathology. Clin Exp Allergy. 2009;39:1786-800.
3. 3) visualized in the brain of human and non-human primates. Brain Res. 1990;526:322-7.
4. Pillot C, Heron A, Cochois V, Tardivel-Lacombe J, Ligneau X, Schwartz JC, et al. A detailed mapping of the histamine H(3) receptor and its gene transcripts in rat brain. Neuroscience. 2002;114:173-93.
5. 3-receptors. Nature. 1987;327:117-23.
6. Arrang JM, Garbarg M, Schwartz JC. Auto-inhibition of brain histamine release mediated by a novel class (H3) of histamine receptor. Nature. 1983;302:832-7.
7. 3 antagonists for treatment of cognitive deficits in CNS diseases. Curr Top Med Chem. 2010;10:153-69.
8. 4 receptors as novel drug targets. Expert Opin Investig Drugs. 2009;18:1519-31.
9. 3 receptor antagonists go to clinics. Biol Pharm Bull. 2008;31:2163-81.
10. Pierre S, Eschenhagen T, Geisslinger G, Scholich K. Capturing adenylyl cyclases as potential drug targets. Nat Rev Drug Discov. 2009;8:321-35.
11. 3 receptors and pain modulation: peripheral, spinal and brain interactions. J Pharmacol Exp Ther. 2011;336:30-7.
12. 3 receptors. J Pain. 2005;6:193-200.
13. Farzin D, Asghari L, Nowrouzi M. Rodent antinociception following acute treatment with different histamine receptor agonists and antagonists. Pharmacol Biochem Behav. 2002;72:751-60.
14. 3 receptor antagonists GSK207040 and GSK334429 improve scopolamine-induced memory impairment and capsaicin-induced secondary allodynia in rats. Biochem Pharmacol. 2007;73:1182-94.
15. 3 receptors inhibits formalin-induced inflammation and nociception, respectively. Pharmacol Biochem Behav. 2007;88:122-9.
16. 3 receptor antagonist in the preclinical models of pain in rats and the involvement of central noradrenergic systems. Brain Res. 2010;1354:74-84.
17. 3 receptor antagonists GSK189254 and GSK334429 are efficacious in surgically-induced and virally-induced rat models of neuropathic pain. Pain. 2008;138:61-9.
18. Huang L, Adachi N, Nagaro T, Liu K, Arai T. Histaminergic involvement in neuropathic pain produced by partial ligation of the sciatic nerve in rats. Reg Anesth Pain Med. 2007;32:124-9.
19. Meier G, Apelt J, Reichert U, Grassmann S, Ligneau X, Elz S, et al. Influence of imidazole replacement in different structural classes of histamine H(3)-receptor antagonists. Eur J Pharm Sci. 2001;13:249-59.
20. 3-receptor antagonist. Arch Pharm (Weinheim). 2000;333:315-6.
21. Linke B, Pierre S, Coste O, Angioni C, Becker W, Maier TJ, et al. Toponomics analysis of drug-induced changes in arachidonic acid-dependent signaling pathways during spinal nociceptive processing. J Proteome Res. 2009;8:4851-9.
22. Decosterd I, Woolf CJ. Spared nerve injury: an animal model of persistent peripheral neuropathic pain. Pain. 2000;87:149-58.
23. Sango K, McDonald MP, Crawley JN, Mack ML, Tifft CJ, Skop E, et al. Mice lacking both subunits of lysosomal beta-hexosaminidase display gangliosidosis and mucopolysaccharidosis. Nat Genet. 1996;14:348-52.
24. Hargreaves K, Dubner R, Brown F, Flores C, Joris J. A new and sensitive method for measuring thermal nociception in cutaneous hyperalgesia. Pain. 1988;32:77-88.
25. 3-receptor inverse agonists studied with BF2.649. Biochem Pharmacol. 2007;73:1215-24.
26. 3-receptor antagonists. Naunyn Schmiedebergs Arch Pharmacol. 1998;358:623-7.
27. 3 receptor: evidence for multiple isoforms. J Neurochem. 2004;90:1331-8.
28. Rossbach K, Nassenstein C, Gschwandtner M, Schnell D, Sander K, Seifert R, et al. Histamine H, H and H receptors are involved in pruritus. Neuroscience. 2011;190:89-102.
29. Bautista DM, Jordt SE, Nikai T, Tsuruda PR, Read AJ, Poblete J, et al. TRPA1 mediates the inflammatory actions of environmental irritants and proalgesic agents. Cell. 2006;124:1269-82.
30. Kwan KY, Allchorne AJ, Vollrath MA, Christensen AP, Zhang DS, Woolf CJ, et al. TRPA1 contributes to cold, mechanical, and chemical nociception but is not essential for hair-cell transduction. Neuron. 2006;50:277-89.
31. Mills C, McMackin M, Jaffe R, Yu J, Zininberg E, Slee D, et al. Effects of the transient receptor potential vanilloid 1 antagonist A-425619 on body temperature and thermoregulation in the rat. Neuroscience. 2008;156:165-74.
32. Moran MM, McAlexander MA, Biro T, Szallasi A. Transient receptor potential channels as therapeutic targets. Nat Rev Drug Discov. 2011;10:601-20.
33. 3 receptors and pain modulation: peripheral, spinal, and brain interactions. J Pharmacol Exp Ther. 2011;336:30-7.
34. Fundin BT, Pfaller K, Rice FL. Different distributions of the sensory and autonomic innervation among the microvasculature of the rat mystacial pad. J Comp Neurol. 1997;389:545-68.
35. Bowsher D, Geoffrey Woods C, Nicholas AK, Carvalho OM, Haggett CE, Tedman B, et al. Absence of pain with hyperhidrosis: a new syndrome where vascular afferents may mediate cutaneous sensation. Pain 2009;147:287-98.
36. Boulant JA. Hypothalamic neurons. Mechanisms of sensitivity to temperature. Ann N Y Acad Sci. 1998;856:108-15.
37. 3 antagonist, ciproxifan, alleviates the memory impairment but enhances the motor effects of MK-801 (dizocilpine) in rats. Neuropharmacology. 2010;59:492-502.
38. Faucard R, Armand V, Heron A, Cochois V, Schwartz JC, Arrang JM. N-methyl-d-aspartate receptor antagonists enhance histamine neuron activity in rodent brain. J Neurochem. 2006;98:1487-96.
39. Bardgett ME, Points M, Roflow J, Blankenship M, Griffith MS. Effects of the H(3) antagonist, thioperamide, on behavioral alterations induced by systemic MK-801 administration in rats. Psychopharmacology (Berl). 2009;205:589-97.
40. 3 receptor-dependent mechanisms regulate ethanol stimulation and conditioned place preference in mice. Psychopharmacology (Berl). 2010;208:75-86.
41. 3 antagonist thioperamide reveals conditioned preference for a context associated with an inactive small dose of cocaine in C57BL/6J mice. Behav Brain Res. 2005;160:161-8.
42. Brosnan-Watters G, Wozniak DF, Nardi A, Olney JW. Acute behavioral effects of MK-801 in the mouse. Pharmacol Biochem Behav. 1996;53:701-11.
43. Wozniak DF, Olney JW, Kettinger L 3rd, Price M, Miller JP. Behavioral effects of MK-801 in the rat. Psychopharmacology (Berl). 1990;101:47-56.
44. Immke DC, Gavva NR. The TRPV1 receptor and nociception. Semin Cell Dev Biol. 2006;17:582-91.
45. Gavva NR, Bannon AW, Surapaneni S, Hovland DN Jr, Lehto SG, Gore A, et al. The vanilloid receptor TRPV1 is tonically activated in vivo and involved in body temperature regulation. J Neurosci. 2007;27:3366-74.
46. Swanson DM, Dubin AE, Shah C, Nasser N, Chang L, Dax SL, et al. Identification and biological evaluation of 4-(3-trifluoromethylpyridin-2-yl) piperazine-1-carboxylic acid (5-trifluoromethylpyridin-2-yl)amide, a high affinity TRPV1 (VR1) vanilloid receptor antagonist. J Med Chem. 2005;48:1857-72.