The brain H3-receptor as a novel therapeutic target for vigilance and sleep-wake disorders

Biochemical Pharmacology

Volumn 73, Issue 8, 2007, Pages 1157-1171

  Parmentier, R ^a,b,c   Anaclet, C ^a,b   Guhennec, C ^c   Brousseau, E ^c   Bricout, D ^c   Giboulot, T ^c   Bozyczko Coyne, D ^d   Spiegel, K ^a   Ohtsu, H ^e   Williams, M ^d   Lin, J S ^a,b  

^a INSERM   (France)

^b UNIVERSITÉ LYON 1   (France)

^c Worldwide Discovery Research   (France)

^d CEPHALON INC   (United States)

^e TOHOKU UNIVERSITY SCHOOL OF MEDICINE   (Japan)

Author keywords

Arousal; Cortical EEG; H3 receptor; Histamine; Knockout mice; Modafinil; Narcolepsy; Psychostimulant; Sleep wake cycle; Sleep wake disorders; Somnolence; Vigilance

Indexed keywords

AMPHETAMINE; AUTORECEPTOR; CAFFEINE; CIPROXIFAN; HISTAMINE H3 RECEPTOR; HISTAMINE H3 RECEPTOR ANTAGONIST; HISTIDINE DECARBOXYLASE; THIOPERAMIDE; ANTIHISTAMINIC AGENT; BENZHYDRYL DERIVATIVE; HISTAMINE; HISTAMINE AGONIST; MODAFINIL;

ALERTNESS; ANIMAL EXPERIMENT; AROUSAL; ARTICLE; BRAIN; CONTROLLED STUDY; DRUG EFFECT; ELECTROCORTICOGRAPHY; MOUSE; NARCOLEPSY; NONHUMAN; PRIORITY JOURNAL; SLEEP WAKING CYCLE; SOMNOLENCE; ANIMAL; ANIMAL MODEL; ELECTROENCEPHALOGRAPHY; METABOLISM; MOUSE MUTANT; PHYSIOLOGY; SLEEP; SLEEP DISORDER; WAKEFULNESS;

ANIMALS; BENZHYDRYL COMPOUNDS; BRAIN; ELECTROENCEPHALOGRAPHY; HISTAMINE; HISTAMINE AGONISTS; HISTAMINE ANTAGONISTS; MICE; MICE, KNOCKOUT; MODELS, ANIMAL; RECEPTORS, HISTAMINE H3; SLEEP; SLEEP DISORDERS; WAKEFULNESS;

EID: 33947161911     PISSN: 00062952     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bcp.2007.01.002     Document Type: Article

References (64)

1. Schwartz J.C., Pollard H., and Quach T.T. Histamine as a neurotransmitter in mammalian brain: neurochemical evidence. J Neurochem 35 (1980) 26-33
2. Haas H.L., and Panula P. The role of histamine and the tuberomammillary nucleus in the nervous system. Nat Rev Neurosci 4 (2003) 121-130
3. Brown R.E., Stevens D.R., and Haas H.L. The physiology of brain histamine. Prog Neurobiol 63 (2001) 637-672
4. Lin J.S. Brain structures and mechanisms involved in the control of cortical activation and wakefulness, with emphasis on the posterior hypothalamus and histaminergic neurons. Sleep Med Rev 4 (2000) 471-503
5. Moruzzi G. The sleep-waking cycle. Ergeb Physiol 64 (1972) 1-165
6. Sakai K., El Mansari M., Lin J.S., Zhang J.G., and Vanni-Mercier G. The posterior hypothalamus in the regulation of wakefulness and paradoxical sleep. In: Mancia M., and Marini G. (Eds). The diencephalon and sleep (1990), Raven Press, New York 171-198
7. Steriade M. Alertness, quiet sleep, dreaming. In: Peters A. (Ed). Cerebral cortex vol. 9 (1991), Plenum Publisher, New York 279-357
8. McCormick D.A. Neurotransmitter actions in the thalamus and cerebral cortex and their role in neuromodulation of thalamocortical activity. Prog Neurobiol 39 (1992) 337-388
9. Jones B.E. Arousal systems. Front Biosci 1 8 (2003) s438-s451
10. Panula P., Yang H.Y., and Costa E. Histamine-containing neurons in the rat hypothalamus. Proc Natl Acad Sci USA 81 (1984) 2572-2576
11. Watanabe T., Taguchi Y., Shiosaka S., Tanaka J., Kubota H., Terano Y., et al. Distribution of the histaminergic neuron system in the central nervous system of rats; a fluorescent immunohistochemical analysis with histidine decarboxylase as a marker. Brain Res 295 (1984) 13-25
12. Lin J.S., Luppi P.H., Salvert D., Sakai K., and Jouvet M. Histamine-immunoreactive neurons in the hypothalamus of cats. C R Acad Sci III 303 (1986) 371-376
13. Lin J.S., Hou Y., Sakai K., and Jouvet M. Histaminergic descending inputs to the mesopontine tegmentum and their role in the control of cortical activation and wakefulness in the cat. J Neurosci 16 (1996) 1523-1537
14. Takahashi K., Lin J.S., and Sakai K. Neuronal activity of histaminergic tuberomammillary neurons during wake-sleep states in the mouse. J Neurosci 26 40 (2006) 10292-10298
15. Vanni-Mercier G., Gigout S., Debilly G., and Lin J.S. Waking selective neurons in the posterior hypothalamus and their response to histamine H3-receptor ligands: an electrophysiological study in freely moving cats. Behav Brain Res 144 (2003) 227-241
16. Parmentier R., Ohtsu H., Djebbara-Hannas Z., Valatx J.L., Watanabe T., and Lin J.S. Anatomical, physiological, and pharmacological characteristics of histidine decarboxylase knock-out mice: evidence for the role of brain histamine in behavioral and sleep-wake control. J Neurosci 22 (2002) 7695-7711
17. Crochet S., and Sakai K. Effects of microdialysis application of monoamines on the EEG and behavioural states in the cat mesopontine tegmentum. Eur J Neurosci 11 (1999) 3738-3752
18. Arrang J.M., Garbarg M., and Schwartz J.C. Auto-inhibition of brain histamine release mediated by a novel class (H3) of histamine receptor. Nature 302 (1983) 832-837
19. Arrang J.M., Garbarg M., and Schwartz J.C. Autoinhibition of histamine synthesis mediated by presynaptic H3-receptors. Neuroscience 23 (1987) 149-157
20. Lin J.S., Sakai K., Vanni-Mercier G., Arrang J.M., and Garbarg M. Schwartz JC, and Jouvet M, Involvement of histaminergic neurons in arousal mechanisms demonstrated with H3-receptor ligands in the cat. Brain Res 523 (1990) 325-330
21. 3-receptor on sleep and wakefulness. Eur J Pharmacol 205 (1991) 283-287
22. McLeod R.L., Aslanian R., del P.M., Duffy R., Egan R.W., Kreutner W., et al. SCH 50971, an orally active histamine H3 receptor agonist, inhibits central neurogenic vascular inflammation and produces sedation in the guinea pig. J Pharmacol Exp Ther 287 (1998) 43-50
23. Lamberty Y., Margineanu D.G., Dassesse D., and Klitgaard H. H3 agonist immepip markedly reduces cortical histamine release, but only weakly promotes sleep in the rat. Pharmacol Res 48 (2003) 193-198
24. 3 antagonists/inverse agonists. Biochem Pharmacol 71 (2006) 1103-1113
25. Bastuji H., and Jouvet M. Successful treatment of idiopathic hypersomnia and narcolepsy with modafinil. Prog Neuropsychopharmacol Biol Psychiatry 12 (1988) 695-700
26. US Modafinil in Narcolepsy Multicenter Study Group. Randomized trial of modafinil for the treatment of pathological somnolence in narcolepsy. Ann Neurol 43 (1998) 88-97
27. US., Modafinil in Narcolepsy Multicenter Study Group. Randomized trial of modafinil for the treatment for the excessive daytime somnolence of narcolepsy. Neurology 54 (2000) 1166-1175
28. Cziesler C.A., et al. Modafinil for excessive sleepiness associated with shift-work sleep disorder. N Eng J Med 353 (2005) 476-486
29. Schwartz J.C., Arrang J.M., Garbarg M., Pollard H., and Ruat M. Histaminergic transmission in the mammalian brain. Physiol Rev 71 (1991) 1-51
30. Ligneau X., Lin J., Vanni-Mercier G., Jouvet M., Muir J.L., Ganellin C.R., et al. Neurochemical and behavioral effects of ciproxifan, a potent histamine H3-receptor antagonist. J Pharmacol Exp Ther 287 (1998) 658-666
31. Mignot E., Nishino S., Gulleminault C., and Dement W.C. Modafinil binds to the dopamine uptake carrier site with lower affinity. Sleep 17 (1994) 436-437
32. Wisor J.P., Nishino S., Sora I., Uhl G.H., Mignot E., and Edgar D.M. Dopaminergic role in stimulant-induced wakefulness. J Neurosci 21 (2001) 1787-1794
33. Madras B.K., Xie Z., Lin Z., Jassen A., Panas H., Lynch L., et al. Modafinil occupies dopamine and norepinephrine transporters in vivo and modulates the transporters and trace amine activity in vitro. J Pharmacol Exp Ther 319 (2006) 561-569
34. 3 receptor drugs. Nat Rev Drug Discov 4 (2005) 107-120
35. Lin J.S., Roussel B., Akaoka H., Fort P., Debilly G., and Jouvet M. Role of catecholamines in the modafinil and amphetamine induced wakefulness, a comparative pharmacological study in the cat. Brain Res 591 (1992) 319-326
36. Lin J.S., Gervasoni D., Hou Y., Vanni-Mercier G., Rambert F., Frydman A., et al. Effects of amphetamine and modafinil on the sleep/wake cycle during experimental hypersomnia induced by sleep deprivation in the cat. J Sleep Res 9 (2000) 89-96
37. Touret M., Sallanon-Moulin M., and Jouvet M. Awakening properties of modafinil without paradoxical sleep rebound: comparative study with amphetamine in the rat. Neurosci Lett 189 (1995) 43-46
38. Edgar D.M., and Seidel W.F. Modafinil induces wakefulness without intensifying motor activity or subsequent rebound hypersomnolence in the rat. J Pharmacol Exp Ther 283 (1997) 757-769
39. Cirelli C. How sleep deprivation affects gene expression in the brain: a review of recent findings. J Appl Physiol 92 (2002) 394-400
40. Cirelli C., Faraguna U., and Tononi G. Changes in brain gene expression after long-term sleep deprivation. J Neurochem 98 (2006) 1632-1645
41. Scammell T.E., Estabrooke I.V., McCarthy M.T., Chemelli R.M., Yanagisawa M., Miller M.S., et al. Hypothalamic arousal regions are activated during modafinil-induced wakefulness. J Neurosci 20 (2000) 8620-8628
42. Ishizuka T., Sakamoto Y., Sakurai T., and Yamatodani A. Modafinil increases histamine release in the anterior hypothalamus of rats. Neurosci Lett 339 (2003) 143-146
43. Pompeiano M., Cirelli C., and Tononi G. Immediate-early genes in spontaneous wakefulness and sleep: expression of c-fos and NGFI-A mRNA and protein. J Sleep Res 3 (1994) 80-96
44. Pompeiano M., Cirelli C., Arrighi P., and Tononi G. c-Fos expression during wakefulness and sleep. Neurophysiol Clin 25 (1995) 329-341
45. Sastre J.P., Buda C., Lin J.S., and Jouvet M. Differential c-fos expression in the rhinencephalon and striatum after enhanced sleep-wake states in the cat. Eur J Neurosci 12 (2000) 1397-1410
46. Tanganelli S., Perez dlM, Ferraro L., Mendez-Franco J., Beani L., Rambert F.A., et al. Modafinil and cortical gamma-aminobutyric acid outflow. Modulation by 5-hydroxytryptamine neurotoxins. Eur J Pharmacol 273 (1995) 63-71
47. Ferraro L., Tanganelli S., O'Connor W.T., Antonelli T., Rambert F., and Fuxe K. The vigilance promoting drug modafinil decreases GABA release in the medial preoptic area and in the posterior hypothalamus of the awake rat: possible involvement of the serotonergic 5-HT3 receptor. Neurosci Lett 220 (1996) 5-8
48. Lin J.S., Parmentier R., Valatx J.L., and Watanabe T. Cortical EEG and sleep-wake cycle in histamine H1-receptor knockout mice. 32nd Annual Meeting. Soc Neurosci Abstr (2002)
49. 3 receptor, a putative genetic animal model for REM sleep behavior disorder. Sleep 25 Suppl. A114 (2002)
50. Toyota H., Dugovic C., Koehl M., Laposky A.D., Weber C., Ngo K., et al. Behavioral characterization of mice lacking histamine H(3) receptors. Mol Pharmacol 62 (2002) 389-397
51. Ohtsu H., Tanaka S., Terui T., Hori Y., Makabe-Kobayashi Y., Pejler G., et al. Mice lacking histidine decarboxylase exhibit abnormal mast cells. FEBS Lett 502 (2001) 53-56
52. Chu M., Huang Z.L., Qu W.M., Eguchi N., Yao M.H., and Urade Y. Extracellular histamine level in the frontal cortex is positively correlated with the amount of wakefulness in rats. Neurosci Res 49 (2004) 417-420
53. Lin J.S., Hou Y., and Jouvet M. Potential brain neuronal targets for amphetamine-, methylphenidate-, and modafinil-induced wakefulness, evidenced by c-fos immunocytochemistry in the cat. Proc Natl Acad Sci USA 93 (1996) 14128-14133
54. 1 receptors. Proc Natl Acad Sci USA 93 (1996) 13316-13320
55. 2 receptor-deficient mice. J Clin Invest 105 (2000) 1741-1749
56. 3 receptors results in changes in brain histamine tone leading to an obese phenotype. J Clin Invest 110 (2002) 1791-1799
57. 3 receptor antagonists A-304121 and A-317920. I. In vitro pharmacological effects. J Pharmacol Exp Ther 305 (2003) 887-896
58. 4 receptors: structure-activity relationships of histamine derivatives. Br J Pharmacol 147 (2006) 744-754
59. Nishino S., Fujiki N., Ripley B., Sakurai E., Kato M., Watanabe T., et al. Decreased brain histamine content in hypocretin/orexin receptor-2 mutated narcoleptic dogs. Neurosci Lett 313 (2001) 125-128
60. Mignot E., and Nishino S. Emerging therapies in narcolepsy-cataplexy. Sleep 28 (2005) 754-763
61. 3 receptor ligands and neurological disease. Expert Opin Invest Drugs 13 (2004) 1237-1248
62. 3 receptor as a novel therapeutic target for cognitive and sleep disorders. Trends Pharmacol Sci 25 (2004) 618-625
63. 3 receptor: preclinical pharmacology. J Pharmacol Exp Ther. 320 (2007) 365-375
64. 3 receptor antagonists: from target identification to drug leads. Biochem Pharmacol, this issue.