Summary
The H 1-receptor agonist 2-thiazolylethylamine (2-TEA) given by i.c.v. route dose-dependently increased wakefulness (W) and decreased NREM sleep (NRMS) and REM sleep (REMS) in rats prepared for chronic sleep recordings. The H 1-receptor antagonists pyrilamine and diphenhydramine given by i.p. route decreased W and increased NREMS. Pyrilamine prevented the increase of W and decrease of NREMS produced by 2-TEA. However, REMS reduction was not antagonized, what tends to suggest that two different mechanisms could be involved in the 2-TEA-induced effects on NREMS and REMS.
Cimetidine which blocks H 2-receptors, when given by i.p. route showed no significant effects on sleep and W. Administration of the H 2-receptor agonist dimaprit and the H 2-receptor antagonists cimetidine, metiamide and ramtidine by i.c.v. route induced the appearance of high voltage spikes at cortical leads, thus leaving inconclusive the matter of their effects on sleep and wakefulness.
Our results tend to support the proposal that the H 1-receptor intervenes in sleep-wakefulness regulation. Limitations in the available H 2-receptor agonists and antagonists presently preclude a more detailed analysis of the role of H 2-receptors on sleep and W.
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References
Arrang, J. M., Garbarg, M., Schwartz, J. C.: Auto-inhibition of brain histamine release mediated by a novel class (H 3) of histamine receptor. Nature.302, 832–837 (1983).
Garbarg, M., Barbin, G., Bischoff, S., Pollard, H., Schwartz, J. C.: Dual localization of histamine in an ascending neuronal pathway and in non-neuronal cells evidenced by lesions in the lateral hypothalamic area. Brain Res106, 333–348 (1976).
Hough, L. B., Green, J. P.: Histamine and its receptors in the Nervous System. In: Handbook of Neurochemistry, Vol. VI, pp. 145–211. New York: Plenum. (1984).
Monnier, M., Sauer, R., Hatt, A. M.: The activating effect of histamine in the central nervous system. Int. Rev. Neurobiol12, 265–305 (1970).
Monti, J. M.: Catecholamines and the sleep-wake cycle. I. EEG and behavioral arousal. Life Sci30, 1145–1157 (1982).
Monti, J. M.: Catecholamines and the sleep-wake cycle. II. REM sleep. Life Sci32, 1401–1415 (1983).
Nistico, G., Rotiroti, D., De Sarro, A., Naccari, F., Stephenson, J. D.: Central effects of histamine and H1 and H2 receptors agonists and antagonists after intraventricular infusion in fowls. Res. Comm. Chem. Path. Pharm27, 431–450 (1980).
Panula, P., Yang, H.-Y. T., Costa, E.: Histamine-containing neurons in the rat hypothalamus. Proc. Natl. Acad. Sci. U.S.A81, 2572–2576 (1984).
Roberts, F., Calcutt, C. R.: Histamine and the hypothalamus. Neurosci9, 721–739 (1983).
Roehrs, T. A., Tietz, E. I., Zorick, F. J., Roth, T.: Daytime sleepiness and antihistamines. Sleep9, 283–285 (1984).
Schwartz, J. C.: Histamine receptors in brain. Life Sci25, 895–912 (1979).
Scbwartz, J. C., Barbin, G., Duchemin, A. M., Garbarg, M., Llorens, C., Pollard, H., Quach, T., Rose, C.: Histamine receptors in the brain and their possible functions. In: Pharmacology of Histamine Receptors, pp. 351–391. Bristol: Wright. (1982).
Uzan, A., Le Fur G., Malgouris, C.: Are antihistamines sedative, via a blockade of brain H1 receptors? J. Pharm. Pharmacol31, 701–702 (1979).
Wauquier, A., Van Den Broeck, W. A. E., Awouters, F., Janssen, P. A. J.: A comparison between astemizole and other antihistamines on sleep-wakefulness cycles in dogs. Neuropharmacology20, 853–859 (1981).
Wauquier, A., Van Den Broeck, W. A. E., Awouters, F., Janssen, P. A. J.: Further studies on the distinctive sleep-wakefulness profiles of antihistamines (astemizole, ketotifen, terfenadine) in dogs. Drug Dev. Res4, 617–625 (1984).
Wilcox, B. J., Seybold, V. S.: Localization of neuronal histamine in rat brain. Neurosci. Lett29, 105–110 (1982).
Wolf, P., Monnier, M.: Electroencephalographic, behavioral and visceral effects of intraventricular infusion of histamine in the rabbit. Agents and Actions3, 196 (1973).
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Monti, J.M., Pellejero, T. & Jantos, H. Effects of H1- and H2-histamine receptor agonists and antagonists on sleep and wakefulness in the rat. J. Neural Transmission 66, 1–11 (1986). https://doi.org/10.1007/BF01262953
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DOI: https://doi.org/10.1007/BF01262953