Review of the histamine system and the clinical effects of H1 antagonists: Basis for a new model for understanding the effects of insomnia medications

Lancel, 1999, Role of GABAA receptors in the regulation of sleep: initial sleep responses to peripherally administered modulators and agonists, Sleep, 22, 33, 10.1093/sleep/22.1.33 Lu, 2006, Sleep circuitry and the hypnotic mechanism of GABAA drugs, J Clin Sleep Med, 2, S19 Ebert, 2006, Treating insomnia: current and investigational pharmacological approaches, Pharmacol Ther, 112, 612, 10.1016/j.pharmthera.2005.04.014 Patat, 2001, Pharmacodynamic profile of zaleplon, a new non-benzodiazepine hypnotic agent, Hum Psychopharmacol, 16, 369, 10.1002/hup.310 Walsh, 1995, Hypnotics and caffeine as countermeasures for shiftwork-related sleepiness and sleep disturbance, J Sleep Res, 4, 80, 10.1111/j.1365-2869.1995.tb00233.x Walsh, 1990, Transient insomnia associated with a 3-hour phase advance of sleep time and treatment with zolpidem, J Clin Psychopharmacol, 10, 184, 10.1097/00004714-199006000-00005 Roth, 2008, Daytime pharmacodynamic and pharmacokinetic evaluation of low-dose sublingual transmucosal zolpidem hemitartrate, Hum Psychopharmacol, 23, 13, 10.1002/hup.884 Saper, 2005, Hypothalamic regulation of sleep and circadian rhythms, Nature, 437, 1257, 10.1038/nature04284 Yanai, 1992, Histamine H1 receptors in human brain visualized in vivo by [11C]doxepin and positron emission tomography, Neurosci Lett, 137, 145, 10.1016/0304-3940(92)90390-S Schutte-Rodin, 2008, Clinical guideline for the evaluation and management of chronic insomnia in adults, J Clin Sleep Med, 4, 487, 10.5664/jcsm.27286 Krystal, 2009, A compendium of placebo-controlled trials of medications used for the treatment of insomnia: basis for U.S. clinical practice, Sleep Med Rev, 13, 265, 10.1016/j.smrv.2008.08.001 Monti, 2010, Serotonin 5-HT(2A) receptor antagonists in the treatment of insomnia: present status and future prospects, Drugs Today (Barc), 46, 183, 10.1358/dot.2010.46.3.1437247 Wafford, 2008, Emerging anti-insomnia drugs: tackling sleeplessness and the quality of wake time, Nat Rev Drug Discov, 7, 530, 10.1038/nrd2464 Gyongyosi, 2008, MDMA treatment 6 months earlier attenuates the effects of CP-94,253, a 5-HT1B receptor agonist, on motor control but not sleep inhibition, Brain Res, 22, 34, 10.1016/j.brainres.2008.06.099 Prast, 1993, Modulation by dopamine receptors of the histamine release in the rat hypothalamus, Naunyn Schmiedebergs Arch Pharmacol, 347, 301, 10.1007/BF00167449 Prast, 1994, In vivo modulation of histamine release by autoreceptors and muscarinic acetylcholine receptors in the rat anterior hypothalamus, Naunyn Schmeidebergs Arch Pharmacol, 350, 599, 10.1007/BF00169363 Smith, 2006, Inhibition of [11C]mirtazapine binding by α2-adrenoceptor antagonists studied by positron emission tomography in living porcine brain, Synapse, 59, 463, 10.1002/syn.20262 Gross, 1991, Trimipramine: pharmacological reevaluation and comparison with clozapine, Neuropharmacology, 30, 1159, 10.1016/0028-3908(91)90160-D Hellbom, 2006, Chlorpheniramine, selective serotonin-reuptake inhibitors (SSRIs) and over-the-counter (OTC) treatment, Med Hypotheses, 66, 689, 10.1016/j.mehy.2005.12.006 Trichard, 1998, Binding of antipsychotic drugs to cortical 5-HT2A receptors: a PET study of chlorpromazine, clozapine, and amisulpride in schizophrenic patients, Am J Psychiatry, 155, 505, 10.1176/ajp.155.4.505 Kuoppamaki, 1995, Differential regulation of rat 5-HT2A and 5-HT2C receptors after chronic treatment with clozapine, chlorpromazine and three putative atypical antipsychotic drugs, Neuropsychopharmacology, 13, 139, 10.1016/0893-133X(95)00049-J Orzechowski, 2005, comparative anticholinergic activities of 10 histamine H1 receptor antagonists in two functional models, Eur J Pharmacol, 506, 257, 10.1016/j.ejphar.2004.11.006 Tecott, 1995, Eating disorder and epilepsy in mice lacking 5-HT2C serotonin receptors, Nature, 374, 542, 10.1038/374542a0 Wang, 2006, Deletion of the serotonin 2c receptor from transgenic mice overexpressing leptin does not affect their lipodystrophy but exacerbates their diet-induced obesity, Biochem Biophys Res Commun, 351, 418, 10.1016/j.bbrc.2006.10.033 Haas, 2003, The role of histamine and the tuberomamillary nucleus in the nervous system, Nat Rev Neurosci, 4, 121, 10.1038/nrn1034 Haas, 2008, Histamine in the nervous system, Physiol Rev, 88, 1183, 10.1152/physrev.00043.2007 Michelsen, 2005, Histamine-immunoreactive neurons in the mouse and rat suprachiasmatic nucleus, Eur J Neurosci, 22, 1997, 10.1111/j.1460-9568.2005.04387.x Strakhova, 2009, Localization of histamine H4 receptors in the central nervous system of human and rat, Brain Res, 1250, 41, 10.1016/j.brainres.2008.11.018 Wong, 2003, G protein selectivity is regulated by multiple intracellular regions of GPCRs, Neurosignals, 12, 1, 10.1159/000068914 Kristiansen, 2004, Molecular mechanisms of ligand binding, signaling, and regulation within the superfamily of G-protein-coupled receptors: molecular modeling and mutagenesis approaches to receptor structure and function, Pharmacol Ther, 103, 21, 10.1016/j.pharmthera.2004.05.002 Kanba, 1984, Histamine H1 receptors in human brain labeled with [3H]doxepin, Brain Res, 304, 1, 10.1016/0006-8993(84)90856-4 Bouthenet, 1988, A detailed mapping of histamine H1-receptors in guinea-pig central nervous system established by autoradiography with [125I]iodobolpyramine, Neuroscience, 26, 553, 10.1016/0306-4522(88)90167-4 Barbara, 2002, Histamine H1 receptors in rat dorsal raphe nucleus: pharmacologic characterization and linking to increased neuronal activity, Brain Res, 954, 247, 10.1016/S0006-8993(02)03352-8 Korotkova, 2005, Histamine excites noradrenergic neurons in the locus coeruleus in rats, Neuropharmacology, 49, 129, 10.1016/j.neuropharm.2005.03.001 Cecchi, 2001, Cortical acetylcholine release elicited by stimulation of histamine H1 receptors in the nucleus basalis magnocellularis: a dual-probe microdialysis study in the freely moving rat, Eur J Neurosci, 13, 68, 10.1046/j.1460-9568.2001.01361.x Lin, 1988, Evidence for histaminergic arousal mechanisms in the hypothalamus of cat, Neuropharmacology, 27, 111, 10.1016/0028-3908(88)90159-1 McCormick, 1991, Modulation of neuronal firing mode in cat and guinea pig LGNd by histamine: possible cellular mechanisms of histaminergic control of arousal, J Neurosci, 11, 3188, 10.1523/JNEUROSCI.11-10-03188.1991 Arrang, 1983, Auto-inhibition of brain histamine release mediated by a novel class (H3) of histamine receptor, Nature, 302, 832, 10.1038/302832a0 Monti, 1991, Effects of selective activation or blockade of the histamine H3 receptor on sleep and wakefulness, Eur J Pharmacol, 205, 283, 10.1016/0014-2999(91)90911-9 Passani, 2004, The histamine H3 receptor as a novel therapeutic target for cognitive and sleep disorders, Trends Pharmacol Sci, 25, 618, 10.1016/j.tips.2004.10.003 Eriksson, 2001, Orexin/hypocretin excites the histaminergic neurons of the tuberomammillary nucleus, J Neurosci, 21, 9273, 10.1523/JNEUROSCI.21-23-09273.2001 Okakura, 1992, Glutamatergic regulation of histamine release from rat hypothalamus, Eur J Pharmacol, 213, 189, 10.1016/0014-2999(92)90680-3 Eriksson, 2001, Serotonin excites tuberomammillary neurons by activation of Na(+)/Ca(2+)-exchange, Neuropharmacology, 40, 345, 10.1016/S0028-3908(00)00175-1 Sergeeva, 2007, Dopaminergic excitation of histaminergic tuberomammillary neurons, Acta Physiol, 189, S653 Sherin, 1998, Innervation of histaminergic tuberomammillary neurons by GABAergic and galaninergic neurons in the ventrolateral preoptic nucleus of the rat, J Neurosci, 18, 4705, 10.1523/JNEUROSCI.18-12-04705.1998 Pearlman, 1976, Antihistamines: pharmacology and clinical use, Drugs, 12, 258, 10.2165/00003495-197612040-00002 Schwartz, 2002, Histamine, 179 Lin, 1996, Histaminergic descending inputs to the mesopontine tegmentum and their role in the control of cortical activation and wakefulness in the cat, J Neurosci, 16, 1523, 10.1523/JNEUROSCI.16-04-01523.1996 Huang, 2006, Altered sleep–wake characteristics and lack of arousal response to H3 receptor antagonist in histamine H1 receptor knockout mice, Proc Natl Acad Sci U S A, 103, 4687, 10.1073/pnas.0600451103 Lin, 1994, Hypothalamo-preoptic histaminergic projections in sleep–wake control in the cat, Eur J Neurosci, 6, 618, 10.1111/j.1460-9568.1994.tb00306.x Khateb, 1995, Cholinergic nucleus basalis neurons are excited by histamine in vitro, Neuroscience, 69, 495, 10.1016/0306-4522(95)00264-J Ramesh, 2004, Wakefulness-inducing effects of histamine in the basal forebrain of freely moving rats, Behav Brain Res, 152, 271, 10.1016/j.bbr.2003.10.031 Reiner, 1994, Mechanisms of antihistamine-induced sedation in the human brain: H1 receptor activation reduces a background leakage potassium current, Neuroscience, 59, 579, 10.1016/0306-4522(94)90178-3 Lagos, 2012, Microinjection of the melanin-concentrating hormone into the lateral basal forebrain increases REM sleep and reduces wakefulness in the rat, Life Sci, 90, 895, 10.1016/j.lfs.2012.04.019 Yanovsky, 2012, GABAA receptors involved in sleep and anaesthesia: β1- versus β3-containing assemblies, Pflugers Arch, 463, 187, 10.1007/s00424-011-0988-4 Scammell, 2001, An adenosine A2a agonist increases sleep and induces Fos in ventrolateral preoptic neurons, Neuroscience, 107, 653, 10.1016/S0306-4522(01)00383-9 Strecker, 2000, Adenosinergic modulation of basal forebrain and preoptic/anterior hypothalamic neuronal activity in the control of behavioral state, Behav Brain Res, 115, 183, 10.1016/S0166-4328(00)00258-8 Thakkar, 2008, Adenosine and the homeostatic control of sleep: effects of A1 receptor blockade in the perifornical lateral hypothalamus on sleep-wakefulness, Neuroscience, 153, 875, 10.1016/j.neuroscience.2008.01.017 Tuomisto, 1982, Diurnal variations in brain and pituitary histamine and histamine-n-methyltransferase in the rat and guinea pig, Med Bio, 60, 204 Parmentier, 2002, 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, 7695, 10.1523/JNEUROSCI.22-17-07695.2002 Smriga, 2000, Circadian release of hypothalamic norepinephrine in rats in vivo is depressed during early L-lysine deficiency, J Nutr, 130, 1641 Sun, 2002, Circadian 5-HT production regulated by adrenergic signaling, Proc Natl Acad Sci U S A, 99, 4686, 10.1073/pnas.062585499 Smith, 1992, Quantitative microdialysis of dopamine in the striatum: effect of circadian variation, J Neurosci Methods, 44, 33, 10.1016/0165-0270(92)90111-P Kiyashchenko, 2002, Release of hypocretin (orexin) during waking and sleep states, Neuroscience, 22, 5282, 10.1523/JNEUROSCI.22-13-05282.2002 Lee, 2005, Discharge of identified orexin/hypocretin neurons across the sleep-waking cycle, J Neurosci, 25, 6716, 10.1523/JNEUROSCI.1887-05.2005 Salomon, 2003, Diurnal variation of cerebrospinal fluid hypocretin-1 (Orexin-A) levels in control and depressed subjects, Biol Psychiatry, 54, 96, 10.1016/S0006-3223(02)01740-7 Zeitzer, 2003, circadian and homeostatic regulation of hypocretin in a primate model: implications for the consolidation of wakefulness, J Neurosci, 23, 3555, 10.1523/JNEUROSCI.23-08-03555.2003 Peyron, 2000, A mutation in a case of early onset narcolepsy and a generalized absence of hypocretin peptides in human narcoleptic brains, Nat Med, 6, 991, 10.1038/79690 Baumann, 2005, Hypocretins (orexins) and sleep–wake disorders, Lancet Neurol, 4, 673, 10.1016/S1474-4422(05)70196-4 Chemelli, 1999, Narcolepsy in orexin knockout mice: molecular genetics of sleep regulation, Cell, 98, 437, 10.1016/S0092-8674(00)81973-X Cano, 2008, Neural circuitry of stress-induced insomnia in rats, J Neurosci, 28, 10167, 10.1523/JNEUROSCI.1809-08.2008 McQuade, 1999, Effect of novel environmental stimuli on rat behaviour and central noradrenaline function measured by in vivo microdialysis, Psychopharmacology, 145, 393, 10.1007/s002130051073 Rueter, 1997, A critical review of 5-HT brain microdialysis and behavior, Rev Neurosci, 8, 117, 10.1515/REVNEURO.1997.8.2.117 Bonnavion, 2010, Hypocretins in the control of sleep and wakefulness, Curr Neurol Neurosci Rep, 10, 174, 10.1007/s11910-010-0101-y Glass, 2008, Effects of 2-week treatment with temazepam and diphenhydramine in elderly insomniacs: a randomized, placebo-controlled trial, J Clin Psychopharmacol, 28, 182, 10.1097/JCP.0b013e31816a9e4f Morin, 2005, Valerian-hops combination and diphenhydramine for treating insomnia: a randomized placebo-controlled clinical trial, Sleep, 28, 1465, 10.1093/sleep/28.11.1465 Richardson, 2002, Tolerance to daytime sedative effects of H1 antihistamines, J Clin Psychopharmacol, 22, 511, 10.1097/00004714-200210000-00012 Riemann, 2002, Trimipramine in primary insomnia: results of a polysomnographic double-blind controlled study, Pharmacopsychiatry, 35, 165, 10.1055/s-2002-34119 Hajak, 2001, Doxepin in the treatment of primary insomnia: a placebo-controlled, double-blind, polysomnographic study, J Clin Psychiatry, 62, 453, 10.4088/JCP.v62n0609 Mansbach R. In vitro pharmacological profile of doxepin, a sleep-promoting histamine H1 antagonist. In: Program and abstracts of the ECNP Annual Meeting: Barcelona, Spain; 2008. Stahl, 2008, Selective histamine 1 antagonism: novel hypnotic and pharmacologic actions challenge classical notions of antihistamines, Trends Psychopharmacol, 13, 855 Roth, 2007, Efficacy and safety of doxepin 1 mg, 3 mg, and 6 mg in adults with primary insomnia, Sleep, 30, 1555, 10.1093/sleep/30.11.1555 Scharf, 2008, Efficacy and safety of doxepin 1, 3 and 6 mg in elderly patients with primary insomnia, J Clin Psych, 69, 1557, 10.4088/JCP.v69n1005 Krystal, 2010, Long-term efficacy and safety of doxepin 1 mg and 3 mg in a 12-week sleep laboratory and outpatient trial of elderly subjects with chronic primary insomnia, Sleep, 33, 1553, 10.1093/sleep/33.11.1553 Krystal, 2011, Efficacy and safety of doxepin 3 and 6 mg in a 35-day sleep laboratory trial in adults with chronic primary insomnia, Sleep, 34, 1433 Tyrer, 1990, The benzodiazepine withdrawal symptom questionnaire, J Affective Disord, 19, 53, 10.1016/0165-0327(90)90009-W Geister, 2001, Bioavailability investigation of two different oral formulations of doxepin, Arzneimittelforschung, 51, 189 Virtanen, 1980, Single dose pharmacokinetics of doxepin in healthy volunteers, Acta Pharmacol Toxicol (Copenh), 47, 371, 10.1111/j.1600-0773.1980.tb01575.x Walsh, 2008, Efficacy and safety of zolpidem extended release in elderly primary insomnia patients, Am J Geriatr Psychiatry, 16, 44, 10.1097/JGP.0b013e3181256b01 McCall, 2006, A polysomnography study of eszopiclone in elderly patients with insomnia, Curr Med Res Opin, 22, 1633, 10.1185/030079906X112741 Richelson, 2001, Pharmacology of antidepressants, Mayo Clin Proc, 76, 511, 10.4065/76.5.511 Petroutka, 1982, Antiemetics: neurotransmitter receptor binding predicts therapeutic actions, Lancet, 658, 10.1016/S0140-6736(82)92206-1 Kubo, 1987, Antimuscarinic effects of antihistamines: quantitative evaluation by receptor-binding assay, Jpn J Pharmacol, 43, 277, 10.1254/jjp.43.277 Criado, 2010, Histamine, histamine receptors, and antihistamines: new concepts, An Bras Dermatol, 85, 195, 10.1590/S0365-05962010000200010