Effects of a-fluoromethylhistidine on sleep and wakefulness in the rat

Monti, Jaime M.; D'Angelo, Luisa; Jantos, Héctor; Pazos, Sheila

doi:10.1007/bf01250237

“…Similarly, inhibition of histamine synthesis with injection of -fluoromethylhistidine decreased wakefulness and increased NREM and REM sleep in rats [27]. These results again indicate an important role for histamine in the maintenance of the waking state.…”

Section: Effects Of Histamine On Sleep/wake Cyclesmentioning

confidence: 58%

The Prevalence, Morbidities, and Treatments of Insomnia

Zammit

¹

2007

CNSNDDT

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Insomnia is a common condition that often is co-morbid with other illnesses. It is associated with significant morbidities, including nighttime distress, impaired cognitive functioning, impaired daytime functioning, and increased risk of accidents. People with insomnia utilize healthcare services more often than those without insomnia, and they are at greater risk for the development of certain health problems; most notably psychiatric illness such as depression. It is now known that the significant impact of insomnia warrants diagnosis and treatment. Behavioral and psychopharmacological treatments have been available for some time. However, formerly common classes of therapeutics such as the barbiturates and benzodiazepines have been replaced by new allosteric modulators of the GABA(A) receptor and other therapeutics with novel mechanisms of action. This article presents existing approaches to insomnia treatment, and reviews new treatments, therapeutic targets, and treatment approaches to insomnia under development that may offer promise to practitioners and patients.

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“…Systemic administration of the H 1 receptor antagonists mepyramine98 and cyproheptadine99 caused a significant increase in NREM sleep in cat and rat, respectively. Decreasing brain histamine levels by inhibiting synthesis significantly decreases wakefulness and increases NREM sleep in rat100, 101 and cat 98. These data suggest that histaminergic signaling via the H 1 receptor promotes wakefulness.…”

Section: Biogenic Aminesmentioning

confidence: 72%

Neuropharmacology of Sleep and Wakefulness

Watson

¹

,

Baghdoyan

²

,

Lydic

³

2010

Sleep Medicine Clinics

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Synopsis The development of sedative/hypnotic molecules has been empiric rather than rational. The empiric approach has produced clinically useful drugs but for no drug is the mechanism of action completely understood. All available sedative/hypnotic medications have unwanted side effects and none of these medications creates a sleep architecture that is identical to the architecture of naturally occurring sleep. This chapter reviews recent advances in research aiming to elucidate the neurochemical mechanisms regulating sleep and wakefulness. One promise of rational drug design is that understanding the mechanisms of sedative/hypnotic action will significantly enhance drug safety and efficacy.

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“…105 Systemic administration of the H 1 receptor antagonists mepyramine 106 and cyproheptadine 107 caused a significant increase in NREM sleep in cat and rat, respectively. Decreasing brain histamine levels by inhibiting synthesis significantly decreases wakefulness and increases NREM sleep in rat 108, 109 and cat. 106 These data suggest that histaminergic signaling via the H 1 receptor promotes wakefulness.…”

Section: Biogenic Aminesmentioning

confidence: 94%

Neuropharmacology of Sleep and Wakefulness

Watson

¹

,

Baghdoyan

²

,

Lydic

³

2012

Sleep Medicine Clinics

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Synopsis The development of sedative/hypnotic molecules has been empiric rather than rational. The empiric approach has produced clinically useful drugs but for no drug is the mechanism of action completely understood. All available sedative/hypnotic medications have unwanted side effects and none of these medications creates a sleep architecture that is identical to the architecture of naturally occurring sleep. This chapter reviews recent advances in research aiming to elucidate the neurochemical mechanisms regulating sleep and wakefulness. One promise of rational drug design is that understanding the mechanisms of sedative/hypnotic action will significantly enhance drug safety and efficacy.

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Effects of a-fluoromethylhistidine on sleep and wakefulness in the rat

Cited by 40 publications

References 7 publications

The Prevalence, Morbidities, and Treatments of Insomnia

The Prevalence, Morbidities, and Treatments of Insomnia

Neuropharmacology of Sleep and Wakefulness

Neuropharmacology of Sleep and Wakefulness

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