2010
DOI: 10.1016/j.jsmc.2010.08.003
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Neuropharmacology of Sleep and Wakefulness

Abstract: 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 … Show more

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Cited by 98 publications
(74 citation statements)
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References 180 publications
(188 reference statements)
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“…The sleep-promoting agents are ACh (during REM), GABA, adenosine, melatonin, galanin, and glycine [25]. While many of these neurotransmitters and hormones contribute to sleep promotion, GABA is the primary sleep promoting neurotransmitter upon which most sleep medications act [26]. Barbiturates at low doses promote entry of chloride into GABA-activated channels [27].…”
Section: Neurotransmitters and Hormones In Sleepmentioning
confidence: 99%
See 1 more Smart Citation
“…The sleep-promoting agents are ACh (during REM), GABA, adenosine, melatonin, galanin, and glycine [25]. While many of these neurotransmitters and hormones contribute to sleep promotion, GABA is the primary sleep promoting neurotransmitter upon which most sleep medications act [26]. Barbiturates at low doses promote entry of chloride into GABA-activated channels [27].…”
Section: Neurotransmitters and Hormones In Sleepmentioning
confidence: 99%
“…Benzodiazepines also promote the entry of chloride into GABA-activated channels which subsequently relaxes the post-synaptic neuron [28]. With the exception of exogenous melatonin, a hormone analogue, medications target neurotransmitters, which either counteract a wake-promoting neurotransmitter or activate a sleep-promoting neurotransmitter [26].…”
Section: Neurotransmitters and Hormones In Sleepmentioning
confidence: 99%
“…The high expression of δ subunit-containing GABA A receptors in the thalamus may allow drugs such as gaboxadol to regulate the expression of the thalamocortical oscillations crucial to NREM sleep [108]. It should also be noted that at localized sites in the mesopontine brainstem, higher levels of GABA may actually promote wakefulness at the expense of REM and NREM sleep due to the complex circuits of inhibition and disinhibition involved in switching behavioral states [113].…”
Section: Part 2: Drugs For Diseases Of Sleep-clinical and Molecular Cmentioning
confidence: 99%
“…Drugs used in sleep and wakefulness disorders manipulate complex interplay of neurons and neurotransmitters thus controlling sleep and arousal states at the desired time of the day. 6 Though, sleep medicine has made rapid strides in its field in the past few decades an ideal drug which does not extend its effect the next day and has a no potential for abuse is yet to be found. 6 …”
Section: Introductionmentioning
confidence: 99%
“…6 Though, sleep medicine has made rapid strides in its field in the past few decades an ideal drug which does not extend its effect the next day and has a no potential for abuse is yet to be found. 6 …”
Section: Introductionmentioning
confidence: 99%