Sleep is characterized by altered consciousness, it is split into two distinct stages- rapid eye movement (REM) and non-REM. The circadian clock controls the pattern of sleep and wakefulness. It is regulated by the light levels, temperature, metabolites, neurotransmitters, neuropeptides, and neurohormones, which cause a daily fluctuation in expression levels of many sleep-related genes.
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GR3027 (Golexanolone) is a GABA-A receptor modulating steroid antagonist that selectively antagonizes the enhanced activation of GABAA receptors by neurosteroids such as allopregnanolone and THDOC; inhibits α1β2γ2L receptor 29 ± 5% of THDOC enhancement of the GABA response, does not antagonize the effect of GABA at the GABAA receptor; during the specific conditions used for the different receptors, IC50=250 nM for the α1β2γ2L GABAA receptor and 350 nM for the α5β3γ2L GABAA receptor; restores spatial learning and motor coordination in rats with chronic hyperammonemia and hepatic encephalopathy.
EMD-281014 hydrochloride ((Pruvanserin, LSN2411347, LY-2422347)) is a potent, highly selective 5-HT2A antagonist with Ki of 0.87 nM, displays little to no affinity for 5-HT2C receptors (Ki=557 nM), human D2 receptors and IKr channels; significantly increases swimming and decreases immobility in male congenital learned helpless rats in the forced swim test; reduces dyskinesia and psychosis in the l-DOPA-treated parkinsonian marmoset.
EMD-281014 ((Pruvanserin, LSN2411347, LY-2422347)) is a potent, highly selective 5-HT2A antagonist with Ki of 0.87 nM, displays little to no affinity for 5-HT2C receptors (Ki=557 nM), human D2 receptors and IKr channels; significantly increases swimming and decreases immobility in male congenital learned helpless rats in the forced swim test; reduces dyskinesia and psychosis in the l-DOPA-treated parkinsonian marmoset.
A potent, selective, orally bioavailable Orexin 2 receptor (OX2R) antagonist with Ki/IC50 of 0.5/18 nM; displays >100-fold selectivity over OX1R; promotes sleep and increases both rapid eye movement (REM) and non-REM (NREM) sleep in rats and dogs without inducing cataplexy; also decreases ACTH levels in rats.
Solriamfetol hydrochloride (JZP-110, R-228060, ADX-N05, YKP-10A) is a norepinephrine-dopamine reuptake inhibitor that inhibits dopamine and norepinephrine transporter with IC50 of 2.9 and 4.4 uM, respectively; a wake-promoting agent with dopaminergic and noradrenergic activity.
A partial positive allosteric GABAA receptor modulator; displays activity at the alpha1-subunit, associated with promoting sleep.
Indiplon is a potent GABAA receptor positive allosteric modulator that acts at the benzodiazepine site (Ki values are 1.2 and 1.7 nM in rat frontal cortex and cerebellum respectively); potentiates the GABA-activated chloride current in recombinant GABA(A) receptors in a dose-dependent and reversible manner in 293 cells, 10-fold selective for α1 subunit-containing receptors over GABA(A) receptors containing α2, α3, or α5 subunits.
Almorexant hydrochloride is a dual Orexin receptor OX1/OX2 antagonist with Ki of 1.3/0.17 nM for hOX1/hOX2 respectively; selectively inhibits the functional consequences of OX1 and OX2 receptor activation, such as intracellular Ca2+ mobilization.
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