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Cat. No. Product Name CAS No. Information
PC-60727

ACT-541468

1505484-82-1

A potent, selective, dual orexin receptor 1 and 2 (OX1 and OX2) antagonist with Kb of 0.52 and 0.78 nM, respectively; displays high selectivity over a panel of 130 central and peripheral pharmacological targets; shows potential for treatment of insomnia disorder.

Sleep Disorder

Phase 2 Clinical

PC-60053

Solriamfetol hydrochloride

178429-62-4

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.

Sleep Disorder

Phase 3 Clinical

PC-35454

GR3027

2089238-18-4 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.

Sleep Disorder

Phase 2 Clinical

PC-35384

EMD-281014 hydrochloride

443144-27-2 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.

Sleep Disorder

Discontinued

PC-35383

EMD-281014

443144-26-1 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.

Sleep Disorder

Discontinued

PC-42964

MK-3697

1224846-01-8 MK-3697 is a potent, selective, orally bioavailable Orexin 2 receptor (OX2R) antagonist with Ki of 1.1 nM and IC50 of 16 nM, shows exquisite selectivity over OX1R (Ki=18 uM); MK-3697 is orally efficacious in sleep experiments across species with high OX2R occupancy and low OX1R blockade, demonstrated excellent sleep efficacy across species, and shows potential for the treatment of insomnia.

Sleep Disorder

Phase 2 Discontinued

PC-63035

MK-0249

1167574-41-5 MK-0249 is a novel potent, selective histamine H3 inverse agonist for the treatment of cognitive impairment with schizophrenia.

Sleep Disorder

Phase 1 Discontinued

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