sleep disorders

6-Chloromelatonin is a potent melatonin receptor agonist, a 5-methoxyindole compound that competes for presynaptic melatonin receptor sites in the rabbit retina, inhibiting the calcium-dependent release of [3H]dopamine with higher metabolic stability than melatonin. Chloromelatonin competitively binds to [3H]melatonin at MT2 receptors (pKi=9.77) and may be used to study insomnia and sleep disorders associated with depression.

Triflubazam has a wide range of biological activities that can affect sleep and can be used to treat anxiety syndromes and psychological disorders.

Citenamide (AY-15613) has anticancer and anticonvulsant activity and is used in the study of neurological disorders because of its sleep-promoting properties.

Niaprazine is a histamine H1-receptor antagonist exhibiting significant sedative properties.

TTA-A2 is a selective T-type calcium channel antagonist as a potent anticonvulsant that the Cav3.1 isoform plays a prominent role in mediating. TTA-A2 is equally potent against the Cav3.1 (a1G) and Cav3.2 (a1H) channels with IC50 values of 89 nM and 92 nM, respectively, at -80 and -100 mV holding potentials. TTA-A2 can be used for the research of a variety of human neurological diseases, including sleep disorders and epilepsy.

p-MPPI hydrochloride is a selective 5-HT1A receptor antagonist with antidepressant and anxiolytic-like effects.

SUVN-G3031 is a antagonist of histamine H3 receptor with potential for the treatment of cognitive impairment, dementia, attention deficit hyperactivity disorder, epilepsy, sleep disorders, obesity, schizophrenia, eating disorders, and pain.

TIK-301 is a chlorinated melatonin derivative and a potent, high-affinity, and orally active melatonin MT1 and MT2 receptors agonist (Kis: 0.081 nM and 0.042 nM, respectively). TIK-301 is also a 5-HT2B/5-HT2C receptor antagonist with antidepressant action. TIK-301 has the potential for sleep disorders and other circadian rhythm disorders treatment.

Almorexant hydrochloride (ACT 078573 hydrochloride) is an orally active dual orexin receptor antagonist that blocks the intracellular Ca2+ signaling pathway and, to a certain extent, blocks the excitatory effects of methamphetamine. Almorexant hydrochloride Induces apoptosis and can be used to study sleep disorders.

N-Desmethyl Pimavanserin (AC-279) is the active metabolite of Pimavanserin, a 5-HT2A receptor inverse agonist, which is used in the treatment of sleep disorders such as insomnia.

Mioflazine suppresses nucleoside uptake. Mioflazine is an orally active nucleoside transport inhibitor. It has the potential for sleep disorders treatment.

Bafrekalant is a diazabicyclo-substituted imidazo[1,2-a]pyrimidine derivative that can be used to study sleep-related breathing disorders such as obstructive and central sleep apnoea and snoring.