wakefulness

Bavisant (JNJ-31001074) is a selective and orally active Human H3 receptor antagonist. Bavisant can be used in research on mechanisms of action, involving wakefulness and cognition and the treatment for ADHD.

9-FLUORENOL is a dopamine reuptake inhibitor with IC50 of 9 µM, and a major metabolite of a compound developed as a wakefulness-promoting agent.

Bavisant (JNJ-310010740) dihydrochloride is a highly selective, orally active antagonist of the human H3 receptor with a novel mechanism of action, involving wakefulness and cognition.

Bavisant dihydrochloride hydrate (JNJ31001074AAC) is a highly selective, orally active antagonist of the human H3 receptor with a novel mechanism of action related to wakefulness and cognition, and it has potential as a treatment for ADHD. In a clinical trial, the mean change from baseline in the total ADHD-RS-IV score at day 42 was -8.8 in the placebo group versus -9.3, -11.2, and -12.2 in the bavisant 1 mg/day, 3 mg/day, and 10 mg/day groups, respectively; however, the change in the 10 mg/day group was not statistically superior to placebo (p=0.161). Statistical comparisons of the 1 mg/day and 3 mg/day groups with placebo based on a step-down closed testing procedure were not performed. Bavisant has completed a phase II ADHD trial, but no results have been reported [1]. Clinical trial: A Study to Characterize the Pharmacokinetics and Effect of Food on JNJ-31001074 in Healthy Volunteers. Phase 2. IC50 Value: Target: H3 receptor in vitro.

Orexin 2 Receptor Agonist 3 is an orally active and brain-penetrant agonist of the orexin receptor 2 (OX2) with an EC50 value of 2.5 nM. This compound increases wakefulness in both orexin/ataxin-3 NT1 mouse models and healthy Beagle dogs. It is applicable for research related to narcolepsy.

R06039-696 is a neuropeptide S receptor (NPSR) agonist with an EC50 of 91 nM. It plays a role in regulating various biological functions such as wakefulness, stress and anxiety responses, memory processes, and food intake by activating the neuropeptide S receptor.

R06039-691 is a neuropeptide S receptor (NPSR) agonist with an EC50 of 93 nM. It participates in the regulation of various biological functions, such as wakefulness, stress and anxiety responses, memory processes, and food intake, through the activation of neuropeptide S receptors.

Sunobinop (S 117957) TFA is an orally active and blood-brain barrier-penetrating selective partial agonist of the human nociceptin/orphanin FQ peptide receptor (NOP), with high affinity for human targets (Ki=3.3 nM; EC50=4.03 nM; Emax=47.8%), without activating μ and κ opioid receptors. In rats, Sunobinop TFA significantly reduces wakefulness and increases non-rapid eye movement (NREM) sleep through NOP receptor activation, without significant side effects on learning, memory, reward, respiration, or intestinal function at effective doses. It also displays competitive antagonist properties in certain signaling pathways [such as β-Arrestin 2 recruitment]. Sunobinop TFA can be employed in research involving insomnia, moderate to severe alcohol use disorder, and incontinence due to bladder overactivity.

Basimglurant (RG7090; RO4917523) sulfate is a selective, orally bioavailable negative allosteric modulator of the metabotropic glutamate receptor 5 (mGluR5) that can cross the blood-brain barrier. It exhibits a Ki of 1.4 nM for [³H]-ABP688 and 35.6 nM for [³H]-MPEP. Basimglurant sulfate inhibits mGlu5-mediated signaling pathways and receptor constitutive activity, modulates nucleus accumbens dopamine levels, and exerts anxiolytic, antidepressant-like, analgesic, and wakefulness-promoting effects, while altering δ-wave power during non-rapid eye movement sleep. It is applicable in research related to depression, fragile X syndrome, and anxiety disorders.

Adrafinil, (R)- is the R isomer of Adrafinil -- a eugeroic that was formerly used to promote alertness, attention, wakefulness, mood, and other parameters, particularly in the elderly.

ABD459 is a neutral antagonist of the central cannabinoid 1 (CB1) receptor (Ki = 8.6 nM). It inhibits food consumption in nonfasted mice without affecting motor activity. ABD459 reduces active food seeking for 5-6 hours after treatment, with no rebound after washout. ABD459 also diminishes rapid eye movement (REM) sleep, with no alterations of wakefulness or non-REM sleep.

Potent trace amine 1 (TA1) receptor agonist (EC50 values are 0.12, 35 and 17-85 nM for mouse, rat and human receptors, respectively). Increases wakefulness and reduces REM and NREM sleep duration in wild type mice. Inhibits spontaneous locomotor activity in dopamine transport (DAT) knockout mice. Espinoza et al (2018) Biochemical and functional characterization of the trace amine-associated receptor 1 (TAAR1) agonist RO5263397. Front.Pharmacol. 9 645 PMID:29977204 |Galley et al (2015) Discovery and characterization of 2-aminooxazolines as highly potent, selective, and orally active TAAR1 agonists. ACS.Med.Chem.Letts. 7 192 PMID:26985297 |Schwartz et al (2017) Trace amine-associated receptor 1 regulates wakefulness and EEG spectral composition. Neuropsychopharmacology. 42 1305 PMID:27658486

Irdabisant hydrochloride (CEP-26401) is a selective, orally active, and blood-brain barrier penetrating histamine H3 receptor (H3R) inverse agonist, demonstrating high affinity with K*i values of 7.2 nM and 2.0 nM for rat and human H3R, respectively. Exhibiting relatively low hERG current inhibitory activity with an IC*50 of 13.8 μM, this compound has shown to enhance cognition and promote wakefulness in rat social recognition models, suggesting potential applications in schizophrenia or cognitive impairment research.

Paraxanthine-D6 is intended for use as an internal standard for the quantification of paraxanthine by GC- or LC-MS. Paraxanthine (T4973) is an active metabolite of caffeine. It is formed via N3-demethylation of caffeine by the cytochrome P450 (CYP) isoform CYP1A2. Paraxanthine (T4973) is an adenosine A1 and A2 receptor antagonist. In vivo, paraxanthine increases striatal cGMP and extracellular striatal dopamine levels and locomotor activity, as well as inhibits motor depression induced by the adenosine A1 agonist CPA or the adenosine A2 receptor agonist CGS 21680 in rats not habituated to caffeine. It also promotes wakefulness and increases locomotor activity and core temperature in narcoleptic transgenic mice without increasing behavioral anxiety.

Neuropeptide S(Mouse) TFA, an endogenous agonist for the neuropeptide S receptor (NPSR) with an EC50 value of 3 nM, plays a significant role in physiological processes by inducing the mobilization of intracellular Ca2+. This compound elevates locomotor activity and wakefulness, and simultaneously decreases anxiety-like behavior in mice.

Neuropeptide S(Rat) TFA, a robust endogenous agonist for the neuropeptide S receptor (NSPR) with an EC50 of 3.2 nM, enhances locomotor activity and promotes wakefulness while concurrently diminishing anxiety-like behavior in mice.

Firazorexton hydrate (TAK-994) is a brain-penetrant, orally active agonist of the orexin type 2 receptor (OX2R) with a potent EC50 of 19 nM, effectively reducing wakefulness fragmentation and cataplexy-like episodes in mouse models of narcolepsy [1].

RTIOXA-43 is an OX2R/OX1R (orexin receptor) dual agonist that increases wakefulness and attenuates episodic sleep symptoms and is commonly used in studies related to narcolepsy and neural signaling.

Orexin B, human-13C6,15N (Human orexin B-13C6,15N) TFA is a variant of Orexin B, human, labeled with 13C and 15N isotopes. This compound acts as an agonist of the orexin receptors (Orexin Receptor, OX Receptor), with Ki values of 420 nM for OXR1 and 36 nM for OXR2. Orexin B, human plays a role in the regulation of appetite, wakefulness, cardiovascular function, and neuroendocrine activity.

Orexin B, human-13C18,15N3 (Human orexin B-13C18,15N3) TFA is the 13C and 15N labeled form of Orexin B, human. This compound acts as an agonist for the orexin receptor (Orexin Receptor, OX Receptor) with Ki values of 420 nM for OXR1 and 36 nM for OXR2. Orexin B, human plays a role in regulating appetite, wakefulness, cardiovascular functions, and neuroendocrine processes.

Potent endogenous neuropeptide S receptor (NPSR) agonist (EC50 = 3 nM). Induces mobilization of intracellular Ca2+. Increases locomotor activity and wakefulness in mice. Also reduces anxiety-like behavior in mice.

Potent endogenous neuropeptide S receptor (NSPR) agonist (EC50 = 3.2 nM). Increases locomotor activity and wakefulness in mice. Also reduces anxiety-like behavior in mice.

Potent endogenous neuropeptide S receptor agonist (EC50 = 9.4 nM). Increases locomotor activity and wakefulness in mice. Also reduces anxiety-like behavior in mice.

CCHa1 peptide, a signaling peptide, plays a role in modulating wakefulness. Produced by enteroendocrine cells within the gut, it targets specific dopamine neurons in the brain to regulate an animal's response to sensory inputs such as mechanical vibrations, thereby aiding in the suppression of wakefulness. This peptide holds promise for research into sleep quality and sensory adaptiveness.