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.

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.

Paraxanthine-d6 is intended for use as an internal standard for the quantification of paraxanthine by GC- or LC-MS. Paraxanthine is an active metabolite of caffeine. It is formed via N3-demethylation of caffeine by the cytochrome P450 (CYP) isoform CYP1A2. Paraxanthine 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.

Bavisant dihydrochloride hydrate (JNJ31001074AAC) is a highly selective, orally active antagonist of the human H3 receptor with a novel mechanism of action, involving wakefulness and cognition, with potential as a treatment for ADHD. in vivo: Mean change

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.

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

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

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

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.

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.

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.

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.

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.

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

Paraxanthine (1,7-dimethylxanthine) is a metabolite of caffeine (sc-202514) which functions as an adenosine receptor ligand and a PARP-1 inhibitor in pulmonary epithelial cells. Studies suggest that Paraxanthine is structurally similar to caffeine and possibly mediates the physiological effects of caffeine. Also Paraxanthine acts as a competitive phosphodiesterase inhibitor, which increases intracellular cAMP, activates PKA, inhibits TNF-α and leukotriene synthesis. In addition, Paraxanthine acts as a Na+/K+ ATPase enzymatic effector.