Name | Samelisant |
Description | Samelisant (SUVN-G3031) is a selective and inverse agonist of H3 receptor with Kis of 8.7 nM and 9.8 nM for human and rat. Samelisant has anticataplectic effects and can be used in studies about narcolepsy. |
In vitro | Samelisant (1, 10, and 100 nM) increases the pEC50 from 8.5 to 8.2, 7.3, and 6.2 for human H3 receptor and from 8.2 to 7.9, 7.4, and 6.4 for rat H3 receptor, respectively. Samelisant modulates dopamine and norepinephrine levels in the cerebral cortex. Samelisant reversibly binds to the orthosteric site with Kbs of 1.3 nM and 1.1 nM[1]. |
In vivo | In orexin knockout mice subjected to sleep EEG, Samelisant (10 and 30 mg/kg; p.o.) significantly increases wakefulness and concomitantly decreases NREM sleep. Samelisant significantly decreases direct REM sleep onset episodes and dose-dependently increases the level of tele-methylhistamine[1]. |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
Solubility Information | DMSO : 50 mg/mL (112.01 mM), Sonication and heating to 60℃ are recommended.
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Keywords | SUVN-G-3031 | SUVN-G 3031 | Samelisant |
Inhibitors Related | Chlorphenesin | Meclizine dihydrochloride | Mirtazapine | Lidocaine | Famotidine | Mebhydrolin napadisylate | Amitriptyline hydrochloride | Sodium butanoate | Nizatidine | Alginic acid | Trazodone hydrochloride | Mianserin hydrochloride |
Related Compound Libraries | Pain-Related Compound Library | Anti-Neurodegenerative Disease Compound Library | Bioactive Compound Library | Neuronal Signaling Compound Library | Membrane Protein-targeted Compound Library | Anti-Cancer Clinical Compound Library | Neurotransmitter Receptor Compound Library | Drug Repurposing Compound Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | GPCR Compound Library | Anti-Cancer Drug Library |