2. GPCR/G Protein Neuronal Signaling Immunology/Inflammation
  3. Histamine Receptor
  4. Samelisant free base

Samelisant free base  (Synonyms: SUVN-G3031 free base)

Cat. No.: HY-122608
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Samelisant (SUVN-G3031) free base is a potent and selective histamine H3 receptor (H3R) inverse agonist with good brain penetration and oral bioavailability. Samelisant free base has a similar binding affinity towards human (hH3R; Ki=8.7 nM) and rat (rH3R;Ki=9.8 nM) H3R indicating no inter-species differences. Samelisant free base can be used for the research of sleep-related disorders.

For research use only. We do not sell to patients.

Samelisant free base Chemical Structure

Samelisant free base Chemical Structure

CAS No. : 1394808-82-2

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Description

Samelisant (SUVN-G3031) free base is a potent and selective histamine H3 receptor (H3R) inverse agonist with good brain penetration and oral bioavailability. Samelisant free base has a similar binding affinity towards human (hH3R; Ki=8.7 nM) and rat (rH3R;Ki=9.8 nM) H3R indicating no inter-species differences. Samelisant free base can be used for the research of sleep-related disorders[1].

In Vitro

Samelisant free base displays inverse agonist activity and it exhibits very high selectivity towards H3R. The pEC50 value of histamine (8.5) for human H3 receptor increases to 8.2, 7.3 and 6.2 after treatment with 1, 10 and 100 nM of Samelisant, respectively. The pEC50 value of histamine (8.2) for rat H3 receptor increases to 7.9, 7.4 and 6.4 after treatment with 1, 10 and 100 nmol/L of Samelisant, respectively[1].
Samelisant free base binds to the orthosteric site in a reversible manner with Kb values of 1.3 nM and 1.1 nM deduced from pA2 value for human and rat H3R, respectively[1].
Samelisant free base also modulates dopamine and norepinephrine levels in the cerebral cortex while it has no effects on dopamine levels in the striatum or nucleus accumbens[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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In Vivo

Treatment with Samelisant (10 and 30 mg/kg, p.o.) free base produces a significant increase in wakefulness with a concomitant decrease in non-rapid eye movement sleep (NREM) sleep in orexin knockout mice subjected to sleep electroencephalography (EEG)[1].
Samelisant free base also produces a significant decrease in direct rapid eye movement (REM) sleep onset (DREM) episodes, demonstrating its anticataplectic effects in an animal model relevant to narcolepsy[1].
Samelisant free base treatment in mice produces a dose-dependent increase in tele-methylhistamine levels indicating the activation of histaminergic neurotransmission[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Wistar rats or male C57BL6J mice[1]
Dosage: 1, 3, 10, and 30 mg/kg
Administration: Oral administration
Result: Produced a dose-dependent increase in t-MH levels in the frontal cortex, hypothalamus and cerebrospinal fluid (CSF) of male Wistar rats. Produced a significant increase in t-MH levels of the frontal cortex, striatum and hypothalamus in mice.
Clinical Trial
Molecular Weight

373.49

Formula

C21H31N3O3
CAS No.
SMILES

O=C(NC1=CC=C(OC2CCN(C3CCC3)CC2)C=C1)CN4CCOCC4
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Samelisant free base Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Samelisant1394808-82-2SUVN-G3031Histamine ReceptorhistamineH3RbrainpenetrationoralbioavailabilitysleepInhibitorinhibitorinhibit

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