Samelisant free base
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.
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- CAS No.: 1394808-82-2
- 화학식: C21H31N3O3
- 분자량:373.49
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
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Biological Activity
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.
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.
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Animal Model:Male Wistar rats or male C57BL6J mice[1]
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Dosage:1, 3, 10, and 30 mg/kg
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Administration:Oral administration
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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.
Chemical Information
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CAS No. 1394808-82-2
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분자량 373.49
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화학식 C21H31N3O3
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SMILES
O=C(NC1=CC=C(OC2CCN(C3CCC3)CC2)C=C1)CN4CCOCC4
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Synonyms
SUVN-G3031 free base
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Samelisant free base Related Classifications
HY-122608 Related Classifications
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