Clobenpropit
Clobenpropit is a potent histamine H3-receptor antagonist. Clobenpropit decreases dopamine release and increases histamine levels in the hypothalamus. Clobenpropit shows antipsychotic-like activities. Clobenpropit causes a resuscitating effect in rats subjected to the hemorrhagic shock.
At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (Clobenpropit dihydrobromide) usually boasts enhanced water solubility and stability.
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- CAS No.: 145231-45-4
- Formule: C14H17ClN4S
- Masse moléculaire:308.83
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Other In-stock Forms of Clobenpropit
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
IC50 & Target
[1]|
H3 receptor |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | EC50 |
1.7 nM
Compound: clobenpropit
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Inverse agonist activity at mouse histamine H3 receptor overexpressed in HEK293 cells by [35S]GTPgammaS binding assay
Inverse agonist activity at mouse histamine H3 receptor overexpressed in HEK293 cells by [35S]GTPgammaS binding assay
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[PMID: 19553110] |
| HT-1080 | IC50 |
1 nM
Compound: Clobenpropit
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Antagonist activity against human histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assay
Antagonist activity against human histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assay
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[PMID: 20833043] |
| HT-1080 | IC50 |
1 nM
Compound: Clobenpropit
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Antagonist activity against mouse histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assay
Antagonist activity against mouse histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assay
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[PMID: 20833043] |
In Vivo
Clobenpropit (1, 2, 5 μmoL/kg; i.v.) causes a resuscitating effect in rats subjected to the hemorrhagic shock[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:150-200g, 12-week-old male wistar albino rats[1]
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Dosage:15 mg/kg
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Administration:I.p.; once daily for 7 days
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Result:Exhibited a significant reduction of hyperlocomotor activities induced by a single-dose administration of MK-801 (0.2 mg/kg, i.p.), and reduced the MK-801-induced dopamine release, exhibited further increase in histamine levels in the hypothalamus.
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Animal Model:205-470g, adult male Wistar rats[2]
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Dosage:1, 2, 5 μmoL/kg (after 6-hydroxydopamine (50 mg/kg (SC) for 3 consecutive days)
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Administration:I.v.
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Result:Triggered a statistically significant increase of mean arterial pressure (MAP) (dose 2 μmol/kg) and heart rate (HR) (doses of 1, 2, 5 μmol/kg).
Chemical Information
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CAS No. 145231-45-4
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Masse moléculaire 308.83
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Formule C14H17ClN4S
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SMILES
N=C(SCCCC1=CN=CN1)NCC2=CC=C(Cl)C=C2
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Mahmood D, et al. The Effect of Subchronic Dosing of Ciproxifan and Clobenpropit on Dopamine and Histamine Levels in Rats. J Exp Neurosci. 2015 Aug 31;9:73-80. [Content Brief]
[2]. Wanot B, et al. Cardiovascular effects of H3 histamine receptor inverse agonist/ H4 histamine receptor agonist, clobenpropit, in hemorrhage-shocked rats. PLoS One. 2018 Aug 2;13(8):e0201519. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Clobenpropit Related Classifications
HY-115447 Related Classifications
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