2. GPCR/G Protein Neuronal Signaling Immunology/Inflammation
  3. Histamine Receptor
  4. 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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Clobenpropit Chemical Structure

Clobenpropit Chemical Structure

CAS No. : 145231-45-4

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Description

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[1][2].

IC50 & Target[1]

H3 receptor

 

In Vivo

Clobenpropit (15 mg/kg; i.p.; once daily for 7 days) counteracts the modulatory effects of MK-801 (HY-15084B) on dopamine and histamine levels and prevents MK-801-induced hyper locomotor behaviors[1].
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.

Animal Model: 150-200g, 12-week-old male wistar albino rats[1]
Dosage: 15 mg/kg
Administration: I.p.; once daily for 7 days
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.
Animal Model: 205-470g, adult male Wistar rats[2]
Dosage: 1, 2, 5 μmoL/kg (after 6-hydroxydopamine (50 mg/kg (SC) for 3 consecutive days)
Administration: I.v.
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).
Molecular Weight

308.83

Formula

C14H17ClN4S
CAS No.
SMILES

N=C(SCCCC1=CN=CN1)NCC2=CC=C(Cl)C=C2
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Storage

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

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  • 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:

Clobenpropit145231-45-4Histamine Receptordopaminehistamineantipsychotic-likehemorrhagic shockMAPHRInhibitorinhibitorinhibit

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