Conessine dihydrobromide
Conessine dihydrobromide is an orally active and BBB-penetrable selective histamine H3 receptor antagonist. The pKi values of Conessine dihydrobromide for rat and human H3 receptors are 7.61 and 8.27, respectively. Conessine dihydrobromide is an inhibitor of the multidrug efflux pump system in Pseudomonas aeruginosa and can enhance the activity of antibiotics. Conessine dihydrobromide has antimalarial activity. Conessine dihydrobromide can also be used in the research of muscle atrophy.
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- CAS No.: 5913-82-6
- Formule: C24H42Br2N2
- Masse moléculaire:518.41
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Stockage:
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Activité biologique
Description
In Vitro
Conessine (2.5-20 μM; 24 h) dihydrobromide inhibits p53-, NF-κB-, and FoxO3a-dependent transcription in HEK293 cells[1].
Conessine (10 μM) dihydrobromide reduces the levels of MuRF1 and atrogin-1 in Dexamethasone (HY-14648)-treated C2C12 myotube cells[1].
Conessine (72 h) dihydrobromide has antimalarial activity, with IC50 values of 1.9 and 1.3 μg/mL in the schizont maturation method and pLDH assay, respectively[2].
Conessine (74 h) dihydrobromide is cytotoxic to L-6 cells, with an IC50 of 14 μg/mL[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Conessine (0.1-10 mg/kg; subcutaneously; single dose) dihydrobromide can exacerbate ethanol-induced psychostimulant effects in mice[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c mice aged 4-6 weeks old (22-26 g) were infected with Plasmodium berghei[2]
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Dosage:10, 20 and 50 mg/kg
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Administration:Oral administration; 4 days
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Result:Significantly reduced parasitaemia in infected mice. The parasite inhibition rates were 88.95% at 10 mg/kg, 56.6% at 20 mg/kg, and 50.99% at 50 mg/kg on day 7. The mean survival time of mice in the 10 mg/kg group was 13.3 days, in the 20 mg/kg group was 11.6 days, and in the 50 mg/kg group was 11.5 days.
Affected the liver and kidney function of mice, as shown by the changes in the levels of alkaline phosphatase (ALP), bilirubin, urea, and creatinine in serum.
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Animal Model:Male Swiss mice (30-35 g) treated ethanol[3]
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Dosage:0.1, 1 and 10 mg/kg
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Administration:Subcutaneously; single dose
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Result:Exacerbated ethanol effects on locomotor activity in a dose-dependent manner.
Had reinforcing proprieties per se in the conditionedplace preference (CPP) procedure at dose of 10 mg/kg, but it did not alter the acquisition of ethanol CPP.
Blocked ethanol effects on dopaminergic and noradrenergic neurotransmission.
Chemical Information
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CAS No. 5913-82-6
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Masse moléculaire 518.41
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Formule C24H42Br2N2
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SMILES
C[C@H]1[C@]2([H])[C@]3(CN1C)[C@](CC2)([H])[C@@]4([H])[C@]([C@@]5(C(C[C@H](CC5)N(C)C)=CC4)C)([H])CC3.Br.Br
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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]. Kim H, et al. Conessine treatment reduces dexamethasone-induced muscle atrophy by regulating MuRF1 and atrogin-1 expression [published online ahead of print, 2018 Feb 1]. J Microbiol Biotechnol. 2018;10.4014.jmb.1711.11009 [Content Brief]
[2]. Dua VK, et al. Anti-malarial property of steroidal alkaloid conessine isolated from the bark of Holarrhena antidysenterica. Malar J. 2013 Jun 10;12:194. [Content Brief]
[3]. Morais-Silva G, et al. Conessine, an H3 receptor antagonist, alters behavioral and neurochemical effects of ethanol in mice. Behav Brain Res. 2016 May 15;305:100-7. [Content Brief]
[4]. Siriyong T, et al. Conessine as a novel inhibitor of multidrug efflux pump systems in Pseudomonas aeruginosa. BMC Complement Altern Med. 2017 Aug 14;17(1):405. [Content Brief]
[5]. Zhao C, et al. The alkaloid conessine and analogues as potent histamine H3 receptor antagonists. J Med Chem. 2008 Sep 11;51(17):5423-30. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Conessine dihydrobromide Related Classifications
HY-107566A Related Classifications
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