Conessine dihydrobromide

Cat. No.: HY-107566A: Data Sheet Handling Instructions
FAQs
Technical Support

Conessine dihydrobromide is an orally active and BBB-penetrable selective histamine H3 receptor antagonist. The pK_i 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.

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

Conessine dihydrobromide Chemical Structure

CAS No. : 5913-82-6

Size		Stock
MOQ		Minimum order quantity
50 mg		Get quote
100 mg		Get quote
250 mg		Get quote
Other size		Get quote

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Other In-stock Forms of Conessine dihydrobromide:

Conessine

Other Forms of Conessine dihydrobromide:

Conessine In-stock

Featured Recommendations

•Related Small Molecules:

•Related Proteins:

View All Histamine Receptor Isoform Specific Products:

View All Isoforms

H₁ Receptor H₂ Receptor H₃ Receptor H₄ Receptor Histamine Receptor

View All Parasite Isoform Specific Products:

View All Isoforms

Amebae Coccidia Leishmania Mite Plasmodium Toxoplasma Trypanosoma Schistosome

View All NF-κB Isoform Specific Products:

View All Isoforms

NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

View All FOXO Isoform Specific Products:

View All Isoforms

FOXO1 FOXO3

Biological Activity
Purity & Documentation
References
Customer Review

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 (10-50 mg/kg; oral administration; 4 days) dihydrobromide significantly reduces parasitaemia in mice infected with P. berghei^[2].
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.

Animal Model:	BALB/c mice aged 4-6 weeks old (22-26 g) were infected with Plasmodium berghei^[2]
Dosage:	10, 20 and 50 mg/kg
Administration:	Oral administration; 4 days
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.

Animal Model:	Male Swiss mice (30-35 g) treated ethanol^[3]
Dosage:	0.1, 1 and 10 mg/kg
Administration:	Subcutaneously; single dose
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.

Molecular Weight

518.41

Formula

C₂₄H₄₂Br₂N₂

CAS No.

5913-82-6

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[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]