Conessine

Conessine is an orally active and BBB-penetrable selective histamine H3 receptor antagonist. The pKi values of Conessine for rat and human H3 receptors are 7.61 and 8.27, respectively. Conessine is an inhibitor of the multidrug efflux pump system in Pseudomonas aeruginosa and can enhance the activity of antibiotics. Conessine has antimalarial activity. Conessine can also be used in the research of muscle atrophy[1][2][3][4][5].

Product Specifications

CAS Number

[546-06-5]

UNSPSC

12352005

Hazard Statement

H315, H319, H335

Target

Bacterial; FOXO; Histamine Receptor; MDM-2/p53; NF-κB; Parasite

Type

Natural Products

Related Pathways

Anti-infection; Apoptosis; GPCR/G Protein; Immunology/Inflammation; Metabolic Enzyme/Protease; Neuronal Signaling; NF-κB

Applications

COVID-19-immunoregulation

Field of Research

Infection; Neurological Disease

Assay Protocol

https://www.medchemexpress.com/conessine.html

Purity

99.87

Solubility

DMSO : 3.33 mg/mL (ultrasonic; warming; heat to 60°C) |Ethanol : 25 mg/mL (ultrasonic)

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

Molecular Formula

C24H40N2

Molecular Weight

356.59

Precautions

H315, H319, H335

References & Citations

[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.|[2]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.|[3]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.|[4]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.|[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.