Conessine (dihydrobromide)

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^{[1][2][3][4][5]}. 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]. 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].