(±)-Carbinoxamine

(±)-Carbinoxamine is a blood-brain barrier-permeable histamine H1 receptor antagonist. (±)-Carbinoxamine blocks the action of histamine on H1 receptors, reducing symptoms such as sneezing, rhinitis, rhinorrhea, erythema, pruritus and urticaria. (±)-Carbinoxamine inhibits influenza virus entry into cells via endocytosis, targets the early stage of the viral life cycle, and simultaneously reduces viral replication levels in the lungs, alleviating pathological damage and inflammatory responses in lung tissues. (±)-Carbinoxamine can be used in research on allergic rhinitis, influenza, etc.^[1][2] In Vitro:(±)-Carbinoxamine (72 h) potently inhibits infection of MDCK cells by multiple influenza A strains (H7N9, H1N1 2009, H1N1 1934, H3N2) and one influenza B strain (BY), with IC₅₀ values ranging from 3.56 to 15.54 μM^[1].
(±)-Carbinoxamine (0-1000 μM; 72 h) exhibits low cytotoxicity against MDCK cells, with a CC₅₀ of 297.30 μM, thus showing a high selection index against various influenza virus strains^[1].
(±)-Carbinoxamine (20 μM; 0-12 h) inhibits infection of MDCK cells by A/Shanghai/37T/2009 (H1N1) at the early stage of the viral life cycle; the inhibition rate reaches 99% when added at 0.5 h post-infection, and drops to 23% when added at 4 h post-infection^[1].
(±)-Carbinoxamine (48 h) specifically inhibits the entry of A/Shanghai/4664T/2013 (H7N9) pseudovirus into MDCK cells, with an IC₅₀ of 8.98 μM, and does not affect the entry of other pseudoviruses or HIV-1^[1].
(±)-Carbinoxamine (1.6-100 μM; 1.5 h) does not inhibit the neuraminidase activity of A/Puerto Rico/8/1934 (H1N1) virus even at concentrations as high as 100 μM^[1].
(±)-Carbinoxamine (12 h) reduces viral RNA synthesis in a dose-dependent manner in MDCK cells infected with the A/Puerto Rico/8/1934 (H1N1) virus^[1].
(±)-Carbinoxamine (10 μM; 12 h) reduces the number of NP-positive MDCK cells infected with A/Puerto Rico/8/1934 (H1N1) virus^[1]. In Vivo:(±)-Carbinoxamine (1-10 mg/kg; i.p.; daily; 5 days) provides 77.7% survival protection against lethal H7N9 influenza virus challenge in female C57BL/6 mice, while also reducing viral load and lung pathology in a dose-dependent manner^[1].