1. GPCR/G Protein Neuronal Signaling Immunology/Inflammation
  2. Histamine Receptor
  3. (±)-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.

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(±)-Carbinoxamine

(±)-Carbinoxamine Chemical Structure

CAS No. : 486-16-8

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Description

(±)-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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

290.79

Formula

C16H19ClN2O

CAS No.
SMILES

CN(CCOC(C1=CC=CC=N1)C2=CC=C(C=C2)Cl)C

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

Purity & Documentation
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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(±)-Carbinoxamine
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HY-B1589
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