Chlorpheniramine, a histamine H1 antagonist used in allergic reactions, hay fever, rhinitis, urticaria, and asthma. It has also been used in veterinary applications. One of the most widely used of the classical antihistaminics, it generally causes less drowsiness and sedation than promethazine. Chlorpheniramine binds to the histamine H1 receptor. This blocks the action of endogenous histamine, which subsequently leads to temporary relief of the negative symptoms brought on by histamine.
|Cell lines||MCF-7, MDA-MB 231, and Ehrlich|
|Preparation method||Exposing cells to various concentrations of Chlorpheniramine for 48 hours. Cells are washed, detached, and counted with a Coulter counter to determine cell growth.|
|Concentrations||Dissolved in water, final concentrations ~500 μM|
|Incubation time||48 hours|
|Animal models||Male NC/Nga mice, male ICR mice and female BALB/c mice with atopic dermatitis|
|Formulation||Suspended in 1% (v/v) Tween 80|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO 70 mg/mL|
|Related Histamine Receptor Products|
Fexofenadine is a nonsedating antihistamine drug which is indicated for treatment of seasonal allergic rhinitis.
|Roxatidine Acetate HCl
Roxatidine Acetate HCl is a specific and competitive histamin H2-receptor antagonist, with IC50 of 3.2 μM, inhibits gastric acid secretion and ulcer formation.
Ranitidine is a histamine H2-receptor antagonist, used to treat stomach or intestinal ulcers.
Mizolastine is a histamine H1-receptor antagonist with IC50 of 47 nM used in the treatment of hay fever (seasonal allergic rhinitis), hives and other allergic reactions.
Loratadine is a histamine H1 receptor antagonist, used to treat allergies. Also acts as a selective inhibitor of B(0)AT2 with IC50 of 4 μM.
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