Chlorphenamine maleate #CAS113-92-8

Chlorphenamine maleate #CAS113-92-8

Chlorpheniraminemaleate, (±)2-[p-chloro-α-[2-dimethylamino)ethyl]benzyl]pyridine bimaleate (Chlor-Trimeton), is a white crystallinepowder that is soluble in water (1:3.4), in alcohol(1:10), and in chloroform (1:10). It has a pKa of 9.2, and anaqueous solution has a pH between 4 and 5. Chlorination ofpheniramine in the para position of the phenyl ring increasespotency 10-fold with no appreciable change in toxicity.Most of the antihistaminic activity resides with thedextro isomer .The usual dose is 2 to 4 mg 3 or 4 times a day. It has a halflifeof 12 to 15 hours.

A halogenated amine, ester. Amines are chemical bases. They neutralize acids to form salts plus water. These acid-base reactions are exothermic. The amount of heat that is evolved per mole of amine in a neutralization is largely independent of the strength of the amine as a base. Amines may be incompatible with isocyanates, halogenated organics, peroxides, phenols (acidic), epoxides, anhydrides, and acid halides. Flammable gaseous hydrogen is generated by amines in combination with strong reducing agents, such as hydrides. Esters react with acids to liberate heat along with alcohols and acids. Strong oxidizing acids may cause a vigorous reaction that is sufficiently exothermic to ignite the reaction products. Heat is also generated by the interaction of esters with caustic solutions. Flammable hydrogen is generated by mixing esters with alkali metals and hydrides.

Chlorpheniramine is a histamine H1 receptor antagonist with an IC75 value of 0.0016 μg/ml for reversal of histamine-induced spasms in isolated guinea pig ileum. It protects against intravenous histamine-induced death (PD50 = 0.15 mg/kg) and delays induction of aerosolized histamine-induced coughing (ED100sec = 0.44 mg/kg) in guinea pigs. Chlorpheniramine (20 mg/kg, i.p.) prevents histamine-induced passive cutaneous anaphylaxis (PCA) in rabbits. It also reduces respiratory resistance and hypersecretion of tracheobronchial fluid in a dog model of histamine-induced asthma. Formulations containing chlorpheniramine have been used in the treatment of seasonal allergies.

Application Of Chlorphenamine maleate 

An antagonist of the histamine H1-receptor

(±)-Chlorpheniramine maleate salt has been used:

as H1 receptor antagonist to determine the receptor function

to block the effect of compound 48/80 on plasma IGF-I

as a standard for fast sensing and determination by sequential injector coupled with potentiometer

Antihistaminic

The indications of chlorpheniramine maleate are for colds and allergic diseases of the skin and mucous membranes. Its main functions include urticaria, eczema, dermatitis, drug eruption, pruritus of the skin, neurodermatitis, insect bites, sun-induced dermatitis, and also allergic dermatitis, vasomotor rhinitis, and drug and food allergies. Besides having a strong competitive blocking effect on the H1 receptors on the target cells of allergic reactions, which plays an anti-allergic role by antagonizing the H1 receptors, it also has an anti-M cholinergic receptor effect. Therefore, after taking the medicine, symptoms such as dry mouth, constipation, thickened sputum, and dry nasal mucosa may occur.

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