[3-(4-chlorophenyl)-3-(2-pyridyl)propyl]dimethylamine, (2Z)but-2-enedioic acid

DescriptionChlorpheniramine 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.

UsesAn antagonist of the histamine H1-receptor

Uses(±)-Chlorpheniramine maleate salt has been used:as H1 receptor antagonist to determine the receptor functionto block the effect of compound 48/80 on plasma IGF-Ias a standard for fast sensing and determination by sequential injector coupled with potentiometer

UsesAntihistaminic

General DescriptionChlorpheniraminemaleate, (±)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 (see under “Dexchlorpheniramine Maleate” ).The usual dose is 2 to 4 mg 3 or 4 times a day. It has a halflifeof 12 to 15 hours.

General DescriptionOdorless white crystalline solid or white powder with a bitter taste. pH (2% aqueous solution) 5. pH (1% aqueous solution) 4-5.