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CAS NO.113-92-8
99%(1-1000)Kilogram
factory 113-92-8 best quality Chlorpheniramine maleate supplier
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 (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.
Chlorpheniramine Maleate is a small molecule H1-receptor antagonist. Increased ornithine decarboxylase activity induced in an ischemia-reperfusion state was attenuated by Chlorpheniramine Maleate, indicating that this increase is mediated through engagement of the H1-receptor by histamine. Histamine-mediated repair of intestinal mucosa following ischemia-reperfusion was also demonstrated to operate through the H1-receptor with Chlorpheniramine Maleate. Induction of ornithine decarboxylase was blocked by Chlorpheniramine Maleate in Ehrlich carcinoma and MCF-7 cells. The positive inotropic effect of H1-receptor stimulation by histamine on protein tyrosine phosphorylation in guinea pig left atrium was antagonized by Chlorpheniramine Maleate.
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.
(±)-Chlorpheniramine maleate, H1 antagonist
Potent H1 antagonist and SNRI
Potent H1 antagonist (Ki = 2 nM) and serotonin-norepinephrine reuptake inhibitor (SNRI). Shows antiallergic, antidepressant and antianxiolytic activity.
> 99%
113-92-8