113-92-8 Usage
Description
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.
Chemical Properties
White Solid
Uses
Different sources of media describe the Uses of 113-92-8 differently. You can refer to the following data:
1. An antagonist of the histamine H1-receptor
2. Antihistaminic
3. (±)-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
Brand name
Trimeton (Schering-Plough); Teldrin (GlaxoSmithKline).
General Description
Different sources of media describe the General Description of 113-92-8 differently. You can refer to the following data:
1. 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.
2. Odorless white crystalline solid or white powder with a bitter taste. pH (2% aqueous solution) 5. pH (1% aqueous solution) 4-5.
Air & Water Reactions
Water soluble.
Reactivity Profile
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.
Fire Hazard
Flash point data for Chlorpheniramine maleate are not available; however, Chlorpheniramine maleate is probably combustible.
Biochem/physiol Actions
Chlorpheniramine maleate (CPM) can prevent rhinitis and urticaria. It is used to cure several allergic conditions. This antihistamine is used in small-animal veterinary practices.
Safety Profile
Poison by ingestion, intravenous, and subcutaneous routes. Experimental reproductive effects. Used as an antihistamine. Mutation data reported. When heated to decomposition it emits very toxic fumes of Cland NOx.
Veterinary Drugs and Treatments
Antihistamines are used in veterinary medicine to reduce or help
prevent histamine
mediated adverse effects. Chlorpheniramine
is one the more commonly used antihistamines in the cat for the
treatment of pruritus. It may also be of benefit as a mild sedative in
small animals due to its CNS depressant effects.
Dosage forms
4 to 6 mg PO q4–6h. Maximum daily dose is 24 mg for adults
and children 12 years or older. Found frequently in combination with
acetaminophen and pseudoephedrine.
Check Digit Verification of cas no
The CAS Registry Mumber 113-92-8 includes 6 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 3 digits, 1,1 and 3 respectively; the second part has 2 digits, 9 and 2 respectively.
Calculate Digit Verification of CAS Registry Number 113-92:
(5*1)+(4*1)+(3*3)+(2*9)+(1*2)=38
38 % 10 = 8
So 113-92-8 is a valid CAS Registry Number.
InChI:InChI=1/C16H19ClN2.C4H4O4/c1-19(2)12-10-15(16-5-3-4-11-18-16)13-6-8-14(17)9-7-13;5-3(6)1-2-4(7)8/h3-9,11,15H,10,12H2,1-2H3;1-2H,(H,5,6)(H,7,8)
113-92-8Relevant articles and documents
Chlorpheniramine maleate crystal form preparation method
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Paragraph 0023-0031, (2021/12/07)
The invention discloses a chlorpheniramine maleate crystal form preparation method which is different from an existing crystal form preparation method, wherein two solvents are used in the crystallization process, the impurity content in a finished product is effectively reduced, the yield and the purity are improved, the crystal form is stable, the crystal form cannot be changed due to the change of the solvent proportion, and industrial production is facilitated.
Chlorpheniramine maleate salifying substance and synthesis method and application thereof
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Paragraph 0024-0035, (2020/08/25)
The invention provides a chlorpheniramine maleate salifying substance and a synthesis method and application thereof. The synthesis method comprises the following steps: weighing the following raw material components in parts by weight: 80-90 parts of maleic acid, 460-530 parts of absolute ethyl alcohol, 190-210 parts of chlorpheniramine hydrolysate, 4-10 parts of activated carbon and the like, then stirring and mixing the weighed raw material components to obtain a preheated mixture, transferring the preheated mixture into a filter pressing kettle, carrying out filter pressing and purification to obtain a filter pressing feed liquid of a crystallization kettle, cooling the filter pressing feed liquid of the crystallization kettle, carrying out centrifugal filtration, flushing by absoluteethyl alcohol after filtration, carrying out centrifugation again to obtain the chlorpheniramine maleate salifying substance. By adopting the synthesis method disclosed by the invention, the purity and the final yield of the synthesized chlorpheniramine maleate salifying substance are improved, and the impurity content of the chlorpheniramine maleate salifying substance is reduced.
A new method for synthesizing of chlorpheniramine maleate (by machine translation)
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, (2019/11/12)
The invention belongs to the field of organic synthesis of the drug, in particular to a new synthetic method of chlorpheniramine maleate. The invention comprises the following sequence of steps: (1) under acidic conditions, to [...] in cobalt catalyst, in the presence of a [...] and 2 - halo pyridine react, generating 2 - to the benzylic pyridine; (2) 2 - to the benzylic pyridine in under the action of the sodium amide and N, N - dimethyl base halogen ethane reaction, generating the cream, chlorpheniramine and maleic acid and get chlorpheniramine maleate. The method of reaction steps is relatively short, the raw material is cheap, the process is simple, easy to operate, does not need special reaction conditions, therefore is more suitable for industrial production. (by machine translation)
