16110-51-3 Usage
Uses
Used in Pharmaceutical Industry:
Cromoglicic acid is used as a prophylactic agent for the prevention of various types of asthma attacks, including seasonal, constant, and physically caused asthma. It is also used in the treatment of allergic rhinitis, mastocytosis, and vernal conjunctivitis.
Used in Allergy Management:
Cromoglicic acid is used as an anti-allergic agent for the management of allergic rhinitis, which is a common condition affecting the nasal passages. It helps to reduce the symptoms of sneezing, itching, and nasal congestion.
Used in Asthma Treatment:
Cromoglicic acid is used as a bronchodilator in the treatment of bronchial asthma. It helps to relax and widen the airways, making it easier for patients to breathe.
Used in Mast Cell Stabilization:
Cromoglicic acid is used as a mast cell stabilizer, which helps to prevent the release of histamine and other inflammatory mediators from mast cells. This property makes it useful in the treatment of conditions such as mastocytosis and vernal conjunctivitis, where mast cell activation plays a significant role in the disease process.
Therapeutic Function
Bronchodilator
Air & Water Reactions
Water soluble.
Reactivity Profile
Carboxylic acids donate hydrogen ions if a base is present to accept them. They react in this way with all bases, both organic (for example, the amines) and inorganic. Their reactions with bases, called "neutralizations", are accompanied by the evolution of substantial amounts of heat. Neutralization between an acid and a base produces water plus a salt. Carboxylic acids in aqueous solution and liquid or molten carboxylic acids can react with active metals to form gaseous hydrogen and a metal salt. Such reactions occur in principle for solid carboxylic acids as well, but are slow if the solid acid remains dry. Even "insoluble" carboxylic acids may absorb enough water from the air and dissolve sufficiently in Cromoglicic acid to corrode or dissolve iron, steel, and aluminum parts and containers. Carboxylic acids, especially in aqueous solution, also react with sulfites, nitrites, thiosulfates (to give H2S and SO3), dithionites (SO2), to generate flammable and/or toxic gases and heat.
Fire Hazard
Flash point data for Cromoglicic acid are not available. Cromoglicic acid is probably combustible.
Mechanism of action
Cromolyn stabilizes the membranes of mast cells, stopping the release of allergy mediators
and suppressing activation of eosinophiles, neutrophilis, thrombocytes, and
macrophages, which take part in the formation of bronchospasms.
Cromylyn differs from the majority of medications taken for obstructive diseases of the
respiratory tract in that it is used only as a preventative agent.
Clinical Use
Cromolyn generally is used prophylactically for bronchial asthma (as an inhaled powder), for
prevention of exercise-induced bronchospasm, and for seasonal and perennial allergic rhinitis
(nasal solution). Topically, it also is used as eye drops for allergic conjunctivitis and keratitis.
In
the management of asthmatic conditions, it is administered using a power-operated nebulizer.
The bioavailability is very low with oral administration because of poor absorption. By
inhalation, the powder is irritating to some patients. After inhalation, much less than 10% of
the dose reaches the systemic circulation. An oral dosage form is used for mastocytosis.
Synthesis
Cromolyn, 5,5[(2-hydroxytrimethylen)dioxy] bis 4-oxo-4H-1-benzopiran-2-
carboxylic acid (23.3.9), are synthesized by reacting 2,6-dihydroxyacetophenone with
epichlorohydrine, during which the chlorine atom in epichlorohydrine is replaced and an
opening of the epoxide ring takes place, resulting in a bis-product 23.3.7. Cyclization of
this product into a bis-derivative 23.3.8 is accomplished using diethyloxalate, subsequent
alkaline hydrolysis of the ester groups of which gives the desired cromolyn (23.3.9).
Environmental Fate
The major prophylactic effect of cromolyn is centered on
inhibition of the degranulation of pulmonary mast cells
causing a reduction in histamine release, reduced leukotriene
production, and inhibition of release of inflammatory mediators
from several cell types.
Toxicity evaluation
Cromolyn is a mast cell stabilizer and typically marketed as the
sodium salt in the United States. It is typically found in solution
as a clear and colorless liquid. Cromolyn is soluble in
water and the solution is completely soluble in water.
Check Digit Verification of cas no
The CAS Registry Mumber 16110-51-3 includes 8 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 5 digits, 1,6,1,1 and 0 respectively; the second part has 2 digits, 5 and 1 respectively.
Calculate Digit Verification of CAS Registry Number 16110-51:
(7*1)+(6*6)+(5*1)+(4*1)+(3*0)+(2*5)+(1*1)=63
63 % 10 = 3
So 16110-51-3 is a valid CAS Registry Number.
InChI:InChI=1/C23H16O11/c24-11(9-31-12-4-5-16-13(6-12)14(25)7-19(33-16)22(27)28)10-32-17-2-1-3-18-21(17)15(26)8-20(34-18)23(29)30/h1-8,11,24H,9-10H2,(H,27,28)(H,29,30)
16110-51-3Relevant articles and documents
METHOD OF SCREENING COMPOUND USEFUL IN TREATING ALLERGIC DISEASE
-
Page/Page column 7-8, (2010/04/30)
The present invention provides a method of screening for a compound useful for treatment of an allergic disease by identifying a molecule targeted by Intal upon exertion of its efficacy as an anti-allergic agent (hereinafter referred as a target) and using the target, as well as a new type of anti-allergic agent comprising a compound obtainable by the screening as an active ingredient for treatment of an allergic disease.
PREPARATION FOR EXTERNAL APPLICATION COMPRISING SALT OF MAST CELL DEGRANULATION INHIBITOR HAVING CARBOXYL GROUP WITH ORGANIC AMINE
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Page/Page column 7, (2008/12/07)
Mast cell degranulation inhibitors having a carboxyl group have not been developed as external preparations due to the low transdermal permeability thereof. By formulating external preparations thereof, side effects on the internal organs by oral administration can be avoided. Some of the mast cell degranulation inhibitors show drastically inferior photostability, which is also one cause of suppressed development of the drug as an external preparation. The present invention aims at improving the transdermal permeability and photostability of mast cell degranulation inhibitors by forming a salt of the mast cell degranulation inhibitor with an organic amine. Consequently, an external preparation of a mast cell degranulation inhibitor can be provided and the photostability of the mast cell degranulation inhibitor itself, and a preparation containing same can be improved.
NOVEL DRUG DISCOVERY TARGET AND MEDICINE ACTING ON THE SAME
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Page/Page column 12-13, (2008/06/13)
The present invention provides a pharmaceutical composition comprising as an active ingredient a compound that specifically binds to MFP-2 or a functional fragment thereof and a screening method for the compound; the compound and a pharmaceutical composition comprising the same are highly useful as anti-inflammatory agents and anti-allergic agents.
Use of electrolytes (ions in solution) to suppress charging of inhalation aerosols
-
, (2008/06/13)
Formulations are disclosed as are aerosols created therefrom. The formulations are comprised of (a) a pharmaceutically active drug which does not ionize in solution; (b) an electrolyte; and (c) a solvent which is preferably water and/or ethanol. The electrolyte reduces electrostatic charging on particles of aerosol formed thereby enhancing characteristics of the aerosol particles which are important for efficient, repeatable intrapulmonary drug delivery.
Method of treating atopic eczema
-
, (2008/06/13)
The present invention relates to methods of treating chronic skin disorders by externally applying to the skin compounds by the following formula STR1 and therapeutically acceptable salts, esters and amides thereof, wherein R1 through R6 and X are as hereinafter defined.