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Pemirolast potassium

Pemirolast potassium structure

CAS No:
100299-08-9
Formula:
C10H8N6O.K
Chemical Name:
Pemirolast potassium
Synonyms:
4H-Pyrido[1,2-a]pyrimidin-4-one,9-methyl-3-(2H-tetrazol-5-yl)-,potassium salt (1:1);4H-Pyrido[1,2-a]pyrimidin-4-one,9-methyl-3-(1H-tetrazol-5-yl)-,potassium salt;TBX (pharmaceutical);BMY 26517;Pemirolast potassium;TBX;Alegysal;Alamast;Pemirolast potassium salt;Pemilaston;Ulgixal;Potassium 9-methyl-3-(2,3,4-triaza-1-azanidacyclopenta-2,4-dien-5-yl)pyrido[2,1-b]pyrimidin-4-one;Potassium 5-(9-methyl-4-oxo-4H-pyrido[1,2-a]pyrimidin-3-yl)tetrazol-1-ide;1210648-64-8
Categories:
Active Pharmaceutical Ingredients > Antiallergic Drugs

Description

Crystalline SolidPemirolast potassium is a new potent antiallergic mast cell stabilizer with a similarmechanism to sodium cromoglycate. Its main indication is bronchial asthma. Anotherindication under investigation is as a gastroprotective agent.Pemirolast potassium, 9-methyl-3-(1H-tetrazol-5-yl)-4Hpyrido[1, 2- ]pyrimidin-4-one potassium (Alamast), is ayellow, water-soluble powder. It can be considered an analogof one portion of the cromolyn structure in which thecarboxyl group has been rep

Pemirolast Potassium is the potassium salt form of pemirolast, a pyrimidinone derivative with antiallergic property. Pemirolast potassium exerts its action by blocking the antigen-mediated calcium ion influx into mast cells. This prevents mast cell degranulation, resulting in mast cell stabilization and inhibition of the release of inflammatory mediators, histamine and leukotrienes, which are involved in the allergic process. Pemirolast potassium also prevents inflammatory mediator release from eosinophils.

Pemirolast potassium Basic Attributes

Molecular Weight：

266.3

Exact Mass：

266.031830

UNII：

497A17OUUE

DSSTox ID：

DTXSID7046623

NCI Thesaurus Code：

C47654

Characteristics

PSA：

72.3

Appearance：

light yellow to yellow with a green cast

Melting Point：

310-311°C (dec.)

Boiling Point：

454.8°C at 760 mmHg

Flash Point：

228.9ºC

Water Solubility：

H2O: ≥18mg/mL

Storage Conditions：

-20°C Freezer, Under Inert Atmosphere

Vapor Pressure：

3.3X10-6 mm Hg at 25 deg C /Estimated/

Safety Information

Transport codes：

NONH for all modes of transport

wgk germany：

RTECS Number：

UV1164470

Precautionary statement(s)：

P264, P270, P301+P312, P330, P501

Hazard Statements：

H302

GHS Classification：

|Warning|H302 (100%): Harmful if swallowed [Warning Acute toxicity, oral]|P264, P270, P301+P312, P330, and P501|Aggregated GHS information provided by 39 companies from 2 notifications to the ECHA C&L Inventory.

Drug Information

MeSH：

Drugs that bind to but do not activate histamine receptors, thereby blocking the actions of histamine or histamine agonists. Classical antihistaminics block the histamine H1 receptors only. (See all compounds classified as Histamine Antagonists.)

MeSH Entry Terms：

9-methyl-3-(1H-tetrazol-5-yl)-4H-pyrido(1,2-a)pyrimidin-4-one

Pemirolast potassium Use and Manufacturing

Uses

Pemirolast potassium (BMY 26517) is a histamine H1 antagonist and mast cell stabilizer that acts as an antiallergic agent This product is a new type of mast cell membrane stabilizer, which is jointly developed by Bumai-Squibb and Tokyo Tanabe Pharmaceutical Company to inhibit the release of allergic mediators caused by antigens.

Use Classification：

Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients

Computed Properties

Molecular Weight:266.30
Hydrogen Bond Acceptor Count:6
Rotatable Bond Count:1
Exact Mass:266.03184035
Monoisotopic Mass:266.03184035
Topological Polar Surface Area:72.3
Heavy Atom Count:18
Complexity:495
Covalently-Bonded Unit Count:2
Compound Is Canonicalized:Yes

Drug Function and Efficacy

This product inhibits the release of chemical mediators by inhibiting inositol phosphate metabolism, and has an inhibitory effect on the influx of extracellular Ca2 and the release of intracellular Ca2; it also inhibits the release of arachidonic acid and the activity of phosphodiesterase, increasing the level of cyclic adenosine monophosphate (c-AMP); it has the effect of relaxing bronchial smooth muscle in vitro.

This ingredient has been used in drugs with the following functions (note: it does not mean that the ingredient itself has the following health functions)

Related Drugs

Pemirolast Potassium Eye Drops
Ingredients	The main ingredient of this product: Pemirolast potassium.
Specifications	5ml:5mg

Pemirolast Potassium Tablets
Ingredients	The main ingredient of this product is pyrimirolast potassium, whose chemical name is 9-methyl-3-(1H-5-tetrazolyl)-4H-pyrido[1,2-]pyrimidin-4-one potassium.
Indication	Not yet clear
Specifications	10mg
Manufacturer	China National Medicines Guorui Pharmaceutical Co., Ltd.

Pemirolast Potassium Eye Drops
Ingredients	Main ingredients: The main ingredient of this product is Pemirolast Potassium
Indication	Not yet clear.
Specifications	5 ml: 5 mg

See More Related Drugs

Registered Holders

Lesheng Pharmaceutical Shijiazhuang Co., Ltd.

China
Active
SPH Qingdao Growful Pharmaceutical Co., Ltd.

China
Active
Jiangsu Feima Pharmaceutical Co., Ltd.

China
Active

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CAS No.: 100299-08-9

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