Abstract Medical efficacy Precautions References
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Mizolastine

Abstract Medical efficacy Precautions References
Product Name
Mizolastine
CAS No.
108612-45-9
Chemical Name
Mizolastine
Synonyms
MKC 431;Mizollen;Zolistan;MistaMine;SL 850324;Mizostatin;MIZOLASTINE;Mizolastine>Mizolastine HCl;Mizolastine inn
CBNumber
CB7150058
Molecular Formula
C24H25FN6O
Formula Weight
432.49
MOL File
108612-45-9.mol
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Mizolastine Property

Melting point:
217°
Density 
1.34±0.1 g/cm3(Predicted)
storage temp. 
Refrigerator
solubility 
Chloroform (Slightly, Heated), DMSO, Methanol (Slightly, Heated)
form 
Solid
pka
9.73±0.40(Predicted)
color 
White
Merck 
14,6221
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Safety

RTECS 
UW7481284
HS Code 
2933.39.9200
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

H312Harmful in contact with skin

H332Harmful if inhaled

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P271Use only outdoors or in a well-ventilated area.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.

P312Call a POISON CENTER or doctor/physician if you feel unwell.

P322Specific measures (see …on this label).

P330Rinse mouth.

P363Wash contaminated clothing before reuse.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

TCI Chemical
Product number
M2756
Product name
Mizolastine
Purity
>98.0%(HPLC)(T)
Packaging
1g
Price
$119
Updated
2024/03/01
TCI Chemical
Product number
M2756
Product name
Mizolastine
Purity
>98.0%(HPLC)(T)
Packaging
5g
Price
$469
Updated
2024/03/01
TRC
Product number
M385400
Product name
Mizolastine
Packaging
250mg
Price
$290
Updated
2021/12/16
Matrix Scientific
Product number
094171
Product name
2-((1-(1-(4-Fluorobenzyl)-1H-benzo[d]imidazol-2-yl)-piperidin-4-yl)(methyl)amino)pyrimidin-4(1H)-one
Purity
95+%
Packaging
250mg
Price
$378
Updated
2021/12/16
ChemScene
Product number
CS-1997
Product name
Mizolastine
Purity
99.33%
Packaging
500mg
Price
$400
Updated
2021/12/16
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Mizolastine Chemical Properties,Usage,Production

Abstract

Mizolastine (Mizollen) is a non-sedating antihistamine. It blocks H1 receptors and is commonly fast-acting. It does not prevent the actual release of histamine from mast cells, just prevents it binding to receptors.

Medical efficacy

Mizolastine is a second generation antihistamine agent with high affinity and specificity for histamine H(1) receptors. Mizolastine has demonstrated antiallergic effects in animals and healthy volunteers and anti-inflammatory activity in animal models. Double-blind trials
have shown mizolastine to be significantly more effective than placebo and as effective as other second generation antihistamine agents, such as loratadine or cetirizine, in the management of patients with perennial or seasonal allergic rhinitis and in patients with
chronic idiopathic urticaria.
It not only has a strong anti-histamine but also has inflammatory neurotransmitters inhibit action, such as inhibit the generation of leukotrienes, reduce edema. Thus in theory, mizolastine has both anti-histamine and anti-allergic effects. The role of anti-inflammatory activity, for the treatment of acute urticaria preferred drug, significantly the onset of action is faster than other antihistamines, and the medication can reduce the number of the wheal hours after 1-3 hours, itching abated, and maintain a long time, up to 24 hours.
At present, the clinical treatment is mainly used for the treatment of adults or children over 12 years of age suffering from urticaria and other skin allergy symptoms, seasonal allergic rhinitis (hay fever) and perennial allergic rhinitis.

Precautions

Don't take this medicine in these conditions:

  • If you are pregnant or breast-feeding.
  • If you have any problems with the way your liver works.
  • If you have a heart condition or an abnormal heart rhythm.
  • If you have epilepsy.
  • If you have a rare inherited blood disorder called porphyria.
  • If you are taking or using any other medicines. This includes any medicines you are taking which are available to buy without a prescription, such as herbal and complementary medicines.
  • If you have ever had an allergic reaction to another antihistamine, or to any other medicine.

References

http://patient.info/medicine/mizolastine-tablets-mizollen
https://en.wikipedia.org/wiki/Mizolastine
https://www.ncbi.nlm.nih.gov/pubmed/18020585

Description

Mizolastine was marketed in Germany and Switzerland as Mizollen for the symptomatic relief of seasonal and perennial allergic rhinoconjunctivitis and urticaria. Mizolastine is a new long-acting, orally active antihistaminic agent with a rapid onset of action ; the two most recent H1 antagonists launched were fexofenadine, metabolite of terfenadine (Sepracor, 1996) and Olopatadine (Kyowa Hakko, 1997). Mizolastine can be prepared in 2 steps from 2-chloro 1- (4-fluorobenzyl)benzimidazole by successive condensations of appropriate amine and thioether. Mizolastine selectively blocks the peripheral H1 receptors (but not the serotonergic, noradrenergic, muscarinic receptors) with a minimal occupancy of brain receptors, and therefore does not elicit any sedative effects. Moreover, Mizolastine does not produce cardiac rhythm disorders which have been associated with certain non-sedating antihistamines in humans.

Chemical Properties

White Solid

Originator

Synthelabo (France)

Uses

A highly selective histamine H1-receptor antagonist (with no anticholinergic, antiadrenergic, or antiserotonin activity) for use in the treatment of allergic disorders, especially rhinitis and urticaria.

Uses

Allergic rhinitis;Blocking H1 receptors

Definition

ChEBI: Mizolastine is a member of benzimidazoles.

brand name

Mizollen

Clinical Use

Antihistamine:
Symptomatic relief of allergy, e.g. hayfever, urticaria

Drug interactions

Potentially hazardous interactions with other drugs
Anti-arrhythmics: increased risk of ventricular arrhythmias - avoid with amiodarone, disopyramide, flecainide, mexiletine, procainamide and propafenone.
Antibacterials: metabolism possibly inhibited by macrolides - avoid; increased risk of ventricular arrhythmias with moxifloxacin - avoid.
Antidepressants: risk of ventricular arrhythmias with citalopram and escitalopram - avoid.
Antifungals: metabolism inhibited by itraconazole and ketoconazole and possibly imidazoles - avoid.
Antimalarials: avoid with piperaquine with artenimol.
Antivirals: concentration possibly increased by ritonavir; increased risk of ventricular arrhythmias with saquinavir - avoid.
Beta-blockers: increased risk of ventricular arrhythmias with sotalol - avoid.
Ciclosporin: use with caution due to inhibition of ciclosporin metabolism.
Cytotoxics: possible increased risk of ventricular arrhythmias with vandetanib.
Avoid concomitant treatment with any drug that could prolong QT interval.
Caution with drugs that inhibit cytochrome P450 enzymes (may elevate mizolastine levels)

Metabolism

Mainly metabolised by glucuronidation although other metabolic pathways are involved, including metabolism by the cytochrome P450 isoenzyme CYP3A4, with the formation of inactive hydroxylated metabolites

Mizolastine Preparation Products And Raw materials

Raw materials

Preparation Products

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Mizolastine Suppliers

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View Lastest Price from Mizolastine manufacturers

Hebei Yanxi Chemical Co., Ltd.
Product
Mizolastine 108612-45-9
Price
US $0.00/kg
Min. Order
1kg
Purity
98.0 ~ 102%
Supply Ability
20tons
Release date
2023-09-21
Henan Bao Enluo International TradeCo.，LTD
Product
Mizolastine 108612-45-9
Price
US $100.00/kg
Min. Order
1kg
Purity
99%
Supply Ability
1000tons
Release date
2023-08-02
Zhuozhou Wenxi import and Export Co., Ltd
Product
Mizolastine 108612-45-9
Price
US $15.00-10.00/KG
Min. Order
1KG
Purity
99%+ HPLC
Supply Ability
Monthly supply of 1 ton
Release date
2021-07-10

108612-45-9, MizolastineRelated Search:

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  • 4(1h)-pyrimidinone,2-((1-(1-((4-fluorophenyl)methyl)-1h-benzimidazol-2-yl)-4-p
  • iperidinyl)methylamino)-
  • 2-[[1-[1-[(4-fluorophenyl)methyl]benzoimidazol-2-yl]-4-piperidyl]-methyl-amino]-3h-pyrimidin-4-one
  • MIZOLASTINE
  • 2-[[1-[1-[(4-fluorophenyl)methyl]-1H-benzimidazol-2-yl]-4-piperidinyl]methylamino]-4(1H)-pyrimidinone
  • Mizolastine HCl
  • 2-[[1-[1-(4-fluorobenzyl)benzimidazol-2-yl]-4-piperidyl]-methyl-amino]-1H-pyrimidin-6-one
  • 2-[[1-[1-[(4-fluorophenyl)methyl]benzimidazol-2-yl]piperidin-4-yl]-methyl-amino]-1H-pyrimidin-6-one
  • 2-[[1-[1-[(4-fluorophenyl)methyl]benzimidazol-2-yl]piperidin-4-yl]-methylamino]-1H-pyrimidin-6-one
  • Mizolastine inn
  • 2-[[1-[1-[(4-fluorophenyl)methyl]-2-benzimidazolyl]-4-piperidinyl]-methylamino]-1H-pyrimidin-6-one
  • MistaMine
  • Mizollen
  • MKC 431
  • SL 850324
  • Zolistan
  • 4(3H)-PyriMidinone,2-[[1-[1-[(4-fluorophenyl)Methyl]-1H-benziMidazol-2-yl]-4-piperidinyl]MethylaMino]-
  • 2-((1-(1-(4-Fluorobenzyl)-1H-benzo[d]iMidazol-2-yl)piperidin-4-yl)(Methyl)aMino)pyriMidin-4(1H)-one
  • 2-((1-(1-(4-Fluorobenzyl)-1H-benzo[d]imidazol-2-yl)-piperidin-4-yl)(methyl)amino)pyrimidin-4(1H)-
  • Mizolastine (Mizollen)
  • Mizolastine, >=99%
  • 2-[{1-[1-(4-fluorobenzyl)-1H-benzimidazol-2-yl]piperidin-4-yl}(methyl)amino]pyrimidin-4(1H)-one
  • 2-((1-(1-(4-Fluorobenzyl)-1H-benzo[d]imidazol-2-yl)-piperidin-4-yl)(methyl)amino)pyrimidin-4(1
  • Mizolastine 4(1h)-pyrimidinone,2-((1-(1-((4-fluorophenyl)methyl)-1h-benzimidazol-2-yl)-4-p
  • Mizolastine Mizolastine
  • Mizolastine&gt
  • Mizolastine USP/EP/BP
  • Mizolastine zhou
  • Mizolastine (SL 850324)
  • Mizolastine 108612-45-9
  • 2-[(1-{1-[(4-fluorophenyl)methyl]-1H-1,3-benzodiazol-2-yl}piperidin-4-yl)(methyl)amino]-3,4-dihydropyrimidin-4-one
  • Imimidistine impurity
  • Mizostatin
  • Mizostatin/Mizostatin
  • 108612-45-9
  • C24H25FN6O
  • Other APIs
  • Aromatics
  • Heterocycles
  • Inhibitors
  • Intermediates & Fine Chemicals
  • Pharmaceuticals
  • Antihistaminic
  • APIs