Introduction：Basic information about CAS 108612-45-9|Mizolastine, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
| Common Name | Mizolastine |
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| CAS Number | 108612-45-9 | Molecular Weight | 432.493 |
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| Density | 1.3±0.1 g/cm3 | Boiling Point | / |
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| Molecular Formula | C24H25FN6O | Melting Point | 217° |
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| MSDS | / | Flash Point | / |
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Names
| Name | 2-((1-(1-(4-Fluorobenzyl)-1H-benzo[d]imidazol-2-yl)piperidin-4-yl)(methyl)amino)pyrimidin-4(1H)-one |
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| Synonym | More Synonyms |
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Mizolastine BiologicalActivity
| Description | Mizolastine is a histamine H1-receptor antagonist with IC50 of 47 nM used in the treatment of hay fever (seasonal allergic rhinitis), hives and other allergic reactions. Target: Histamine H1-receptorMizolastine is a histamine H1-receptor antagonist with IC50 of 47 nM used in the treatment of hay fever (seasonal allergic rhinitis), hives and other allergic reactions. It does not prevent the actual release of histamine from mast cells, just prevents it binding to receptors. Side effects can include dry mouth and throat.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. Available data also suggest that prophylactic administration of mizolastine is significantly more effective than placebo and as effective as prophylactic terfenadine in delaying the onset of symptoms of seasonal allergic rhinitis. |
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| Related Catalog | Signaling Pathways >>GPCR/G Protein >>Histamine ReceptorSignaling Pathways >>Immunology/Inflammation >>Histamine ReceptorResearch Areas >>Inflammation/Immunology |
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| References | [1]. Prakash A, et al. Mizolastine: a review of its use in allergic rhinitis and chronic idiopathic urticaria. BioDrugs. 1998 Jul;10(1):41-63. |
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Chemical & Physical Properties
| Density | 1.3±0.1 g/cm3 |
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| Melting Point | 217° |
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| Molecular Formula | C24H25FN6O |
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| Molecular Weight | 432.493 |
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| Exact Mass | 432.207397 |
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| PSA | 70.05000 |
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| LogP | 3.42 |
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| Index of Refraction | 1.682 |
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| InChIKey | PVLJETXTTWAYEW-UHFFFAOYSA-N |
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| SMILES | CN(c1nccc(=O)[nH]1)C1CCN(c2nc3ccccc3n2Cc2ccc(F)cc2)CC1 |
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Toxicological Information
CHEMICAL IDENTIFICATION - RTECS NUMBER :
- UW7481284
- CHEMICAL NAME :
- 4(1H)-Pyrimidinone, 2-((1-(1-((4-fluorophenyl)methyl)-1H-benzimidazol-2-y l)-4-piperidinyl) methylamino)-
- CAS REGISTRY NUMBER :
- 108612-45-9
- LAST UPDATED :
- 199806
- DATA ITEMS CITED :
- 1
HEALTH HAZARD DATAACUTE TOXICITY DATA - TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Mammal - species unspecified
- DOSE/DURATION :
- >1 gm/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- REFERENCE :
- USXXAM United States Patent Document. (U.S. Patent Office, Box 9, Washington, DC 20231) Volume(issue)/page/year: #4820710
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Safety Information
| RTECS | UW7481284 |
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| HS Code | 2933990090 |
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Customs
| HS Code | 2933990090 |
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| Summary | 2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0% |
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Synonyms
