Details
Stereochemistry | ACHIRAL |
Molecular Formula | C24H25FN6O |
Molecular Weight | 432.4933 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CN(C1CCN(CC1)C2=NC3=C(C=CC=C3)N2CC4=CC=C(F)C=C4)C5=NC=CC(=O)N5
InChI
InChIKey=PVLJETXTTWAYEW-UHFFFAOYSA-N
InChI=1S/C24H25FN6O/c1-29(23-26-13-10-22(32)28-23)19-11-14-30(15-12-19)24-27-20-4-2-3-5-21(20)31(24)16-17-6-8-18(25)9-7-17/h2-10,13,19H,11-12,14-16H2,1H3,(H,26,28,32)
Molecular Formula | C24H25FN6O |
Molecular Weight | 432.4933 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
DescriptionSources: http://www.ncbi.nlm.nih.gov/pubmed/18020585Curator's Comment: description was created based on several sources, including
http://www.medicines.org.uk/emc/medicine/19970/SPC/Mizollen+10+mg+modified-release+tablets
Sources: http://www.ncbi.nlm.nih.gov/pubmed/18020585
Curator's Comment: description was created based on several sources, including
http://www.medicines.org.uk/emc/medicine/19970/SPC/Mizollen+10+mg+modified-release+tablets
Mizolastine (Mizollen) is a long-acting H1 -antihistamine indicated for the symptomatic relief of seasonal allergic rhinoconjunctivitis (hay fever), perennial allergic rhinoconjunctivitis and urticaria. 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. Side effects can include dry mouth and throat
CNS Activity
Sources: https://www.researchgate.net/publication/289165298_Influence_of_mizolastine_on_central_nervous_system
Curator's Comment: Mizolastine did not influence on the central nervous system (CNS) at up to 1,500 times the effective dosage
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
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Target ID: CHEMBL231 Sources: http://www.ncbi.nlm.nih.gov/pubmed/7612054 |
47.0 nM [IC50] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
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Primary | Mizollen Approved UseMizolastine is a long-acting H1 -antihistamine indicated for the symptomatic relief of seasonal allergic rhinoconjunctivitis (hay fever), perennial allergic rhinoconjunctivitis and urticaria. Launch Date2003 |
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Primary | Mizollen Approved UseMizolastine is a long-acting H1 -antihistamine indicated for the symptomatic relief of seasonal allergic rhinoconjunctivitis (hay fever), perennial allergic rhinoconjunctivitis and urticaria. Launch Date2003 |
PubMed
Title | Date | PubMed |
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In vivo and in vitro interaction of the novel selective histamine H1 receptor antagonist mizolastine with H1 receptors in the rodent. | 1995 May |
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Mizolastine: a review of its use in allergic rhinitis and chronic idiopathic urticaria. | 1998 Jul |
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Antiallergic effects of H1-receptor antagonists. | 2000 |
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Inhibition of HERG1 K(+) channels by the novel second-generation antihistamine mizolastine. | 2000 Nov |
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Cetirizine and loratadine: minimal risk of QT prolongation. | 2010 Feb |
Patents
Sample Use Guides
In Vivo Use Guide
Sources: http://www.ncbi.nlm.nih.gov/pubmed/11421924
10 mg daily was administered for 14 days during the pollen season
Route of Administration:
Oral
In Vitro Use Guide
Sources: http://www.ncbi.nlm.nih.gov/pubmed/11060489
The highest dose of mizolastine (6 x 10(-6) M), corresponding to 10-fold the peak plasma level after a single oral administration of 10 mg, was able to act on fibroblasts, significantly downregulating the expression of CD54 (p<0.05). Regarding T lymphocyte proliferation, the addition of mizolastine did not induce any significant change; furthermore, mizolastine was ineffective at all of the tested concentrations on both HLA-DR expression and CD4+/CD8+ ratio.
Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 18:00:42 GMT 2023
by
admin
on
Sat Dec 16 18:00:42 GMT 2023
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Record UNII |
244O1F90NA
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Record Status |
Validated (UNII)
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Record Version |
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Classification Tree | Code System | Code | ||
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NCI_THESAURUS |
C29578
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WHO-ATC |
R06AX25
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WHO-VATC |
QR06AX25
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Code System | Code | Type | Description | ||
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SUB09018MIG
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DB12523
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244O1F90NA
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m7577
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C66171
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108612-45-9
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1824
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65906
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MIZOLASTINE
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CHEMBL94454
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100000080903
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DTXSID5046801
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61455
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6663
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C076170
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TARGET -> INHIBITOR |
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ACTIVE MOIETY |
Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
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Biological Half-life | PHARMACOKINETIC |
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Volume of Distribution | PHARMACOKINETIC |
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