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Details

Stereochemistry ACHIRAL
Molecular Formula C24H25FN6O
Molecular Weight 432.4942
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of MIZOLASTINE

SMILES

CN(C1CCN(CC1)c2nc3ccccc3n2Cc4ccc(cc4)F)c5nccc(n5)O

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)

HIDE SMILES / InChI

Molecular Formula C24H25FN6O
Molecular Weight 432.4942
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Description
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

Curator's Comment:: Mizolastine did not influence on the central nervous system (CNS) at up to 1,500 times the effective dosage

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
47.0 nM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Mizollen

Approved Use

Mizolastine is a long-acting H1 -antihistamine indicated for the symptomatic relief of seasonal allergic rhinoconjunctivitis (hay fever), perennial allergic rhinoconjunctivitis and urticaria.

Launch Date

1.04690883E12
Primary
Mizollen

Approved Use

Mizolastine is a long-acting H1 -antihistamine indicated for the symptomatic relief of seasonal allergic rhinoconjunctivitis (hay fever), perennial allergic rhinoconjunctivitis and urticaria.

Launch Date

1.04690883E12
PubMed

PubMed

TitleDatePubMed
In vivo and in vitro interaction of the novel selective histamine H1 receptor antagonist mizolastine with H1 receptors in the rodent.
1995 May
Mizolastine: a review of its use in allergic rhinitis and chronic idiopathic urticaria.
1998 Jul
Antiallergic effects of H1-receptor antagonists.
2000
Inhibition of HERG1 K(+) channels by the novel second-generation antihistamine mizolastine.
2000 Nov
Cetirizine and loratadine: minimal risk of QT prolongation.
2010 Feb
Patents

Sample Use Guides

10 mg daily was administered for 14 days during the pollen season
Route of Administration: Oral
In Vitro Use Guide
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 Sat Jun 26 05:25:00 UTC 2021
Edited
by admin
on Sat Jun 26 05:25:00 UTC 2021
Record UNII
244O1F90NA
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
MIZOLASTINE
INN   JAN   MART.   MI   WHO-DD  
INN  
Official Name English
MIZOLLEN
Brand Name English
MIZOLASTINE [INN]
Common Name English
MIZOLASTINE [WHO-DD]
Common Name English
MIZOLASTINE [MI]
Common Name English
MIZOLASTINE [MART.]
Common Name English
2-((1-(1-(P-FLUOROBENZYL)-2-BENZIMIDAZOLYL)-4-PIPERIDYL)METHYLAMINO)-4(3H)-PYRIMIDINONE
Common Name English
MIZOLASTINE [JAN]
Common Name English
Classification Tree Code System Code
NCI_THESAURUS C29578
Created by admin on Sat Jun 26 05:25:00 UTC 2021 , Edited by admin on Sat Jun 26 05:25:00 UTC 2021
WHO-ATC R06AX25
Created by admin on Sat Jun 26 05:25:00 UTC 2021 , Edited by admin on Sat Jun 26 05:25:00 UTC 2021
WHO-VATC QR06AX25
Created by admin on Sat Jun 26 05:25:00 UTC 2021 , Edited by admin on Sat Jun 26 05:25:00 UTC 2021
Code System Code Type Description
EVMPD
SUB09018MIG
Created by admin on Sat Jun 26 05:25:00 UTC 2021 , Edited by admin on Sat Jun 26 05:25:00 UTC 2021
PRIMARY
DRUG BANK
DB12523
Created by admin on Sat Jun 26 05:25:00 UTC 2021 , Edited by admin on Sat Jun 26 05:25:00 UTC 2021
PRIMARY
FDA UNII
244O1F90NA
Created by admin on Sat Jun 26 05:25:00 UTC 2021 , Edited by admin on Sat Jun 26 05:25:00 UTC 2021
PRIMARY
MERCK INDEX
M7577
Created by admin on Sat Jun 26 05:25:00 UTC 2021 , Edited by admin on Sat Jun 26 05:25:00 UTC 2021
PRIMARY Merck Index
NCI_THESAURUS
C66171
Created by admin on Sat Jun 26 05:25:00 UTC 2021 , Edited by admin on Sat Jun 26 05:25:00 UTC 2021
PRIMARY
CAS
108612-45-9
Created by admin on Sat Jun 26 05:25:00 UTC 2021 , Edited by admin on Sat Jun 26 05:25:00 UTC 2021
PRIMARY
DRUG CENTRAL
1824
Created by admin on Sat Jun 26 05:25:00 UTC 2021 , Edited by admin on Sat Jun 26 05:25:00 UTC 2021
PRIMARY
PUBCHEM
65906
Created by admin on Sat Jun 26 05:25:00 UTC 2021 , Edited by admin on Sat Jun 26 05:25:00 UTC 2021
PRIMARY
WIKIPEDIA
MIZOLASTINE
Created by admin on Sat Jun 26 05:25:00 UTC 2021 , Edited by admin on Sat Jun 26 05:25:00 UTC 2021
PRIMARY
ChEMBL
CHEMBL94454
Created by admin on Sat Jun 26 05:25:00 UTC 2021 , Edited by admin on Sat Jun 26 05:25:00 UTC 2021
PRIMARY
EPA CompTox
108612-45-9
Created by admin on Sat Jun 26 05:25:00 UTC 2021 , Edited by admin on Sat Jun 26 05:25:00 UTC 2021
PRIMARY
RXCUI
61455
Created by admin on Sat Jun 26 05:25:00 UTC 2021 , Edited by admin on Sat Jun 26 05:25:00 UTC 2021
PRIMARY RxNorm
INN
6663
Created by admin on Sat Jun 26 05:25:00 UTC 2021 , Edited by admin on Sat Jun 26 05:25:00 UTC 2021
PRIMARY
MESH
C076170
Created by admin on Sat Jun 26 05:25:00 UTC 2021 , Edited by admin on Sat Jun 26 05:25:00 UTC 2021
PRIMARY
Related Record Type Details
BINDER->LIGAND
TARGET -> INHIBITOR
Kd
Related Record Type Details
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Biological Half-life PHARMACOKINETIC
Volume of Distribution PHARMACOKINETIC